Anisatin
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Basic Info
| Common Name | Anisatin(F04789) |
| 2D Structure | |
| Description | Anisatin is a plant toxin found in the Japanese star anise (Illicium anisatum). The Japanese star anise has been burned as incense in Japan, where it is known as shikimi, as well as used in topical folk remedies. (L1226) |
| FRCD ID | F04789 |
| CAS Number | 5230-87-5 |
| PubChem CID | 115121 |
| Formula | C15H20O8 |
| IUPAC Name | None |
| InChI Key | GEVWHIDSUOMVRI-QWNPAUMXSA-N |
| InChI | InChI=1S/C15H20O8/c1-6-3-7(16)15(21)13(6)4-8(23-10(18)9(13)17)12(2,20)14(15)5-22-11(14)19/h6-9,16-17,20-21H,3-5H2,1-2H3/t6-,7-,8-,9+,12+,13+,14+,15-/m1/s1 |
| Canonical SMILES | CC1CC(C2(C13CC(C(C24COC4=O)(C)O)OC(=O)C3O)O)O |
| Isomeric SMILES | C[C@@H]1C[C@H]([C@]2([C@@]13C[C@H]([C@]([C@@]24COC4=O)(C)O)OC(=O)[C@@H]3O)O)O |
| Wikipedia | Anisatin |
| Synonyms |
Spiro(6H-4,9a-methanocyclopent(d)oxocin-6,3'-oxetane)-2,2'(1H)-dione, 4a-beta,5,6a,7,8,9-hexahydro-5,9a-dimethyl-1-alpha,5-beta,6a-beta,7-beta-tetrahydroxy-
Anisatin
(-)-Anisatin
UNII-W9K8802FZL
W9K8802FZL
5230-87-5
Spiro(6H-4,9a-methanocyclopent(d)oxocin-6,3'-oxetane)-2,2'(1H)-dione, hexahydro-1,5,6a,7-tetrahydroxy-5,9-dimethyl-, (1R,3'S,4R,5R,6aR,7R,9R,9aS)-
Spiro(6H-4,9a-methanocyclopent(d)oxocin-6,3'-oxetane)-2,2'(1H)-dione, hexahydro-1,5,6a,7-tetrahydroxy-5,9-dimethyl-, (1R-(1alpha,4beta,5beta,6beta,6abeta,7beta,9alpha,9abeta))-
aniasatin
AC1L3GK8
|
| Classifies |
Plant Toxin
|
| Update Date | Nov 13, 2018 17:07 |
Chemical Taxonomy
| Kingdom | Organic compounds |
| Superclass | Lipids and lipid-like molecules |
| Class | Prenol lipids |
| Subclass | Terpene lactones |
| Intermediate Tree Nodes | Not available |
| Direct Parent | Terpene lactones |
| Alternative Parents | |
| Molecular Framework | Aliphatic heteropolycyclic compounds |
| Substituents | Terpene lactone - Sesquiterpenoid - Prezizaane sesquiterpenoid - Delta valerolactone - Delta_valerolactone - Dicarboxylic acid or derivatives - Oxane - Tertiary alcohol - Beta_propiolactone - Cyclic alcohol - Secondary alcohol - Carboxylic acid ester - Oxetane - Lactone - Oxacycle - Organoheterocyclic compound - Carboxylic acid derivative - Polyol - Carbonyl group - Hydrocarbon derivative - Organic oxygen compound - Alcohol - Organic oxide - Organooxygen compound - Aliphatic heteropolycyclic compound |
| Description | This compound belongs to the class of organic compounds known as terpene lactones. These are prenol lipids containing a lactone ring. |
Properties
| Property Name | Property Value |
|---|---|
| Molecular Weight | 328.317 |
| Hydrogen Bond Donor Count | 4 |
| Hydrogen Bond Acceptor Count | 8 |
| Rotatable Bond Count | 0 |
| Complexity | 621 |
| Monoisotopic Mass | 328.116 |
| Exact Mass | 328.116 |
| XLogP | -1.9 |
| Formal Charge | 0 |
| Heavy Atom Count | 23 |
| Defined Atom Stereocenter Count | 8 |
| 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- | 0.7212 |
| Human Intestinal Absorption | HIA+ | 0.8046 |
| Caco-2 Permeability | Caco2- | 0.7947 |
| P-glycoprotein Substrate | Substrate | 0.8132 |
| P-glycoprotein Inhibitor | Non-inhibitor | 0.8135 |
| Non-inhibitor | 0.9927 | |
| Renal Organic Cation Transporter | Non-inhibitor | 0.9040 |
| Distribution | ||
| Subcellular localization | Mitochondria | 0.6897 |
| Metabolism | ||
| CYP450 2C9 Substrate | Non-substrate | 0.8723 |
| CYP450 2D6 Substrate | Non-substrate | 0.8605 |
| CYP450 3A4 Substrate | Substrate | 0.5935 |
| CYP450 1A2 Inhibitor | Non-inhibitor | 0.8986 |
| CYP450 2C9 Inhibitor | Non-inhibitor | 0.9369 |
| CYP450 2D6 Inhibitor | Non-inhibitor | 0.9418 |
| CYP450 2C19 Inhibitor | Non-inhibitor | 0.9182 |
| CYP450 3A4 Inhibitor | Non-inhibitor | 0.8916 |
| CYP Inhibitory Promiscuity | Low CYP Inhibitory Promiscuity | 0.9932 |
| Excretion | ||
| Toxicity | ||
| Human Ether-a-go-go-Related Gene Inhibition | Weak inhibitor | 0.9962 |
| Non-inhibitor | 0.7800 | |
| AMES Toxicity | Non AMES toxic | 0.7506 |
| Carcinogens | Non-carcinogens | 0.9571 |
| Fish Toxicity | High FHMT | 0.9536 |
| Tetrahymena Pyriformis Toxicity | High TPT | 0.9910 |
| Honey Bee Toxicity | High HBT | 0.6854 |
| Biodegradation | Not ready biodegradable | 0.9594 |
| Acute Oral Toxicity | III | 0.4390 |
| Carcinogenicity (Three-class) | Non-required | 0.5972 |
| Model | Value | Unit |
|---|---|---|
| Absorption | ||
| Aqueous solubility | -3.0596 | LogS |
| Caco-2 Permeability | -0.1551 | LogPapp, cm/s |
| Distribution | ||
| Metabolism | ||
| Excretion | ||
| Toxicity | ||
| Rat Acute Toxicity | 2.7689 | LD50, mol/kg |
| Fish Toxicity | 1.6732 | pLC50, mg/L |
| Tetrahymena Pyriformis Toxicity | 0.5179 | pIGC50, ug/L |
References
| Title | Journal | Date | Pubmed ID |
|---|---|---|---|
| Rapid and simple neurotoxin-based distinction of Chinese and Japanese star anise by direct plant spray mass spectrometry. | J Chromatogr A | 2013 Nov 22 | 23932223 |
| Analysis of the neurotoxin anisatin in star anise by LC-MS/MS. | Food Addit Contam Part A Chem Anal Control Expo Risk Assess | 2013 | 23802692 |
| Rapid control of Chinese star anise fruits and teas for neurotoxic anisatin by Direct Analysis in Real Time high resolution mass spectrometry. | J Chromatogr A | 2012 Oct 12 | 22484123 |
| Combination of TLC and HPLC-MS/MS methods. Approach to a rational quality control of Chinese star anise. | J Agric Food Chem | 2006 Mar 22 | 16536563 |
| Molecular mechanisms of toxicity of important food-borne phytotoxins. | Mol Nutr Food Res | 2005 Feb | 15635687 |
| Synthetic studies toward anisatin: a formal synthesis of (+/-)-8-deoxyanisatin. | Org Lett | 2001 Jan 25 | 11430054 |
Targets
- 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
- Mechanism of Action:
- Anisatin acts as a GABA system antagonist. It binds non-competitively to the picrotoxinin site of the GABA receptor, prolonging the closed time of the receptor channel and reducing the probability of it opening.
References
- Ikeda T, Ozoe Y, Okuyama E, Nagata K, Honda H, Shono T, Narahashi T: Anisatin modulation of the gamma-aminobutyric acid receptor-channel in rat dorsal root ganglion neurons. Br J Pharmacol. 1999 Aug;127(7):1567-76. [10455311 ]
- 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
- Mechanism of Action:
- Anisatin acts as a GABA system antagonist. It binds non-competitively to the picrotoxinin site of the GABA receptor, prolonging the closed time of the receptor channel and reducing the probability of it opening.
References
- Ikeda T, Ozoe Y, Okuyama E, Nagata K, Honda H, Shono T, Narahashi T: Anisatin modulation of the gamma-aminobutyric acid receptor-channel in rat dorsal root ganglion neurons. Br J Pharmacol. 1999 Aug;127(7):1567-76. [10455311 ]
- 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
- Mechanism of Action:
- Anisatin acts as a GABA system antagonist. It binds non-competitively to the picrotoxinin site of the GABA receptor, prolonging the closed time of the receptor channel and reducing the probability of it opening.
References
- Ikeda T, Ozoe Y, Okuyama E, Nagata K, Honda H, Shono T, Narahashi T: Anisatin modulation of the gamma-aminobutyric acid receptor-channel in rat dorsal root ganglion neurons. Br J Pharmacol. 1999 Aug;127(7):1567-76. [10455311 ]
- 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
- Mechanism of Action:
- Anisatin acts as a GABA system antagonist. It binds non-competitively to the picrotoxinin site of the GABA receptor, prolonging the closed time of the receptor channel and reducing the probability of it opening.
References
- Ikeda T, Ozoe Y, Okuyama E, Nagata K, Honda H, Shono T, Narahashi T: Anisatin modulation of the gamma-aminobutyric acid receptor-channel in rat dorsal root ganglion neurons. Br J Pharmacol. 1999 Aug;127(7):1567-76. [10455311 ]
- 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
- Mechanism of Action:
- Anisatin acts as a GABA system antagonist. It binds non-competitively to the picrotoxinin site of the GABA receptor, prolonging the closed time of the receptor channel and reducing the probability of it opening.
References
- Ikeda T, Ozoe Y, Okuyama E, Nagata K, Honda H, Shono T, Narahashi T: Anisatin modulation of the gamma-aminobutyric acid receptor-channel in rat dorsal root ganglion neurons. Br J Pharmacol. 1999 Aug;127(7):1567-76. [10455311 ]
- 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
- Mechanism of Action:
- Anisatin acts as a GABA system antagonist. It binds non-competitively to the picrotoxinin site of the GABA receptor, prolonging the closed time of the receptor channel and reducing the probability of it opening.
References
- Ikeda T, Ozoe Y, Okuyama E, Nagata K, Honda H, Shono T, Narahashi T: Anisatin modulation of the gamma-aminobutyric acid receptor-channel in rat dorsal root ganglion neurons. Br J Pharmacol. 1999 Aug;127(7):1567-76. [10455311 ]
- 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
- Mechanism of Action:
- Anisatin acts as a GABA system antagonist. It binds non-competitively to the picrotoxinin site of the GABA receptor, prolonging the closed time of the receptor channel and reducing the probability of it opening.
References
- Ikeda T, Ozoe Y, Okuyama E, Nagata K, Honda H, Shono T, Narahashi T: Anisatin modulation of the gamma-aminobutyric acid receptor-channel in rat dorsal root ganglion neurons. Br J Pharmacol. 1999 Aug;127(7):1567-76. [10455311 ]
- 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
- Mechanism of Action:
- Anisatin acts as a GABA system antagonist. It binds non-competitively to the picrotoxinin site of the GABA receptor, prolonging the closed time of the receptor channel and reducing the probability of it opening.
References
- Ikeda T, Ozoe Y, Okuyama E, Nagata K, Honda H, Shono T, Narahashi T: Anisatin modulation of the gamma-aminobutyric acid receptor-channel in rat dorsal root ganglion neurons. Br J Pharmacol. 1999 Aug;127(7):1567-76. [10455311 ]
- 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:
- GABRG2
- Uniprot ID:
- P18507
- Molecular Weight:
- 54161.78 Da
- Mechanism of Action:
- Anisatin acts as a GABA system antagonist. It binds non-competitively to the picrotoxinin site of the GABA receptor, prolonging the closed time of the receptor channel and reducing the probability of it opening.
References
- Ikeda T, Ozoe Y, Okuyama E, Nagata K, Honda H, Shono T, Narahashi T: Anisatin modulation of the gamma-aminobutyric acid receptor-channel in rat dorsal root ganglion neurons. Br J Pharmacol. 1999 Aug;127(7):1567-76. [10455311 ]
- 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
- Mechanism of Action:
- Anisatin acts as a GABA system antagonist. It binds non-competitively to the picrotoxinin site of the GABA receptor, prolonging the closed time of the receptor channel and reducing the probability of it opening.
References
- Ikeda T, Ozoe Y, Okuyama E, Nagata K, Honda H, Shono T, Narahashi T: Anisatin modulation of the gamma-aminobutyric acid receptor-channel in rat dorsal root ganglion neurons. Br J Pharmacol. 1999 Aug;127(7):1567-76. [10455311 ]
- 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
- Mechanism of Action:
- Anisatin acts as a GABA system antagonist. It binds non-competitively to the picrotoxinin site of the GABA receptor, prolonging the closed time of the receptor channel and reducing the probability of it opening.
References
- Ikeda T, Ozoe Y, Okuyama E, Nagata K, Honda H, Shono T, Narahashi T: Anisatin modulation of the gamma-aminobutyric acid receptor-channel in rat dorsal root ganglion neurons. Br J Pharmacol. 1999 Aug;127(7):1567-76. [10455311 ]
- 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. Rho-1 GABA receptor could play a role in retinal neurotransmission.
- Gene Name:
- GABRR1
- Uniprot ID:
- P24046
- Molecular Weight:
- 55882.91 Da
- Mechanism of Action:
- Anisatin acts as a GABA system antagonist. It binds non-competitively to the picrotoxinin site of the GABA receptor, prolonging the closed time of the receptor channel and reducing the probability of it opening.
References
- Ikeda T, Ozoe Y, Okuyama E, Nagata K, Honda H, Shono T, Narahashi T: Anisatin modulation of the gamma-aminobutyric acid receptor-channel in rat dorsal root ganglion neurons. Br J Pharmacol. 1999 Aug;127(7):1567-76. [10455311 ]
- 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. Rho-2 GABA receptor could play a role in retinal neurotransmission.
- Gene Name:
- GABRR2
- Uniprot ID:
- P28476
- Molecular Weight:
- 54150.41 Da
- Mechanism of Action:
- Anisatin acts as a GABA system antagonist. It binds non-competitively to the picrotoxinin site of the GABA receptor, prolonging the closed time of the receptor channel and reducing the probability of it opening.
References
- Ikeda T, Ozoe Y, Okuyama E, Nagata K, Honda H, Shono T, Narahashi T: Anisatin modulation of the gamma-aminobutyric acid receptor-channel in rat dorsal root ganglion neurons. Br J Pharmacol. 1999 Aug;127(7):1567-76. [10455311 ]
- 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:
- GABRR3
- Uniprot ID:
- A8MPY1
- Molecular Weight:
- 54271.1 Da
- Mechanism of Action:
- Anisatin acts as a GABA system antagonist. It binds non-competitively to the picrotoxinin site of the GABA receptor, prolonging the closed time of the receptor channel and reducing the probability of it opening.
References
- Ikeda T, Ozoe Y, Okuyama E, Nagata K, Honda H, Shono T, Narahashi T: Anisatin modulation of the gamma-aminobutyric acid receptor-channel in rat dorsal root ganglion neurons. Br J Pharmacol. 1999 Aug;127(7):1567-76. [10455311 ]
- 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
- Mechanism of Action:
- Anisatin acts as a GABA system antagonist. It binds non-competitively to the picrotoxinin site of the GABA receptor, prolonging the closed time of the receptor channel and reducing the probability of it opening.
References
- Ikeda T, Ozoe Y, Okuyama E, Nagata K, Honda H, Shono T, Narahashi T: Anisatin modulation of the gamma-aminobutyric acid receptor-channel in rat dorsal root ganglion neurons. Br J Pharmacol. 1999 Aug;127(7):1567-76. [10455311 ]
- 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
- Mechanism of Action:
- Anisatin acts as a GABA system antagonist. It binds non-competitively to the picrotoxinin site of the GABA receptor, prolonging the closed time of the receptor channel and reducing the probability of it opening.
References
- Ikeda T, Ozoe Y, Okuyama E, Nagata K, Honda H, Shono T, Narahashi T: Anisatin modulation of the gamma-aminobutyric acid receptor-channel in rat dorsal root ganglion neurons. Br J Pharmacol. 1999 Aug;127(7):1567-76. [10455311 ]
- 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:
- Anisatin acts as a GABA system antagonist. It binds non-competitively to the picrotoxinin site of the GABA receptor, prolonging the closed time of the receptor channel and reducing the probability of it opening.
References
- Ikeda T, Ozoe Y, Okuyama E, Nagata K, Honda H, Shono T, Narahashi T: Anisatin modulation of the gamma-aminobutyric acid receptor-channel in rat dorsal root ganglion neurons. Br J Pharmacol. 1999 Aug;127(7):1567-76. [10455311 ]
- 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
- Mechanism of Action:
- Anisatin acts as a GABA system antagonist. It binds non-competitively to the picrotoxinin site of the GABA receptor, prolonging the closed time of the receptor channel and reducing the probability of it opening.
References
- Ikeda T, Ozoe Y, Okuyama E, Nagata K, Honda H, Shono T, Narahashi T: Anisatin modulation of the gamma-aminobutyric acid receptor-channel in rat dorsal root ganglion neurons. Br J Pharmacol. 1999 Aug;127(7):1567-76. [10455311 ]
- 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
- Mechanism of Action:
- Anisatin acts as a GABA system antagonist. It binds non-competitively to the picrotoxinin site of the GABA receptor, prolonging the closed time of the receptor channel and reducing the probability of it opening.
References
- Ikeda T, Ozoe Y, Okuyama E, Nagata K, Honda H, Shono T, Narahashi T: Anisatin modulation of the gamma-aminobutyric acid receptor-channel in rat dorsal root ganglion neurons. Br J Pharmacol. 1999 Aug;127(7):1567-76. [10455311 ]