Ethanol
(right click,save link as to download,it is a temp file,please download as soon as possible, you can also use CTRL+S to save the whole html page)
Basic Info
| Common Name | Ethanol(F03879) |
| 2D Structure | |
| Description | Ethanol is a clear, colorless liquid rapidly absorbed from the gastrointestinal tract and distributed throughout the body. It has bactericidal activity and is used often as a topical disinfectant. It is widely used as a solvent and preservative in pharmaceutical preparations as well as serving as the primary ingredient in alcoholic beverages. Indeed, ethanol has widespread use as a solvent of substances intended for human contact or consumption, including scents, flavorings, colorings, and medicines. Ethanol has a depressive effect on the central nervous system and because of its psychoactive effects, it is considered a drug. Ethanol has a complex mode of action and affects multiple systems in the brain, most notably it acts as an agonist to the GABA receptors. Death from ethanol consumption is possible when blood alcohol level reaches 0.4%. A blood level of 0.5% or more is commonly fatal. Levels of even less than 0.1% can cause intoxication, with unconsciousness often occurring at 0.3-0.4 %. Ethanol is metabolized by the body as an energy-providing carbohydrate nutrient, as it metabolizes into acetyl CoA, an intermediate common with glucose metabolism, that can be used for energy in the citric acid cycle or for biosynthesis. Ethanol within the human body is converted into acetaldehyde by alcohol dehydrogenase and then into acetic acid by acetaldehyde dehydrogenase. The product of the first step of this breakdown, acetaldehyde, is more toxic than ethanol. Acetaldehyde is linked to most of the clinical effects of alcohol. It has been shown to increase the risk of developing cirrhosis of the liver,[77] multiple forms of cancer, and alcoholism. Industrially, ethanol is produced both as a petrochemical, through the hydration of ethylene, and biologically, by fermenting sugars with yeast. Small amounts of ethanol are endogenously produced by gut microflora through anaerobic fermentation. However most ethanol detected in biofluids and tissues likely comes from consumption of alcoholic beverages. Absolute ethanol or anhydrous alcohol generally refers to purified ethanol, containing no more than one percent water. Absolute alcohol is not intended for human consumption. It often contains trace amounts of toxic benzene (used to remove water by azeotropic distillation). Consumption of this form of ethanol can be fatal over a short time period. Generally absolute or pure ethanol is used as a solvent for lab and industrial settings where water will disrupt a desired reaction. Pure ethanol is classed as 200 proof in the USA and Canada, equivalent to 175 degrees proof in the UK system. |
| FRCD ID | F03879 |
| CAS Number | 64-17-5 |
| PubChem CID | 702 |
| Formula | C2H6O |
| IUPAC Name | ethanol |
| InChI Key | LFQSCWFLJHTTHZ-UHFFFAOYSA-N |
| InChI | InChI=1S/C2H6O/c1-2-3/h3H,2H2,1H3 |
| Canonical SMILES | CCO |
| Isomeric SMILES | CCO |
| Wikipedia | Ethanol |
| Synonyms |
Methylcarbinol
Algrain
ethanol
ethyl alcohol
alcohol
grain alcohol
64-17-5
Ethyl hydroxide
Ethyl hydrate
Alkohol
|
| Classifies |
Predicted: Pollutant
|
| Update Date | Nov 13, 2018 17:07 |
Chemical Taxonomy
| Kingdom | Organic compounds |
| Superclass | Organic oxygen compounds |
| Class | Organooxygen compounds |
| Subclass | Alcohols and polyols |
| Intermediate Tree Nodes | Not available |
| Direct Parent | Primary alcohols |
| Alternative Parents | |
| Molecular Framework | Aliphatic acyclic compounds |
| Substituents | Hydrocarbon derivative - Primary alcohol - Aliphatic acyclic compound |
| Description | This compound belongs to the class of organic compounds known as primary alcohols. These are compounds comprising the primary alcohol functional group, with the general structure RCOH (R=alkyl, aryl). |
Properties
| Property Name | Property Value |
|---|---|
| Molecular Weight | 46.069 |
| Hydrogen Bond Donor Count | 1 |
| Hydrogen Bond Acceptor Count | 1 |
| Rotatable Bond Count | 0 |
| Complexity | 2.8 |
| Monoisotopic Mass | 46.042 |
| Exact Mass | 46.042 |
| XLogP | -0.1 |
| Formal Charge | 0 |
| Heavy Atom Count | 3 |
| Defined Atom Stereocenter Count | 0 |
| Undefined Atom Stereocenter Count | 0 |
| Defined Bond Stereocenter Count | 0 |
| Undefined Bond Stereocenter Count | 0 |
| Isotope Atom Count | 0 |
| Covalently-Bonded Unit Count | 1 |
ADMET
| Model | Result | Probability |
|---|---|---|
| Absorption | ||
| Blood-Brain Barrier | BBB+ | 0.9539 |
| Human Intestinal Absorption | HIA+ | 0.9948 |
| Caco-2 Permeability | Caco2+ | 0.7260 |
| P-glycoprotein Substrate | Non-substrate | 0.8197 |
| P-glycoprotein Inhibitor | Non-inhibitor | 0.9678 |
| Non-inhibitor | 0.9542 | |
| Renal Organic Cation Transporter | Non-inhibitor | 0.9157 |
| Distribution | ||
| Subcellular localization | Lysosome | 0.6185 |
| Metabolism | ||
| CYP450 2C9 Substrate | Non-substrate | 0.7857 |
| CYP450 2D6 Substrate | Non-substrate | 0.9266 |
| CYP450 3A4 Substrate | Non-substrate | 0.8073 |
| CYP450 1A2 Inhibitor | Non-inhibitor | 0.7260 |
| CYP450 2C9 Inhibitor | Non-inhibitor | 0.9346 |
| CYP450 2D6 Inhibitor | Non-inhibitor | 0.9702 |
| CYP450 2C19 Inhibitor | Non-inhibitor | 0.9296 |
| CYP450 3A4 Inhibitor | Non-inhibitor | 0.9772 |
| CYP Inhibitory Promiscuity | Low CYP Inhibitory Promiscuity | 0.9163 |
| Excretion | ||
| Toxicity | ||
| Human Ether-a-go-go-Related Gene Inhibition | Weak inhibitor | 0.9319 |
| Non-inhibitor | 0.9586 | |
| AMES Toxicity | Non AMES toxic | 0.9132 |
| Carcinogens | Carcinogens | 0.7654 |
| Fish Toxicity | Low FHMT | 0.8123 |
| Tetrahymena Pyriformis Toxicity | Low TPT | 0.9901 |
| Honey Bee Toxicity | High HBT | 0.7896 |
| Biodegradation | Ready biodegradable | 0.9074 |
| Acute Oral Toxicity | III | 0.5323 |
| Carcinogenicity (Three-class) | Non-required | 0.5808 |
| Model | Value | Unit |
|---|---|---|
| Absorption | ||
| Aqueous solubility | 1.0373 | LogS |
| Caco-2 Permeability | 1.3617 | LogPapp, cm/s |
| Distribution | ||
| Metabolism | ||
| Excretion | ||
| Toxicity | ||
| Rat Acute Toxicity | 1.3676 | LD50, mol/kg |
| Fish Toxicity | 4.0125 | pLC50, mg/L |
| Tetrahymena Pyriformis Toxicity | -1.9569 | pIGC50, ug/L |
References
| Title | Journal | Date | Pubmed ID |
|---|---|---|---|
| Determination of diffusion and partition coefficients of model migrants by directcontact and vapour phase transfer from low-density polyethylene films into cake. | Food Addit Contam Part A Chem Anal Control Expo Risk Assess | 2018Mar | 29067891 |
| Effect of a one-off sporidesmin challenge on the milk production of dairy cows. | N Z Vet J | 2018 Sep | 29949719 |
| Expression of Gre2p improves tolerance of engineered xylose-fermenting Saccharomyces cerevisiae to glycolaldehyde under xylose metabolism. | Appl Microbiol Biotechnol | 2018 Sep | 30027490 |
| The protective effects of Sauropus spatulifolius on acute lung injury induced by lipopolysaccharide. | J Sci Food Agric | 2018 Sep | 29460280 |
| Biofilm formation and antimicrobial sensitivity of lactobacilli contaminants fromsugarcane-based fuel ethanol fermentation. | Antonie Van Leeuwenhoek | 2018 Sep | 29478220 |
| Effects of ultrasonic assisted cooking on the chemical profiles of taste andflavor of spiced beef. | Ultrason Sonochem | 2018 Sep | 29739511 |
| Combination of probiotic yeast and lactic acid bacteria as starter culture toproduce maize-based beverages. | Food Res Int | 2018 Sep | 30007675 |
| Biological Characterization of an Edible Species from Brazilian Biodiversity: From Pharmacognostic Data to Ethnopharmacological Investigation. | J Med Food | 2018 Oct 10 | 30307781 |
| Identification of non volatile migrant compounds and NIAS in polypropylene films used as food packaging characterized by UPLC-MS/QTOF. | Talanta | 2018 Oct 1 | 30029443 |
| Structural characteristics and bioactive properties of a novel polysaccharidefrom Flammulina velutipes. | Carbohydr Polym | 2018 Oct 1 | 30007599 |
| Impact of low-dose chronic exposure to bisphenol A and its analogue bisphenol B, bisphenol F and bisphenol S on hypothalamo-pituitary-testicular activities in adult rats: A focus on the possible hormonal mode of action. | Food Chem Toxicol | 2018 Nov | 30120946 |
| Effects of Maillard reaction products in a glucose-glycine alcoholic solution on antioxidative and antimutagenic activities. | J Sci Food Agric | 2018 Nov | 29645274 |
| Simultaneous Preconcentration and Determination of Brilliant Blue and Sunset Yellow in Foodstuffs by Solid-Phase Extraction Combined UV-Vis Spectrophotometry. | J AOAC Int | 2018 May 29 | 29843864 |
| Intestinal HIF-1α deletion exacerbates alcoholic liver disease by inducingintestinal dysbiosis and barrier dysfunction. | J Hepatol | 2018 May 25 | 29803899 |
| Yeast Derived LysA2 Can Control Bacterial Contamination in Ethanol Fermentation. | Viruses | 2018 May 24 | 29795003 |
| Novel Flaxseed Gum Nanocomposites Are Slow Release Iron Supplements. | J Agric Food Chem | 2018 May 23 | 29737167 |
| Green Extraction of Natural Antioxidants from the Sterculia nobilis Fruit Wasteand Analysis of Phenolic Profile. | Molecules | 2018 May 2 | 29724043 |
| Behavior of 11 Foodborne Bacteria on Whole and Cut Mangoes var. Ataulfo and Kent and Antibacterial Activities of Hibiscus sabdariffa Extracts and Chemical Sanitizers Directly onto Mangoes Contaminated with Foodborne Bacteria. | J Food Prot | 2018 May | 29620488 |
| Oolong tea and LR-White resin: a new method of plant sample preparation for transmission electron microscopy. | J Microsc | 2018 May | 29334400 |
| Potential silver nanoparticles migration from commercially available polymeric baby products into food simulants. | Food Addit Contam Part A Chem Anal Control Expo Risk Assess | 2018 May | 29210600 |
Targets
- General Function:
- Ligand-gated ion channel activity
- Specific Function:
- After binding acetylcholine, the AChR responds by an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane.
- Gene Name:
- CHRNA5
- Uniprot ID:
- P30532
- Molecular Weight:
- 53053.965 Da
References
- Dopico AM, Lovinger DM: Acute alcohol action and desensitization of ligand-gated ion channels. Pharmacol Rev. 2009 Mar;61(1):98-114. doi: 10.1124/pr.108.000430. Epub 2009 Mar 6. [19270242 ]
- General Function:
- Inhibitory extracellular ligand-gated ion channel activity
- Specific Function:
- GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
- Gene Name:
- GABRG3
- Uniprot ID:
- Q99928
- Molecular Weight:
- 54288.16 Da
References
- Santhakumar V, Wallner M, Otis TS: Ethanol acts directly on extrasynaptic subtypes of GABAA receptors to increase tonic inhibition. Alcohol. 2007 May;41(3):211-21. [17591544 ]
- General Function:
- Zinc ion binding
- Gene Name:
- ADH1B
- Uniprot ID:
- P00325
- Molecular Weight:
- 39854.21 Da
References
- Hernandez-Tobias A, Julian-Sanchez A, Pina E, Riveros-Rosas H: Natural alcohol exposure: is ethanol the main substrate for alcohol dehydrogenases in animals? Chem Biol Interact. 2011 May 30;191(1-3):14-25. doi: 10.1016/j.cbi.2011.02.008. Epub 2011 Feb 15. [21329681 ]
- General Function:
- Zinc ion binding
- Gene Name:
- ADH1C
- Uniprot ID:
- P00326
- Molecular Weight:
- 39867.27 Da
References
- Hernandez-Tobias A, Julian-Sanchez A, Pina E, Riveros-Rosas H: Natural alcohol exposure: is ethanol the main substrate for alcohol dehydrogenases in animals? Chem Biol Interact. 2011 May 30;191(1-3):14-25. doi: 10.1016/j.cbi.2011.02.008. Epub 2011 Feb 15. [21329681 ]
- General Function:
- Transmitter-gated ion channel activity
- Specific Function:
- The glycine receptor is a neurotransmitter-gated ion channel. Binding of glycine to its receptor increases the chloride conductance and thus produces hyperpolarization (inhibition of neuronal firing).
- Gene Name:
- GLRA1
- Uniprot ID:
- P23415
- Molecular Weight:
- 52623.35 Da
- Mechanism of Action:
- The sedative effects of ethanol are mediated through binding to GABA receptors and glycine receptors (alpha 1 and alpha 2 subunits). In its role as an anti-infective, ethanol acts as an osmolyte or dehydrating agent that disrupts the osmotic balance across cell membranes.
References
- Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [17139284 ]
- General Function:
- Transmitter-gated ion channel activity
- Specific Function:
- The glycine receptor is a neurotransmitter-gated ion channel. Binding of glycine to its receptor increases the chloride conductance and thus produces hyperpolarization (inhibition of neuronal firing).
- Gene Name:
- GLRA2
- Uniprot ID:
- P23416
- Molecular Weight:
- 52001.585 Da
- Mechanism of Action:
- The sedative effects of ethanol are mediated through binding to GABA receptors and glycine receptors (alpha 1 and alpha 2 subunits). In its role as an anti-infective, ethanol acts as an osmolyte or dehydrating agent that disrupts the osmotic balance across cell membranes.
References
- Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [17139284 ]
- General Function:
- Steroid hydroxylase activity
- Specific Function:
- Metabolizes several precarcinogens, drugs, and solvents to reactive metabolites. Inactivates a number of drugs and xenobiotics and also bioactivates many xenobiotic substrates to their hepatotoxic or carcinogenic forms.
- Gene Name:
- CYP2E1
- Uniprot ID:
- P05181
- Molecular Weight:
- 56848.42 Da
- Mechanism of Action:
- Ethanol binds to the ubiquitination site of CYP2E1. Ethanol binds to the enzyme and blocks access to the ubiquitination site by the ubiquitin conjugating system. The ubiquitin binding site is at the substrate binding site of the CYP2E1 enzyme, thus preventing ubiquitin from binding at that site.
References
- Bardag-Gorce F, Li J, French BA, French SW: Ethanol withdrawal induced CYP2E1 degradation in vivo, blocked by proteasomal inhibitor PS-341. Free Radic Biol Med. 2002 Jan 1;32(1):17-21. [11755313 ]
- General Function:
- G-protein activated inward rectifier potassium channel activity
- Specific Function:
- This potassium channel is controlled by G proteins. Inward rectifier potassium channels are characterized by a greater tendency to allow potassium to flow into the cell rather than out of it. Their voltage dependence is regulated by the concentration of extracellular potassium; as external potassium is raised, the voltage range of the channel opening shifts to more positive voltages. The inward rectification is mainly due to the blockage of outward current by internal magnesium. This receptor plays a crucial role in regulating the heartbeat.
- Gene Name:
- KCNJ3
- Uniprot ID:
- P48549
- Molecular Weight:
- 56602.84 Da
References
- Spanagel R: Alcoholism: a systems approach from molecular physiology to addictive behavior. Physiol Rev. 2009 Apr;89(2):649-705. doi: 10.1152/physrev.00013.2008. [19342616 ]
- General Function:
- Inward rectifier potassium channel activity
- Specific Function:
- This potassium channel may be involved in the regulation of insulin secretion by glucose and/or neurotransmitters acting through G-protein-coupled receptors. Inward rectifier potassium channels are characterized by a greater tendency to allow potassium to flow into the cell rather than out of it. Their voltage dependence is regulated by the concentration of extracellular potassium; as external potassium is raised, the voltage range of the channel opening shifts to more positive voltages. The inward rectification is mainly due to the blockage of outward current by internal magnesium.
- Gene Name:
- KCNJ6
- Uniprot ID:
- P48051
- Molecular Weight:
- 48450.96 Da
References
- Spanagel R: Alcoholism: a systems approach from molecular physiology to addictive behavior. Physiol Rev. 2009 Apr;89(2):649-705. doi: 10.1152/physrev.00013.2008. [19342616 ]
- General Function:
- G-protein activated inward rectifier potassium channel activity
- Specific Function:
- This receptor is controlled by G proteins. Inward rectifier potassium channels are characterized by a greater tendency to allow potassium to flow into the cell rather than out of it. Their voltage dependence is regulated by the concentration of extracellular potassium; as external potassium is raised, the voltage range of the channel opening shifts to more positive voltages. The inward rectification is mainly due to the blockage of outward current by internal magnesium (By similarity).
- Gene Name:
- KCNJ9
- Uniprot ID:
- Q92806
- Molecular Weight:
- 44019.45 Da
References
- Spanagel R: Alcoholism: a systems approach from molecular physiology to addictive behavior. Physiol Rev. 2009 Apr;89(2):649-705. doi: 10.1152/physrev.00013.2008. [19342616 ]
- General Function:
- G-protein activated inward rectifier potassium channel activity
- Specific Function:
- This potassium channel is controlled by G proteins. Inward rectifier potassium channels are characterized by a greater tendency to allow potassium to flow into the cell rather than out of it. Their voltage dependence is regulated by the concentration of extracellular potassium; as external potassium is raised, the voltage range of the channel opening shifts to more positive voltages. The inward rectification is mainly due to the blockage of outward current by internal magnesium. Can be blocked by external barium.
- Gene Name:
- KCNJ5
- Uniprot ID:
- P48544
- Molecular Weight:
- 47667.3 Da
References
- Spanagel R: Alcoholism: a systems approach from molecular physiology to addictive behavior. Physiol Rev. 2009 Apr;89(2):649-705. doi: 10.1152/physrev.00013.2008. [19342616 ]
- General Function:
- Inhibitory extracellular ligand-gated ion channel activity
- Specific Function:
- GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
- Gene Name:
- GABRA2
- Uniprot ID:
- P47869
- Molecular Weight:
- 51325.85 Da
References
- Santhakumar V, Wallner M, Otis TS: Ethanol acts directly on extrasynaptic subtypes of GABAA receptors to increase tonic inhibition. Alcohol. 2007 May;41(3):211-21. [17591544 ]
- General Function:
- Inhibitory extracellular ligand-gated ion channel activity
- Specific Function:
- GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
- Gene Name:
- GABRA3
- Uniprot ID:
- P34903
- Molecular Weight:
- 55164.055 Da
References
- Santhakumar V, Wallner M, Otis TS: Ethanol acts directly on extrasynaptic subtypes of GABAA receptors to increase tonic inhibition. Alcohol. 2007 May;41(3):211-21. [17591544 ]
- General Function:
- Inhibitory extracellular ligand-gated ion channel activity
- Specific Function:
- Component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the vertebrate brain. Functions also as histamine receptor and mediates cellular responses to histamine. Functions as receptor for diazepines and various anesthetics, such as pentobarbital; these are bound at a separate allosteric effector binding site. Functions as ligand-gated chloride channel.
- Gene Name:
- GABRB2
- Uniprot ID:
- P47870
- Molecular Weight:
- 59149.895 Da
References
- Santhakumar V, Wallner M, Otis TS: Ethanol acts directly on extrasynaptic subtypes of GABAA receptors to increase tonic inhibition. Alcohol. 2007 May;41(3):211-21. [17591544 ]
- General Function:
- Gaba-gated chloride ion channel activity
- Specific Function:
- Component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the vertebrate brain. Functions also as histamine receptor and mediates cellular responses to histamine. Functions as receptor for diazepines and various anesthetics, such as pentobarbital; these are bound at a separate allosteric effector binding site. Functions as ligand-gated chloride channel.
- Gene Name:
- GABRB3
- Uniprot ID:
- P28472
- Molecular Weight:
- 54115.04 Da
References
- Santhakumar V, Wallner M, Otis TS: Ethanol acts directly on extrasynaptic subtypes of GABAA receptors to increase tonic inhibition. Alcohol. 2007 May;41(3):211-21. [17591544 ]
- General Function:
- Gaba-a receptor activity
- Specific Function:
- GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
- Gene Name:
- GABRD
- Uniprot ID:
- O14764
- Molecular Weight:
- 50707.835 Da
References
- Santhakumar V, Wallner M, Otis TS: Ethanol acts directly on extrasynaptic subtypes of GABAA receptors to increase tonic inhibition. Alcohol. 2007 May;41(3):211-21. [17591544 ]
- General Function:
- Inhibitory extracellular ligand-gated ion channel activity
- Specific Function:
- GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
- Gene Name:
- GABRE
- Uniprot ID:
- P78334
- Molecular Weight:
- 57971.175 Da
References
- Santhakumar V, Wallner M, Otis TS: Ethanol acts directly on extrasynaptic subtypes of GABAA receptors to increase tonic inhibition. Alcohol. 2007 May;41(3):211-21. [17591544 ]
- General Function:
- Inhibitory extracellular ligand-gated ion channel activity
- Specific Function:
- GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
- Gene Name:
- GABRG1
- Uniprot ID:
- Q8N1C3
- Molecular Weight:
- 53594.49 Da
References
- Santhakumar V, Wallner M, Otis TS: Ethanol acts directly on extrasynaptic subtypes of GABAA receptors to increase tonic inhibition. Alcohol. 2007 May;41(3):211-21. [17591544 ]
- General Function:
- Gaba-a receptor activity
- Specific Function:
- GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel. In the uterus, the function of the receptor appears to be related to tissue contractility. The binding of this pI subunit with other GABA(A) receptor subunits alters the sensitivity of recombinant receptors to modulatory agents such as pregnanolone.
- Gene Name:
- GABRP
- Uniprot ID:
- O00591
- Molecular Weight:
- 50639.735 Da
References
- Santhakumar V, Wallner M, Otis TS: Ethanol acts directly on extrasynaptic subtypes of GABAA receptors to increase tonic inhibition. Alcohol. 2007 May;41(3):211-21. [17591544 ]
- General Function:
- Receptor binding
- Specific Function:
- Ionotropic receptor with a probable role in the modulation of auditory stimuli. Agonist binding may induce an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane. The channel is permeable to a range of divalent cations including calcium, the influx of which may activate a potassium current which hyperpolarizes the cell membrane. In the ear, this may lead to a reduction in basilar membrane motion, altering the activity of auditory nerve fibers and reducing the range of dynamic hearing. This may protect against acoustic trauma.
- Gene Name:
- CHRNA10
- Uniprot ID:
- Q9GZZ6
- Molecular Weight:
- 49704.295 Da
References
- Dopico AM, Lovinger DM: Acute alcohol action and desensitization of ligand-gated ion channels. Pharmacol Rev. 2009 Mar;61(1):98-114. doi: 10.1124/pr.108.000430. Epub 2009 Mar 6. [19270242 ]
- General Function:
- Drug binding
- Specific Function:
- After binding acetylcholine, the AChR responds by an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane.
- Gene Name:
- CHRNA2
- Uniprot ID:
- Q15822
- Molecular Weight:
- 59764.82 Da
References
- Dopico AM, Lovinger DM: Acute alcohol action and desensitization of ligand-gated ion channels. Pharmacol Rev. 2009 Mar;61(1):98-114. doi: 10.1124/pr.108.000430. Epub 2009 Mar 6. [19270242 ]
- General Function:
- Ligand-gated ion channel activity
- Specific Function:
- After binding acetylcholine, the AChR responds by an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane.
- Gene Name:
- CHRNA3
- Uniprot ID:
- P32297
- Molecular Weight:
- 57479.54 Da
References
- Dopico AM, Lovinger DM: Acute alcohol action and desensitization of ligand-gated ion channels. Pharmacol Rev. 2009 Mar;61(1):98-114. doi: 10.1124/pr.108.000430. Epub 2009 Mar 6. [19270242 ]
- General Function:
- Ligand-gated ion channel activity
- Specific Function:
- After binding acetylcholine, the AChR responds by an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane permeable to sodium ions.
- Gene Name:
- CHRNA4
- Uniprot ID:
- P43681
- Molecular Weight:
- 69956.47 Da
References
- Dopico AM, Lovinger DM: Acute alcohol action and desensitization of ligand-gated ion channels. Pharmacol Rev. 2009 Mar;61(1):98-114. doi: 10.1124/pr.108.000430. Epub 2009 Mar 6. [19270242 ]
- General Function:
- Toxic substance binding
- Specific Function:
- After binding acetylcholine, the AChR responds by an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane. The channel is blocked by alpha-bungarotoxin.
- Gene Name:
- CHRNA7
- Uniprot ID:
- P36544
- Molecular Weight:
- 56448.925 Da
References
- Dopico AM, Lovinger DM: Acute alcohol action and desensitization of ligand-gated ion channels. Pharmacol Rev. 2009 Mar;61(1):98-114. doi: 10.1124/pr.108.000430. Epub 2009 Mar 6. [19270242 ]
- General Function:
- Ligand-gated ion channel activity
- Specific Function:
- After binding acetylcholine, the AChR responds by an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane permeable to sodiun ions.
- Gene Name:
- CHRNB2
- Uniprot ID:
- P17787
- Molecular Weight:
- 57018.575 Da
References
- Dopico AM, Lovinger DM: Acute alcohol action and desensitization of ligand-gated ion channels. Pharmacol Rev. 2009 Mar;61(1):98-114. doi: 10.1124/pr.108.000430. Epub 2009 Mar 6. [19270242 ]
- General Function:
- Drug binding
- Specific Function:
- After binding acetylcholine, the AChR responds by an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane.
- Gene Name:
- CHRNB3
- Uniprot ID:
- Q05901
- Molecular Weight:
- 52728.215 Da
References
- Dopico AM, Lovinger DM: Acute alcohol action and desensitization of ligand-gated ion channels. Pharmacol Rev. 2009 Mar;61(1):98-114. doi: 10.1124/pr.108.000430. Epub 2009 Mar 6. [19270242 ]
- General Function:
- Ligand-gated ion channel activity
- Specific Function:
- After binding acetylcholine, the AChR responds by an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane.
- Gene Name:
- CHRNB4
- Uniprot ID:
- P30926
- Molecular Weight:
- 56378.985 Da
References
- Dopico AM, Lovinger DM: Acute alcohol action and desensitization of ligand-gated ion channels. Pharmacol Rev. 2009 Mar;61(1):98-114. doi: 10.1124/pr.108.000430. Epub 2009 Mar 6. [19270242 ]
- General Function:
- Voltage-gated potassium channel activity
- Specific Function:
- This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. This receptor is a ligand-gated ion channel, which when activated causes fast, depolarizing responses in neurons. It is a cation-specific, but otherwise relatively nonselective, ion channel.
- Gene Name:
- HTR3A
- Uniprot ID:
- P46098
- Molecular Weight:
- 55279.835 Da
References
- Dopico AM, Lovinger DM: Acute alcohol action and desensitization of ligand-gated ion channels. Pharmacol Rev. 2009 Mar;61(1):98-114. doi: 10.1124/pr.108.000430. Epub 2009 Mar 6. [19270242 ]
- General Function:
- Serotonin-activated cation-selective channel activity
- Specific Function:
- This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. This receptor is a ligand-gated ion channel, which when activated causes fast, depolarizing responses. It is a cation-specific, but otherwise relatively nonselective, ion channel.
- Gene Name:
- HTR3B
- Uniprot ID:
- O95264
- Molecular Weight:
- 50291.3 Da
References
- Dopico AM, Lovinger DM: Acute alcohol action and desensitization of ligand-gated ion channels. Pharmacol Rev. 2009 Mar;61(1):98-114. doi: 10.1124/pr.108.000430. Epub 2009 Mar 6. [19270242 ]
- General Function:
- Serotonin-activated cation-selective channel activity
- Specific Function:
- This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. This receptor is a ligand-gated ion channel, which when activated causes fast, depolarizing responses. It is a cation-specific, but otherwise relatively nonselective, ion channel.
- Gene Name:
- HTR3C
- Uniprot ID:
- Q8WXA8
- Molecular Weight:
- 50219.07 Da
References
- Dopico AM, Lovinger DM: Acute alcohol action and desensitization of ligand-gated ion channels. Pharmacol Rev. 2009 Mar;61(1):98-114. doi: 10.1124/pr.108.000430. Epub 2009 Mar 6. [19270242 ]
- General Function:
- Serotonin-activated cation-selective channel activity
- Specific Function:
- This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. This receptor is a ligand-gated ion channel, which when activated causes fast, depolarizing responses. It is a cation-specific, but otherwise relatively nonselective, ion channel.
- Gene Name:
- HTR3D
- Uniprot ID:
- Q70Z44
- Molecular Weight:
- 50190.625 Da
References
- Dopico AM, Lovinger DM: Acute alcohol action and desensitization of ligand-gated ion channels. Pharmacol Rev. 2009 Mar;61(1):98-114. doi: 10.1124/pr.108.000430. Epub 2009 Mar 6. [19270242 ]
- General Function:
- Serotonin-activated cation-selective channel activity
- Specific Function:
- This is one of the several different receptors for 5-hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. This receptor is a ligand-gated ion channel, which when activated causes fast, depolarizing responses. It is a cation-specific, but otherwise relatively nonselective, ion channel.
- Gene Name:
- HTR3E
- Uniprot ID:
- A5X5Y0
- Molecular Weight:
- 51437.415 Da
References
- Dopico AM, Lovinger DM: Acute alcohol action and desensitization of ligand-gated ion channels. Pharmacol Rev. 2009 Mar;61(1):98-114. doi: 10.1124/pr.108.000430. Epub 2009 Mar 6. [19270242 ]
- General Function:
- Zinc ion binding
- Gene Name:
- ADH4
- Uniprot ID:
- P08319
- Molecular Weight:
- 40221.335 Da
References
- Lee SL, Chau GY, Yao CT, Wu CW, Yin SJ: Functional assessment of human alcohol dehydrogenase family in ethanol metabolism: significance of first-pass metabolism. Alcohol Clin Exp Res. 2006 Jul;30(7):1132-42. [16792560 ]
- General Function:
- Zinc ion binding
- Gene Name:
- ADH6
- Uniprot ID:
- P28332
- Molecular Weight:
- 39088.335 Da
References
- Lee SL, Chau GY, Yao CT, Wu CW, Yin SJ: Functional assessment of human alcohol dehydrogenase family in ethanol metabolism: significance of first-pass metabolism. Alcohol Clin Exp Res. 2006 Jul;30(7):1132-42. [16792560 ]
- General Function:
- Zinc ion binding
- Specific Function:
- Could function in retinol oxidation for the synthesis of retinoic acid, a hormone important for cellular differentiation. Medium-chain (octanol) and aromatic (m-nitrobenzaldehyde) compounds are the best substrates. Ethanol is not a good substrate but at the high ethanol concentrations reached in the digestive tract, it plays a role in the ethanol oxidation and contributes to the first pass ethanol metabolism.
- Gene Name:
- ADH7
- Uniprot ID:
- P40394
- Molecular Weight:
- 41480.985 Da
References
- Lee SL, Chau GY, Yao CT, Wu CW, Yin SJ: Functional assessment of human alcohol dehydrogenase family in ethanol metabolism: significance of first-pass metabolism. Alcohol Clin Exp Res. 2006 Jul;30(7):1132-42. [16792560 ]
- General Function:
- Zinc ion binding
- Specific Function:
- Class-III ADH is remarkably ineffective in oxidizing ethanol, but it readily catalyzes the oxidation of long-chain primary alcohols and the oxidation of S-(hydroxymethyl) glutathione.
- Gene Name:
- ADH5
- Uniprot ID:
- P11766
- Molecular Weight:
- 39723.945 Da
References
- Lee SL, Chau GY, Yao CT, Wu CW, Yin SJ: Functional assessment of human alcohol dehydrogenase family in ethanol metabolism: significance of first-pass metabolism. Alcohol Clin Exp Res. 2006 Jul;30(7):1132-42. [16792560 ]
- General Function:
- Vitamin d 24-hydroxylase activity
- Specific Function:
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics.
- Gene Name:
- CYP1A1
- Uniprot ID:
- P04798
- Molecular Weight:
- 58164.815 Da
References
- Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [19934256 ]
- General Function:
- Oxidoreductase activity, acting on paired donors, with incorporation or reduction of molecular oxygen, reduced flavin or flavoprotein as one donor, and incorporation of one atom of oxygen
- Specific Function:
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N3-demethylation. Also acts in the metabolism of aflatoxin B1 and acetaminophen. Participates in the bioactivation of carcinogenic aromatic and heterocyclic amines. Catalizes the N-hydroxylation of heterocyclic amines and the O-deethylation of phenacetin.
- Gene Name:
- CYP1A2
- Uniprot ID:
- P05177
- Molecular Weight:
- 58293.76 Da
References
- Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [19934256 ]
- General Function:
- Steroid hydroxylase activity
- Specific Function:
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Acts as a 1,4-cineole 2-exo-monooxygenase.
- Gene Name:
- CYP2B6
- Uniprot ID:
- P20813
- Molecular Weight:
- 56277.81 Da
References
- Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [19934256 ]
- General Function:
- Steroid hydroxylase activity
- Specific Function:
- Responsible for the metabolism of a number of therapeutic agents such as the anticonvulsant drug S-mephenytoin, omeprazole, proguanil, certain barbiturates, diazepam, propranolol, citalopram and imipramine.
- Gene Name:
- CYP2C19
- Uniprot ID:
- P33261
- Molecular Weight:
- 55930.545 Da
References
- Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [19934256 ]
- General Function:
- Steroid hydroxylase activity
- Specific Function:
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. This enzyme contributes to the wide pharmacokinetics variability of the metabolism of drugs such as S-warfarin, diclofenac, phenytoin, tolbutamide and losartan.
- Gene Name:
- CYP2C9
- Uniprot ID:
- P11712
- Molecular Weight:
- 55627.365 Da
References
- Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [19934256 ]
- General Function:
- Vitamin d3 25-hydroxylase activity
- Specific Function:
- Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4-hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Acts as a 1,8-cineole 2-exo-monooxygenase. The enzyme also hydroxylates etoposide (PubMed:11159812). Catalyzes 4-beta-hydroxylation of cholesterol. May catalyze 25-hydroxylation of cholesterol in vitro (PubMed:21576599).
- Gene Name:
- CYP3A4
- Uniprot ID:
- P08684
- Molecular Weight:
- 57342.67 Da
References
- Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [19934256 ]
- General Function:
- Nucleoside transmembrane transporter activity
- Specific Function:
- Mediates both influx and efflux of nucleosides across the membrane (equilibrative transporter). It is sensitive (ES) to low concentrations of the inhibitor nitrobenzylmercaptopurine riboside (NBMPR) and is sodium-independent. It has a higher affinity for adenosine. Inhibited by dipyridamole and dilazep (anticancer chemotherapeutics drugs).
- Gene Name:
- SLC29A1
- Uniprot ID:
- Q99808
- Molecular Weight:
- 50218.805 Da
References
- Allen-Gipson DS, Jarrell JC, Bailey KL, Robinson JE, Kharbanda KK, Sisson JH, Wyatt TA: Ethanol blocks adenosine uptake via inhibiting the nucleoside transport system in bronchial epithelial cells. Alcohol Clin Exp Res. 2009 May;33(5):791-8. doi: 10.1111/j.1530-0277.2009.00897.x. Epub 2009 Mar 6. [19298329 ]
- General Function:
- Nucleoside transmembrane transporter activity
- Specific Function:
- Mediates equilibrative transport of purine, pyrimidine nucleosides and the purine base hypoxanthine. Very less sensitive than SLC29A1 to inhibition by nitrobenzylthioinosine (NBMPR), dipyridamole, dilazep and draflazine.
- Gene Name:
- SLC29A2
- Uniprot ID:
- Q14542
- Molecular Weight:
- 50112.335 Da
References
- Allen-Gipson DS, Jarrell JC, Bailey KL, Robinson JE, Kharbanda KK, Sisson JH, Wyatt TA: Ethanol blocks adenosine uptake via inhibiting the nucleoside transport system in bronchial epithelial cells. Alcohol Clin Exp Res. 2009 May;33(5):791-8. doi: 10.1111/j.1530-0277.2009.00897.x. Epub 2009 Mar 6. [19298329 ]
- General Function:
- Ionotropic glutamate receptor activity
- Specific Function:
- Receptor for glutamate that functions as ligand-gated ion channel in the central nervous system and plays an important role in excitatory synaptic transmission. L-glutamate acts as an excitatory neurotransmitter at many synapses in the central nervous system. Binding of the excitatory neurotransmitter L-glutamate induces a conformation change, leading to the opening of the cation channel, and thereby converts the chemical signal to an electrical impulse. The receptor then desensitizes rapidly and enters a transient inactive state, characterized by the presence of bound agonist. In the presence of CACNG4 or CACNG7 or CACNG8, shows resensitization which is characterized by a delayed accumulation of current flux upon continued application of glutamate.
- Gene Name:
- GRIA2
- Uniprot ID:
- P42262
- Molecular Weight:
- 98820.32 Da
References
- Dopico AM, Lovinger DM: Acute alcohol action and desensitization of ligand-gated ion channels. Pharmacol Rev. 2009 Mar;61(1):98-114. doi: 10.1124/pr.108.000430. Epub 2009 Mar 6. [19270242 ]
- General Function:
- Extracellular-glutamate-gated ion channel activity
- Specific Function:
- Receptor for glutamate that functions as ligand-gated ion channel in the central nervous system and plays an important role in excitatory synaptic transmission. L-glutamate acts as an excitatory neurotransmitter at many synapses in the central nervous system. Binding of the excitatory neurotransmitter L-glutamate induces a conformation change, leading to the opening of the cation channel, and thereby converts the chemical signal to an electrical impulse. The receptor then desensitizes rapidly and enters a transient inactive state, characterized by the presence of bound agonist. In the presence of CACNG4 or CACNG7 or CACNG8, shows resensitization which is characterized by a delayed accumulation of current flux upon continued application of glutamate.
- Gene Name:
- GRIA3
- Uniprot ID:
- P42263
- Molecular Weight:
- 101155.975 Da
References
- Dopico AM, Lovinger DM: Acute alcohol action and desensitization of ligand-gated ion channels. Pharmacol Rev. 2009 Mar;61(1):98-114. doi: 10.1124/pr.108.000430. Epub 2009 Mar 6. [19270242 ]
- General Function:
- Ionotropic glutamate receptor activity
- Specific Function:
- Receptor for glutamate that functions as ligand-gated ion channel in the central nervous system and plays an important role in excitatory synaptic transmission. L-glutamate acts as an excitatory neurotransmitter at many synapses in the central nervous system. Binding of the excitatory neurotransmitter L-glutamate induces a conformation change, leading to the opening of the cation channel, and thereby converts the chemical signal to an electrical impulse. The receptor then desensitizes rapidly and enters a transient inactive state, characterized by the presence of bound agonist. In the presence of CACNG4 or CACNG7 or CACNG8, shows resensitization which is characterized by a delayed accumulation of current flux upon continued application of glutamate.
- Gene Name:
- GRIA4
- Uniprot ID:
- P48058
- Molecular Weight:
- 100870.085 Da
References
- Dopico AM, Lovinger DM: Acute alcohol action and desensitization of ligand-gated ion channels. Pharmacol Rev. 2009 Mar;61(1):98-114. doi: 10.1124/pr.108.000430. Epub 2009 Mar 6. [19270242 ]
- General Function:
- Primary amine oxidase activity
- Specific Function:
- Important in cell-cell recognition. Appears to function in leukocyte-endothelial cell adhesion. Interacts with integrin alpha-4/beta-1 (ITGA4/ITGB1) on leukocytes, and mediates both adhesion and signal transduction. The VCAM1/ITGA4/ITGB1 interaction may play a pathophysiologic role both in immune responses and in leukocyte emigration to sites of inflammation.
- Gene Name:
- VCAM1
- Uniprot ID:
- P19320
- Molecular Weight:
- 81275.43 Da
References
- Arevalo E, Shanmugasundararaj S, Wilkemeyer MF, Dou X, Chen S, Charness ME, Miller KW: An alcohol binding site on the neural cell adhesion molecule L1. Proc Natl Acad Sci U S A. 2008 Jan 8;105(1):371-5. doi: 10.1073/pnas.0707815105. Epub 2007 Dec 28. [18165316 ]
- General Function:
- Voltage-gated calcium channel activity involved sa node cell action potential
- Specific Function:
- Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hormone or neurotransmitter release, gene expression, cell motility, cell division and cell death. The isoform alpha-1D gives rise to L-type calcium currents. Long-lasting (L-type) calcium channels belong to the 'high-voltage activated' (HVA) group. They are blocked by dihydropyridines (DHP), phenylalkylamines, benzothiazepines, and by omega-agatoxin-IIIA (omega-Aga-IIIA). They are however insensitive to omega-conotoxin-GVIA (omega-CTx-GVIA) and omega-agatoxin-IVA (omega-Aga-IVA).
- Gene Name:
- CACNA1D
- Uniprot ID:
- Q01668
- Molecular Weight:
- 245138.75 Da
References
- Hendricson AW, Thomas MP, Lippmann MJ, Morrisett RA: Suppression of L-type voltage-gated calcium channel-dependent synaptic plasticity by ethanol: analysis of miniature synaptic currents and dendritic calcium transients. J Pharmacol Exp Ther. 2003 Nov;307(2):550-8. Epub 2003 Sep 11. [12970385 ]
- General Function:
- Voltage-gated calcium channel activity
- Specific Function:
- Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hormone or neurotransmitter release, gene expression, cell motility, cell division and cell death. The isoform alpha-1S gives rise to L-type calcium currents. Long-lasting (L-type) calcium channels belong to the 'high-voltage activated' (HVA) group. They are blocked by dihydropyridines (DHP), phenylalkylamines, benzothiazepines, and by omega-agatoxin-IIIA (omega-Aga-IIIA). They are however insensitive to omega-conotoxin-GVIA (omega-CTx-GVIA) and omega-agatoxin-IVA (omega-Aga-IVA). Calcium channels containing the alpha-1S subunit play an important role in excitation-contraction coupling in skeletal muscle.
- Gene Name:
- CACNA1S
- Uniprot ID:
- Q13698
- Molecular Weight:
- 212348.1 Da
References
- Hendricson AW, Thomas MP, Lippmann MJ, Morrisett RA: Suppression of L-type voltage-gated calcium channel-dependent synaptic plasticity by ethanol: analysis of miniature synaptic currents and dendritic calcium transients. J Pharmacol Exp Ther. 2003 Nov;307(2):550-8. Epub 2003 Sep 11. [12970385 ]
- General Function:
- Voltage-gated calcium channel activity
- Specific Function:
- The beta subunit of voltage-dependent calcium channels contributes to the function of the calcium channel by increasing peak calcium current, shifting the voltage dependencies of activation and inactivation, modulating G protein inhibition and controlling the alpha-1 subunit membrane targeting.
- Gene Name:
- CACNB1
- Uniprot ID:
- Q02641
- Molecular Weight:
- 65712.995 Da
References
- Hendricson AW, Thomas MP, Lippmann MJ, Morrisett RA: Suppression of L-type voltage-gated calcium channel-dependent synaptic plasticity by ethanol: analysis of miniature synaptic currents and dendritic calcium transients. J Pharmacol Exp Ther. 2003 Nov;307(2):550-8. Epub 2003 Sep 11. [12970385 ]
- General Function:
- Voltage-gated calcium channel activity
- Specific Function:
- This protein is a subunit of the dihydropyridine (DHP) sensitive calcium channel. Plays a role in excitation-contraction coupling. The skeletal muscle DHP-sensitive Ca(2+) channel may function only as a multiple subunit complex.
- Gene Name:
- CACNG1
- Uniprot ID:
- Q06432
- Molecular Weight:
- 25028.105 Da
References
- Hendricson AW, Thomas MP, Lippmann MJ, Morrisett RA: Suppression of L-type voltage-gated calcium channel-dependent synaptic plasticity by ethanol: analysis of miniature synaptic currents and dendritic calcium transients. J Pharmacol Exp Ther. 2003 Nov;307(2):550-8. Epub 2003 Sep 11. [12970385 ]
- General Function:
- Transmembrane signaling receptor activity
- Specific Function:
- GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
- Gene Name:
- GABRQ
- Uniprot ID:
- Q9UN88
- Molecular Weight:
- 72020.875 Da
References
- Santhakumar V, Wallner M, Otis TS: Ethanol acts directly on extrasynaptic subtypes of GABAA receptors to increase tonic inhibition. Alcohol. 2007 May;41(3):211-21. [17591544 ]
- General Function:
- Voltage-gated calcium channel activity
- Specific Function:
- Regulates the trafficking and gating properties of AMPA-selective glutamate receptors (AMPARs). Promotes their targeting to the cell membrane and synapses and modulates their gating properties by slowing their rates of activation, deactivation and desensitization. Does not show subunit-specific AMPA receptor regulation and regulates all AMPAR subunits. Thought to stabilize the calcium channel in an inactivated (closed) state.
- Gene Name:
- CACNG2
- Uniprot ID:
- Q9Y698
- Molecular Weight:
- 35965.44 Da
References
- Hendricson AW, Thomas MP, Lippmann MJ, Morrisett RA: Suppression of L-type voltage-gated calcium channel-dependent synaptic plasticity by ethanol: analysis of miniature synaptic currents and dendritic calcium transients. J Pharmacol Exp Ther. 2003 Nov;307(2):550-8. Epub 2003 Sep 11. [12970385 ]
- General Function:
- Inhibitory extracellular ligand-gated ion channel activity
- Specific Function:
- GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
- Gene Name:
- GABRA4
- Uniprot ID:
- P48169
- Molecular Weight:
- 61622.645 Da
References
- Santhakumar V, Wallner M, Otis TS: Ethanol acts directly on extrasynaptic subtypes of GABAA receptors to increase tonic inhibition. Alcohol. 2007 May;41(3):211-21. [17591544 ]
- General Function:
- Transporter activity
- Specific Function:
- GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
- Gene Name:
- GABRA5
- Uniprot ID:
- P31644
- Molecular Weight:
- 52145.645 Da
References
- Santhakumar V, Wallner M, Otis TS: Ethanol acts directly on extrasynaptic subtypes of GABAA receptors to increase tonic inhibition. Alcohol. 2007 May;41(3):211-21. [17591544 ]
- General Function:
- Zinc ion binding
- Gene Name:
- ADH1A
- Uniprot ID:
- P07327
- Molecular Weight:
- 39858.37 Da
References
- Hernandez-Tobias A, Julian-Sanchez A, Pina E, Riveros-Rosas H: Natural alcohol exposure: is ethanol the main substrate for alcohol dehydrogenases in animals? Chem Biol Interact. 2011 May 30;191(1-3):14-25. doi: 10.1016/j.cbi.2011.02.008. Epub 2011 Feb 15. [21329681 ]
- General Function:
- Inhibitory extracellular ligand-gated ion channel activity
- Specific Function:
- GABA, the major inhibitory neurotransmitter in the vertebrate brain, mediates neuronal inhibition by binding to the GABA/benzodiazepine receptor and opening an integral chloride channel.
- Gene Name:
- GABRA6
- Uniprot ID:
- Q16445
- Molecular Weight:
- 51023.69 Da
References
- Santhakumar V, Wallner M, Otis TS: Ethanol acts directly on extrasynaptic subtypes of GABAA receptors to increase tonic inhibition. Alcohol. 2007 May;41(3):211-21. [17591544 ]
- General Function:
- Inhibitory extracellular ligand-gated ion channel activity
- Specific Function:
- Component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the vertebrate brain. Functions also as histamine receptor and mediates cellular responses to histamine. Functions as receptor for diazepines and various anesthetics, such as pentobarbital; these are bound at a separate allosteric effector binding site. Functions as ligand-gated chloride channel (By similarity).
- Gene Name:
- GABRA1
- Uniprot ID:
- P14867
- Molecular Weight:
- 51801.395 Da
- Mechanism of Action:
- The sedative effects of ethanol are mediated through binding to GABA receptors and glycine receptors (alpha 1 and alpha 2 subunits). In its role as an anti-infective, ethanol acts as an osmolyte or dehydrating agent that disrupts the osmotic balance across cell membranes.
References
- Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [17139284 ]
- General Function:
- Protein phosphatase 2a binding
- Specific Function:
- NMDA receptor subtype of glutamate-gated ion channels with reduced single-channel conductance, low calcium permeability and low voltage-dependent sensitivity to magnesium. Mediated by glycine. May play a role in the development of dendritic spines. May play a role in PPP2CB-NMDAR mediated signaling mechanism (By similarity).
- Gene Name:
- GRIN3A
- Uniprot ID:
- Q8TCU5
- Molecular Weight:
- 125464.07 Da
- Mechanism of Action:
- The sedative effects of ethanol are mediated through binding to GABA receptors and glycine receptors (alpha 1 and alpha 2 subunits). In its role as an anti-infective, ethanol acts as an osmolyte or dehydrating agent that disrupts the osmotic balance across cell membranes.
References
- Overington JP, Al-Lazikani B, Hopkins AL: How many drug targets are there? Nat Rev Drug Discov. 2006 Dec;5(12):993-6. [17139284 ]
- General Function:
- Ligand-gated ion channel activity
- Specific Function:
- Component of the heteropentameric receptor for GABA, the major inhibitory neurotransmitter in the vertebrate brain. Functions also as histamine receptor and mediates cellular responses to histamine. Functions as receptor for diazepines and various anesthetics, such as pentobarbital; these are bound at a separate allosteric effector binding site. Functions as ligand-gated chloride channel (By similarity).
- Gene Name:
- GABRB1
- Uniprot ID:
- P18505
- Molecular Weight:
- 54234.085 Da
References
- Santhakumar V, Wallner M, Otis TS: Ethanol acts directly on extrasynaptic subtypes of GABAA receptors to increase tonic inhibition. Alcohol. 2007 May;41(3):211-21. [17591544 ]
- General Function:
- Acetylcholine-activated cation-selective channel activity
- Specific Function:
- After binding acetylcholine, the AChR responds by an extensive change in conformation that affects all subunits and leads to opening of an ion-conducting channel across the plasma membrane.
- Gene Name:
- CHRNA6
- Uniprot ID:
- Q15825
- Molecular Weight:
- 56897.745 Da
References
- Dopico AM, Lovinger DM: Acute alcohol action and desensitization of ligand-gated ion channels. Pharmacol Rev. 2009 Mar;61(1):98-114. doi: 10.1124/pr.108.000430. Epub 2009 Mar 6. [19270242 ]
- General Function:
- Calcium channel activity
- Specific Function:
- Ionotropic receptor with a probable role in the modulation of auditory stimuli. Agonist binding induces a conformation change that leads to the opening of an ion-conducting channel across the plasma membrane (PubMed:11752216, PubMed:25282151). The channel is permeable to a range of divalent cations including calcium, the influx of which may activate a potassium current which hyperpolarizes the cell membrane (PubMed:11752216, PubMed:25282151). In the ear, this may lead to a reduction in basilar membrane motion, altering the activity of auditory nerve fibers and reducing the range of dynamic hearing. This may protect against acoustic trauma. May also regulate keratinocyte adhesion (PubMed:11021840).
- Gene Name:
- CHRNA9
- Uniprot ID:
- Q9UGM1
- Molecular Weight:
- 54806.63 Da
References
- Dopico AM, Lovinger DM: Acute alcohol action and desensitization of ligand-gated ion channels. Pharmacol Rev. 2009 Mar;61(1):98-114. doi: 10.1124/pr.108.000430. Epub 2009 Mar 6. [19270242 ]
- General Function:
- L-glucuronate reductase activity
- Specific Function:
- Catalyzes the NADPH-dependent reduction of a variety of aromatic and aliphatic aldehydes to their corresponding alcohols. Catalyzes the reduction of mevaldate to mevalonic acid and of glyceraldehyde to glycerol. Has broad substrate specificity. In vitro substrates include succinic semialdehyde, 4-nitrobenzaldehyde, 1,2-naphthoquinone, methylglyoxal, and D-glucuronic acid. Plays a role in the activation of procarcinogens, such as polycyclic aromatic hydrocarbon trans-dihydrodiols, and in the metabolism of various xenobiotics and drugs, including the anthracyclines doxorubicin (DOX) and daunorubicin (DAUN).
- Gene Name:
- AKR1A1
- Uniprot ID:
- P14550
- Molecular Weight:
- 36572.71 Da
References
- Lee SL, Chau GY, Yao CT, Wu CW, Yin SJ: Functional assessment of human alcohol dehydrogenase family in ethanol metabolism: significance of first-pass metabolism. Alcohol Clin Exp Res. 2006 Jul;30(7):1132-42. [16792560 ]
- General Function:
- Leukotriene-b4 20-monooxygenase activity
- Specific Function:
- Catalyzes the omega- and (omega-1)-hydroxylation of various fatty acids such as laurate, myristate and palmitate. Has little activity toward prostaglandins A1 and E1. Oxidizes arachidonic acid to 20-hydroxyeicosatetraenoic acid (20-HETE).
- Gene Name:
- CYP4A11
- Uniprot ID:
- Q02928
- Molecular Weight:
- 59347.31 Da
References
- Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. doi: 10.1093/nar/gkp970. Epub 2009 Nov 24. [19934256 ]
- General Function:
- Pdz domain binding
- Specific Function:
- Ionotropic glutamate receptor. L-glutamate acts as an excitatory neurotransmitter at many synapses in the central nervous system. Binding of the excitatory neurotransmitter L-glutamate induces a conformation change, leading to the opening of the cation channel, and thereby converts the chemical signal to an electrical impulse. The receptor then desensitizes rapidly and enters a transient inactive state, characterized by the presence of bound agonist. In the presence of CACNG4 or CACNG7 or CACNG8, shows resensitization which is characterized by a delayed accumulation of current flux upon continued application of glutamate.
- Gene Name:
- GRIA1
- Uniprot ID:
- P42261
- Molecular Weight:
- 101505.245 Da
References
- Dopico AM, Lovinger DM: Acute alcohol action and desensitization of ligand-gated ion channels. Pharmacol Rev. 2009 Mar;61(1):98-114. doi: 10.1124/pr.108.000430. Epub 2009 Mar 6. [19270242 ]
- General Function:
- Voltage-gated calcium channel activity
- Specific Function:
- Voltage-sensitive calcium channels (VSCC) mediate the entry of calcium ions into excitable cells and are also involved in a variety of calcium-dependent processes, including muscle contraction, hormone or neurotransmitter release, gene expression, cell motility, cell division and cell death. The isoform alpha-1C gives rise to L-type calcium currents. Long-lasting (L-type) calcium channels belong to the 'high-voltage activated' (HVA) group. They are blocked by dihydropyridines (DHP), phenylalkylamines, benzothiazepines, and by omega-agatoxin-IIIA (omega-Aga-IIIA). They are however insensitive to omega-conotoxin-GVIA (omega-CTx-GVIA) and omega-agatoxin-IVA (omega-Aga-IVA). Calcium channels containing the alpha-1C subunit play an important role in excitation-contraction coupling in the heart. The various isoforms display marked differences in the sensitivity to DHP compounds. Binding of calmodulin or CABP1 at the same regulatory sites results in an opposit effects on the channel function.
- Gene Name:
- CACNA1C
- Uniprot ID:
- Q13936
- Molecular Weight:
- 248974.1 Da
References
- Hendricson AW, Thomas MP, Lippmann MJ, Morrisett RA: Suppression of L-type voltage-gated calcium channel-dependent synaptic plasticity by ethanol: analysis of miniature synaptic currents and dendritic calcium transients. J Pharmacol Exp Ther. 2003 Nov;307(2):550-8. Epub 2003 Sep 11. [12970385 ]