Ciguatoxin 1
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Basic Info
| Common Name | Ciguatoxin 1(F04691) |
| 2D Structure | |
| Description | Ciguatoxin is a fish toxin consisting of apolycyclic ethers produced by Gambierdiscus (dinoflagellates) from gambiertoxins. It is ingested by fish and in turn may be ingested by humans, causing ciguatera poisoning. (L994, L997) |
| FRCD ID | F04691 |
| CAS Number | 11050-21-8 |
| PubChem CID | 5311333 |
| Formula | C60H86O19 |
| IUPAC Name | None |
| InChI Key | VYVRIXWNTVOIRD-LRHBOZQDSA-N |
| InChI | InChI=1S/C60H86O19/c1-28-19-42-44(22-48-54(76-42)30(3)52(65)58-55(77-48)29(2)31(4)60(79-58)25-33(63)27-67-60)73-46-24-51-59(5,78-47(46)20-28)50(64)23-45-36(74-51)11-7-6-10-35-37(71-45)15-16-39-38(69-35)17-18-40-43(70-39)21-49-57(75-40)53(66)56-41(72-49)12-8-9-34(68-56)14-13-32(62)26-61/h6-9,13-18,28-58,61-66H,10-12,19-27H2,1-5H3/b7-6-,14-13+/t28-,29+,30+,31+,32+,33+,34-,35-,36+,37+,38+,39-,40-,41+,42+,43+,44-,45-,46+,47-,48+,49-,50-,51-,52+,53-,54-,55-,56+,57-,58+,59+,60-/m1/s1 |
| Canonical SMILES | CC1CC2C(CC3C(O2)C(C(C4C(O3)C(C(C5(O4)CC(CO5)O)C)C)O)C)OC6CC7C(C(CC8C(O7)CC=CCC9C(O8)C=CC2C(O9)C=CC3C(O2)CC2C(O3)C(C3C(O2)CC=CC(O3)C=CC(CO)O)O)O)(OC6C1)C |
| Isomeric SMILES | C[C@@H]1C[C@H]2[C@@H](C[C@H]3[C@H](O2)[C@H]([C@@H]([C@H]4[C@H](O3)[C@H]([C@@H]([C@]5(O4)C[C@@H](CO5)O)C)C)O)C)O[C@H]6C[C@@H]7[C@]([C@@H](C[C@@H]8[C@@H](O7)C/C=C\C[C@@H]9[C@@H](O8)C=C[C@@H]2[C@@H](O9)C=C[C@@H]3[C@@H](O2)C[C@@H]2[C@@H](O3)[C@@H]([C@@H]3[C@@H](O2)CC=C[C@@H](O3)/C=C/[C@@H](CO)O)O)O)(O[C@@H]6C1)C |
| Synonyms |
Ciguatoxin CTX 1
Pacific ciguatoxin 1
CIGUATOXIN
Ciguatoxin 1
CTX 1
P-CTX 1
UNII-2UKQ3B7696
HSDB 7241
11050-21-8
2UKQ3B7696
|
| Classifies |
Animal Toxin
|
| Update Date | Nov 13, 2018 17:07 |
Chemical Taxonomy
| Kingdom | Organic compounds |
| Superclass | Phenylpropanoids and polyketides |
| Class | Ciguatera toxins |
| Subclass | Not available |
| Intermediate Tree Nodes | Not available |
| Direct Parent | Ciguatera toxins |
| Alternative Parents | |
| Molecular Framework | Aliphatic heteropolycyclic compounds |
| Substituents | Ciguatera toxin fragment - Ketal - Oxepane - Monosaccharide - Oxane - Tetrahydrofuran - Secondary alcohol - Polyol - Organoheterocyclic compound - Oxacycle - Ether - Dialkyl ether - Acetal - Primary alcohol - Organooxygen compound - Hydrocarbon derivative - Organic oxygen compound - Alcohol - Aliphatic heteropolycyclic compound |
| Description | This compound belongs to the class of organic compounds known as ciguatera toxins. These are lipid-soluble polyether compounds consisting of 13 to 14 rings fused by ether linkages into a most rigid ladder-like structure. |
Properties
| Property Name | Property Value |
|---|---|
| Molecular Weight | 1111.329 |
| Hydrogen Bond Donor Count | 6 |
| Hydrogen Bond Acceptor Count | 19 |
| Rotatable Bond Count | 3 |
| Complexity | 2300 |
| Monoisotopic Mass | 1110.576 |
| Exact Mass | 1110.576 |
| XLogP | 2.5 |
| Formal Charge | 0 |
| Heavy Atom Count | 79 |
| Defined Atom Stereocenter Count | 33 |
| Undefined Atom Stereocenter Count | 0 |
| Defined Bond Stereocenter Count | 2 |
| Undefined Bond Stereocenter Count | 0 |
| Isotope Atom Count | 0 |
| Covalently-Bonded Unit Count | 1 |
ADMET
| Model | Result | Probability |
|---|---|---|
| Absorption | ||
| Blood-Brain Barrier | BBB+ | 0.7982 |
| Human Intestinal Absorption | HIA+ | 0.8191 |
| Caco-2 Permeability | Caco2- | 0.7279 |
| P-glycoprotein Substrate | Substrate | 0.7939 |
| P-glycoprotein Inhibitor | Non-inhibitor | 0.5702 |
| Non-inhibitor | 0.9196 | |
| Renal Organic Cation Transporter | Non-inhibitor | 0.8368 |
| Distribution | ||
| Subcellular localization | Mitochondria | 0.5035 |
| Metabolism | ||
| CYP450 2C9 Substrate | Non-substrate | 0.7942 |
| CYP450 2D6 Substrate | Non-substrate | 0.8227 |
| CYP450 3A4 Substrate | Substrate | 0.6472 |
| CYP450 1A2 Inhibitor | Non-inhibitor | 0.8818 |
| CYP450 2C9 Inhibitor | Non-inhibitor | 0.9360 |
| CYP450 2D6 Inhibitor | Non-inhibitor | 0.9504 |
| CYP450 2C19 Inhibitor | Non-inhibitor | 0.8818 |
| CYP450 3A4 Inhibitor | Non-inhibitor | 0.9267 |
| CYP Inhibitory Promiscuity | Low CYP Inhibitory Promiscuity | 0.9566 |
| Excretion | ||
| Toxicity | ||
| Human Ether-a-go-go-Related Gene Inhibition | Weak inhibitor | 0.9687 |
| Non-inhibitor | 0.6158 | |
| AMES Toxicity | Non AMES toxic | 0.8910 |
| Carcinogens | Non-carcinogens | 0.9362 |
| Fish Toxicity | High FHMT | 0.9879 |
| Tetrahymena Pyriformis Toxicity | High TPT | 0.9931 |
| Honey Bee Toxicity | High HBT | 0.7775 |
| Biodegradation | Not ready biodegradable | 1.0000 |
| Acute Oral Toxicity | I | 0.6187 |
| Carcinogenicity (Three-class) | Non-required | 0.5161 |
| Model | Value | Unit |
|---|---|---|
| Absorption | ||
| Aqueous solubility | -3.8763 | LogS |
| Caco-2 Permeability | -0.0915 | LogPapp, cm/s |
| Distribution | ||
| Metabolism | ||
| Excretion | ||
| Toxicity | ||
| Rat Acute Toxicity | 3.5611 | LD50, mol/kg |
| Fish Toxicity | 1.3572 | pLC50, mg/L |
| Tetrahymena Pyriformis Toxicity | 0.8336 | pIGC50, ug/L |
References
| Title | Journal | Date | Pubmed ID |
|---|---|---|---|
| Transcriptomic Analysis of Ciguatoxin-Induced Changes in Gene Expression in Primary Cultures of Mice Cortical Neurons. | Toxins (Basel) | 2018 May 10 | 29748486 |
| Selective Extraction and Purification of Azaspiracids from Blue Mussels ( Mytilus edulis) Using Boric Acid Gel. | J Agric Food Chem | 2018 Mar 21 | 29502403 |
| Ciguatoxin prevalence in 4 commercial fish species along an oceanic exposure gradient in the US Virgin Islands. | Environ Toxicol Chem | 2018 Jul | 29710376 |
| Tectus niloticus (Tegulidae, Gastropod) as a Novel Vector of Ciguatera Poisoning:Clinical Characterization and Follow-Up of a Mass Poisoning Event in Nuku HivaIsland (French Polynesia). | Toxins (Basel) | 2018 Feb 28 | 29495579 |
| Differential toxin profiles of ciguatoxins in marine organisms: Chemistry, fate and global distribution. | Toxicon | 2018 Aug | 29778594 |
| Investigation of ciguatoxins in invasive lionfish from the greater caribbean region: Implications for fishery development. | PLoS One | 2018 | 29924826 |
| Fish-Associated Foodborne Disease Outbreaks: United States, 1998-2015. | Foodborne Pathog Dis | 2017 Sep | 28682115 |
| Acute Exposure to Pacific Ciguatoxin Reduces Electroencephalogram Activity and Disrupts Neurotransmitter Metabolic Pathways in Motor Cortex. | Mol Neurobiol | 2017 Sep | 27613284 |
| Role of Modular Polyketide Synthases in the Production of Polyether Ladder Compounds in Ciguatoxin-Producing Gambierdiscus polynesiensis and G. excentricus (Dinophyceae). | J Eukaryot Microbiol | 2017 Sep | 28211202 |
| The prevalence of benthic dinoflagellates associated with ciguatera fishpoisoning in the central Red Sea. | Harmful Algae | 2017 Sep | 28962981 |
| Quantification of Representative Ciguatoxins in the Pacific Using Quantitative Nuclear Magnetic Resonance Spectroscopy. | Mar Drugs | 2017 Oct 12 | 29023382 |
| Is mannitol the treatment of choice for patients with ciguatera fish poisoning? | Clin Toxicol (Phila) | 2017 Nov | 28535116 |
| An Updated Review of Ciguatera Fish Poisoning: Clinical, Epidemiological, Environmental, and Public Health Management. | Mar Drugs | 2017 Mar 14 | 28335428 |
| Regional Variations in the Risk and Severity of Ciguatera Caused by Eating Moray Eels. | Toxins (Basel) | 2017 Jun 26 | 28672845 |
| Human neuronal cell based assay: A new in vitro model for toxicity evaluation of ciguatoxin. | Environ Toxicol Pharmacol | 2017 Jun | 28437641 |
| [Poisoning caused by marine biotoxins]. | Bundesgesundheitsblatt Gesundheitsforschung Gesundheitsschutz | 2017 Jul | 28516259 |
| Physiological and behavioural impacts of Pacific ciguatoxin-1 (P-CTX-1) on marine medaka (Oryzias melastigma). | J Hazard Mater | 2017 Jan 5 | 27720471 |
| Recent Trends in Marine Phycotoxins from Australian Coastal Waters. | Mar Drugs | 2017 Feb 9 | 28208796 |
| Characterization of Gambierdiscus lapillus sp. nov. (Gonyaulacales, Dinophyceae): a new toxic dinoflagellate from the Great Barrier Reef (Australia). | J Phycol | 2017 Apr | 27885668 |
| Qualitative and quantitative assessment of the presence of ciguatoxin, P-CTX-1B, in Spanish Mackerel (<i>Scomberomorus commerson</i>) from waters in New South Wales (Australia). | Toxicol Rep | 2017 | 28959656 |
Targets
- General Function:
- Voltage-gated sodium channel activity
- Specific Function:
- This protein mediates the voltage-dependent sodium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference across the membrane, the protein forms a sodium-selective channel through which sodium ions may pass in accordance with their electrochemical gradient. It is a tetrodotoxin-resistant sodium channel isoform. Also involved, with the contribution of the receptor tyrosine kinase NTRK2, in rapid BDNF-evoked neuronal depolarization.
- Gene Name:
- SCN11A
- Uniprot ID:
- Q9UI33
- Molecular Weight:
- 204919.66 Da
- Mechanism of Action:
- Ciguatoxin lowers the threshold for opening voltage-gated sodium channels in synapses of the nervous system. The effect of opening a sodium channel will cause depolarization, which could sequentially cause paralysis, heart contraction, and changing the senses of hearing and cold. Because it does not cross the blood brain barrier (BBB), ciguatoxins solely affect the peripheral nervous system (PNS).
References
- Lombet A, Bidard JN, Lazdunski M: Ciguatoxin and brevetoxins share a common receptor site on the neuronal voltage-dependent Na+ channel. FEBS Lett. 1987 Jul 27;219(2):355-9. [2440718 ]
- General Function:
- Voltage-gated sodium channel activity
- Specific Function:
- Mediates the voltage-dependent sodium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference across the membrane, the protein forms a sodium-selective channel through which Na(+) ions may pass in accordance with their electrochemical gradient.
- Gene Name:
- SCN2A
- Uniprot ID:
- Q99250
- Molecular Weight:
- 227972.64 Da
- Mechanism of Action:
- Ciguatoxin lowers the threshold for opening voltage-gated sodium channels in synapses of the nervous system. The effect of opening a sodium channel will cause depolarization, which could sequentially cause paralysis, heart contraction, and changing the senses of hearing and cold. Because it does not cross the blood brain barrier (BBB), ciguatoxins solely affect the peripheral nervous system (PNS).
References
- Lombet A, Bidard JN, Lazdunski M: Ciguatoxin and brevetoxins share a common receptor site on the neuronal voltage-dependent Na+ channel. FEBS Lett. 1987 Jul 27;219(2):355-9. [2440718 ]
- General Function:
- Voltage-gated sodium channel activity
- Specific Function:
- Mediates the voltage-dependent sodium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference across the membrane, the protein forms a sodium-selective channel through which Na(+) ions may pass in accordance with their electrochemical gradient.
- Gene Name:
- SCN3A
- Uniprot ID:
- Q9NY46
- Molecular Weight:
- 226291.905 Da
- Mechanism of Action:
- Ciguatoxin lowers the threshold for opening voltage-gated sodium channels in synapses of the nervous system. The effect of opening a sodium channel will cause depolarization, which could sequentially cause paralysis, heart contraction, and changing the senses of hearing and cold. Because it does not cross the blood brain barrier (BBB), ciguatoxins solely affect the peripheral nervous system (PNS).
References
- Lombet A, Bidard JN, Lazdunski M: Ciguatoxin and brevetoxins share a common receptor site on the neuronal voltage-dependent Na+ channel. FEBS Lett. 1987 Jul 27;219(2):355-9. [2440718 ]
- General Function:
- Voltage-gated sodium channel activity
- Specific Function:
- This protein mediates the voltage-dependent sodium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference across the membrane, the protein forms a sodium-selective channel through which Na(+) ions may pass in accordance with their electrochemical gradient. This sodium channel may be present in both denervated and innervated skeletal muscle.
- Gene Name:
- SCN4A
- Uniprot ID:
- P35499
- Molecular Weight:
- 208059.175 Da
- Mechanism of Action:
- Ciguatoxin lowers the threshold for opening voltage-gated sodium channels in synapses of the nervous system. The effect of opening a sodium channel will cause depolarization, which could sequentially cause paralysis, heart contraction, and changing the senses of hearing and cold. Because it does not cross the blood brain barrier (BBB), ciguatoxins solely affect the peripheral nervous system (PNS).
References
- Lombet A, Bidard JN, Lazdunski M: Ciguatoxin and brevetoxins share a common receptor site on the neuronal voltage-dependent Na+ channel. FEBS Lett. 1987 Jul 27;219(2):355-9. [2440718 ]
- General Function:
- Voltage-gated sodium channel activity
- Specific Function:
- Mediates the voltage-dependent sodium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference across the membrane, the protein forms a sodium-selective channel through which Na(+) ions may pass in accordance with their electrochemical gradient.
- Gene Name:
- SCN7A
- Uniprot ID:
- Q01118
- Molecular Weight:
- 193491.605 Da
- Mechanism of Action:
- Ciguatoxin lowers the threshold for opening voltage-gated sodium channels in synapses of the nervous system. The effect of opening a sodium channel will cause depolarization, which could sequentially cause paralysis, heart contraction, and changing the senses of hearing and cold. Because it does not cross the blood brain barrier (BBB), ciguatoxins solely affect the peripheral nervous system (PNS).
References
- Lombet A, Bidard JN, Lazdunski M: Ciguatoxin and brevetoxins share a common receptor site on the neuronal voltage-dependent Na+ channel. FEBS Lett. 1987 Jul 27;219(2):355-9. [2440718 ]
- General Function:
- Voltage-gated sodium channel activity involved in purkinje myocyte action potential
- Specific Function:
- Crucial in the assembly, expression, and functional modulation of the heterotrimeric complex of the sodium channel. The subunit beta-1 can modulate multiple alpha subunit isoforms from brain, skeletal muscle, and heart. Its association with neurofascin may target the sodium channels to the nodes of Ranvier of developing axons and retain these channels at the nodes in mature myelinated axons.Isoform 2: Cell adhesion molecule that plays a critical role in neuronal migration and pathfinding during brain development. Stimulates neurite outgrowth.
- Gene Name:
- SCN1B
- Uniprot ID:
- Q07699
- Molecular Weight:
- 24706.955 Da
- Mechanism of Action:
- Ciguatoxin lowers the threshold for opening voltage-gated sodium channels in synapses of the nervous system. The effect of opening a sodium channel will cause depolarization, which could sequentially cause paralysis, heart contraction, and changing the senses of hearing and cold. Because it does not cross the blood brain barrier (BBB), ciguatoxins solely affect the peripheral nervous system (PNS).
References
- Lombet A, Bidard JN, Lazdunski M: Ciguatoxin and brevetoxins share a common receptor site on the neuronal voltage-dependent Na+ channel. FEBS Lett. 1987 Jul 27;219(2):355-9. [2440718 ]
- General Function:
- Voltage-gated sodium channel activity involved in cardiac muscle cell action potential
- Specific Function:
- Modulates channel gating kinetics. Causes unique persistent sodium currents. Inactivates the sodium channel opening more slowly than the subunit beta-1. Its association with neurofascin may target the sodium channels to the nodes of Ranvier of developing axons and retain these channels at the nodes in mature myelinated axons (By similarity).
- Gene Name:
- SCN3B
- Uniprot ID:
- Q9NY72
- Molecular Weight:
- 24702.08 Da
- Mechanism of Action:
- Ciguatoxin lowers the threshold for opening voltage-gated sodium channels in synapses of the nervous system. The effect of opening a sodium channel will cause depolarization, which could sequentially cause paralysis, heart contraction, and changing the senses of hearing and cold. Because it does not cross the blood brain barrier (BBB), ciguatoxins solely affect the peripheral nervous system (PNS).
References
- Lombet A, Bidard JN, Lazdunski M: Ciguatoxin and brevetoxins share a common receptor site on the neuronal voltage-dependent Na+ channel. FEBS Lett. 1987 Jul 27;219(2):355-9. [2440718 ]
- General Function:
- Voltage-gated sodium channel activity involved in cardiac muscle cell action potential
- Specific Function:
- Modulates channel gating kinetics. Causes negative shifts in the voltage dependence of activation of certain alpha sodium channels, but does not affect the voltage dependence of inactivation. Modulates the suceptibility of the sodium channel to inhibition by toxic peptides from spider, scorpion, wasp and sea anemone venom.
- Gene Name:
- SCN4B
- Uniprot ID:
- Q8IWT1
- Molecular Weight:
- 24968.755 Da
- Mechanism of Action:
- Ciguatoxin lowers the threshold for opening voltage-gated sodium channels in synapses of the nervous system. The effect of opening a sodium channel will cause depolarization, which could sequentially cause paralysis, heart contraction, and changing the senses of hearing and cold. Because it does not cross the blood brain barrier (BBB), ciguatoxins solely affect the peripheral nervous system (PNS).
References
- Lombet A, Bidard JN, Lazdunski M: Ciguatoxin and brevetoxins share a common receptor site on the neuronal voltage-dependent Na+ channel. FEBS Lett. 1987 Jul 27;219(2):355-9. [2440718 ]
- General Function:
- Voltage-gated sodium channel activity
- Specific Function:
- Mediates the voltage-dependent sodium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference across the membrane, the protein forms a sodium-selective channel through which Na(+) ions may pass in accordance with their electrochemical gradient.
- Gene Name:
- SCN1A
- Uniprot ID:
- P35498
- Molecular Weight:
- 228969.49 Da
- Mechanism of Action:
- Ciguatoxin lowers the threshold for opening voltage-gated sodium channels in synapses of the nervous system. The effect of opening a sodium channel will cause depolarization, which could sequentially cause paralysis, heart contraction, and changing the senses of hearing and cold. Because it does not cross the blood brain barrier (BBB), ciguatoxins solely affect the peripheral nervous system (PNS).
References
- Lombet A, Bidard JN, Lazdunski M: Ciguatoxin and brevetoxins share a common receptor site on the neuronal voltage-dependent Na+ channel. FEBS Lett. 1987 Jul 27;219(2):355-9. [2440718 ]
- General Function:
- Voltage-gated sodium channel activity
- Specific Function:
- Tetrodotoxin-resistant channel that mediates the voltage-dependent sodium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference across the membrane, the protein forms a sodium-selective channel through which sodium ions may pass in accordance with their electrochemical gradient. Plays a role in neuropathic pain mechanisms.
- Gene Name:
- SCN10A
- Uniprot ID:
- Q9Y5Y9
- Molecular Weight:
- 220623.605 Da
- Mechanism of Action:
- Ciguatoxin lowers the threshold for opening voltage-gated sodium channels in synapses of the nervous system. The effect of opening a sodium channel will cause depolarization, which could sequentially cause paralysis, heart contraction, and changing the senses of hearing and cold. Because it does not cross the blood brain barrier (BBB), ciguatoxins solely affect the peripheral nervous system (PNS).
References
- Lombet A, Bidard JN, Lazdunski M: Ciguatoxin and brevetoxins share a common receptor site on the neuronal voltage-dependent Na+ channel. FEBS Lett. 1987 Jul 27;219(2):355-9. [2440718 ]
- General Function:
- Voltage-gated sodium channel activity involved in sa node cell action potential
- Specific Function:
- This protein mediates the voltage-dependent sodium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference across the membrane, the protein forms a sodium-selective channel through which Na(+) ions may pass in accordance with their electrochemical gradient. It is a tetrodotoxin-resistant Na(+) channel isoform. This channel is responsible for the initial upstroke of the action potential. Channel inactivation is regulated by intracellular calcium levels.
- Gene Name:
- SCN5A
- Uniprot ID:
- Q14524
- Molecular Weight:
- 226937.475 Da
- Mechanism of Action:
- Ciguatoxin lowers the threshold for opening voltage-gated sodium channels in synapses of the nervous system. The effect of opening a sodium channel will cause depolarization, which could sequentially cause paralysis, heart contraction, and changing the senses of hearing and cold. Because it does not cross the blood brain barrier (BBB), ciguatoxins solely affect the peripheral nervous system (PNS).
References
- Lombet A, Bidard JN, Lazdunski M: Ciguatoxin and brevetoxins share a common receptor site on the neuronal voltage-dependent Na+ channel. FEBS Lett. 1987 Jul 27;219(2):355-9. [2440718 ]
- General Function:
- Voltage-gated sodium channel activity
- Specific Function:
- Mediates the voltage-dependent sodium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference across the membrane, the protein forms a sodium-selective channel through which Na(+) ions may pass in accordance with their electrochemical gradient. In macrophages and melanoma cells, isoform 5 may participate in the control of podosome and invadopodia formation.
- Gene Name:
- SCN8A
- Uniprot ID:
- Q9UQD0
- Molecular Weight:
- 225278.005 Da
- Mechanism of Action:
- Ciguatoxin lowers the threshold for opening voltage-gated sodium channels in synapses of the nervous system. The effect of opening a sodium channel will cause depolarization, which could sequentially cause paralysis, heart contraction, and changing the senses of hearing and cold. Because it does not cross the blood brain barrier (BBB), ciguatoxins solely affect the peripheral nervous system (PNS).
References
- Lombet A, Bidard JN, Lazdunski M: Ciguatoxin and brevetoxins share a common receptor site on the neuronal voltage-dependent Na+ channel. FEBS Lett. 1987 Jul 27;219(2):355-9. [2440718 ]
- General Function:
- Voltage-gated sodium channel activity
- Specific Function:
- Mediates the voltage-dependent sodium ion permeability of excitable membranes. Assuming opened or closed conformations in response to the voltage difference across the membrane, the protein forms a sodium-selective channel through which Na(+) ions may pass in accordance with their electrochemical gradient. It is a tetrodotoxin-sensitive Na(+) channel isoform. Plays a role in pain mechanisms, especially in the development of inflammatory pain (By similarity).
- Gene Name:
- SCN9A
- Uniprot ID:
- Q15858
- Molecular Weight:
- 226370.175 Da
- Mechanism of Action:
- Ciguatoxin lowers the threshold for opening voltage-gated sodium channels in synapses of the nervous system. The effect of opening a sodium channel will cause depolarization, which could sequentially cause paralysis, heart contraction, and changing the senses of hearing and cold. Because it does not cross the blood brain barrier (BBB), ciguatoxins solely affect the peripheral nervous system (PNS).
References
- Lombet A, Bidard JN, Lazdunski M: Ciguatoxin and brevetoxins share a common receptor site on the neuronal voltage-dependent Na+ channel. FEBS Lett. 1987 Jul 27;219(2):355-9. [2440718 ]
- General Function:
- Voltage-gated sodium channel activity involved in cardiac muscle cell action potential
- Specific Function:
- Crucial in the assembly, expression, and functional modulation of the heterotrimeric complex of the sodium channel. The subunit beta-2 causes an increase in the plasma membrane surface area and in its folding into microvilli. Interacts with TNR may play a crucial role in clustering and regulation of activity of sodium channels at nodes of Ranvier (By similarity).
- Gene Name:
- SCN2B
- Uniprot ID:
- O60939
- Molecular Weight:
- 24325.69 Da
- Mechanism of Action:
- Ciguatoxin lowers the threshold for opening voltage-gated sodium channels in synapses of the nervous system. The effect of opening a sodium channel will cause depolarization, which could sequentially cause paralysis, heart contraction, and changing the senses of hearing and cold. Because it does not cross the blood brain barrier (BBB), ciguatoxins solely affect the peripheral nervous system (PNS).
References
- Lombet A, Bidard JN, Lazdunski M: Ciguatoxin and brevetoxins share a common receptor site on the neuronal voltage-dependent Na+ channel. FEBS Lett. 1987 Jul 27;219(2):355-9. [2440718 ]