Robustoxin
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Basic Info
| Common Name | Robustoxin(F04704) |
| 2D Structure | |
| Description | Robustoxin is a peptide toxin produced by the Sydney funnel-web spider (Atrax robustus). It inhibits both insect and mammalian voltage-gated sodium channels. (T170) It is a low-molecular-weight neurotoxic polypeptide found in the venom of the Sydney funnel-web spider (Atrax robustus). |
| FRCD ID | F04704 |
| CAS Number | 91728-12-0 |
| PubChem CID | 56843298 |
| Formula | C206H313N59O59S9 |
| IUPAC Name | None |
| InChI Key | QFRVAFIKGDBGOZ-ZUSLOBLNSA-N |
| InChI | InChI=1S/C206H313N59O59S9/c1-13-101(5)162-200(318)252-133(78-109-50-54-113(270)55-51-109)183(301)229-104(8)168(286)244-136(80-111-86-223-118-40-20-18-38-115(111)118)187(305)246-135(79-110-52-56-114(271)57-53-110)186(304)250-139(83-155(218)276)190(308)240-128(59-63-152(215)273)179(297)239-127(58-62-151(214)272)170(288)225-89-159(280)232-142(91-266)193(311)256-144-95-329-330-96-145-195(313)257-146-94-327-326-92-117(213)169(287)228-103(7)167(285)233-121(43-23-29-68-208)173(291)234-122(44-24-30-69-209)174(292)237-126(48-34-73-222-206(220)221)176(294)249-140(84-156(219)277)191(309)247-137(81-112-87-224-119-41-21-19-39-116(112)119)188(306)253-143(171(289)226-88-157(278)230-120(42-22-28-67-207)172(290)248-138(82-154(217)275)189(307)241-130(61-65-160(281)282)180(298)251-141(85-161(283)284)192(310)255-145)93-328-331-97-147(197(315)260-162)254-177(295)124(46-26-32-71-211)236-181(299)131(66-75-325-12)243-198(316)150-49-35-74-265(150)204(322)148(258-196(146)314)98-332-333-99-149(205(323)324)259-178(296)125(47-27-33-72-212)235-175(293)123(45-25-31-70-210)238-185(303)134(77-108-36-16-15-17-37-108)245-184(302)132(76-100(3)4)231-158(279)90-227-199(317)164(105(9)267)263-201(319)163(102(6)14-2)261-202(320)166(107(11)269)264-203(321)165(106(10)268)262-182(300)129(242-194(144)312)60-64-153(216)274/h15-21,36-41,50-57,86-87,100-107,117,120-150,162-166,223-224,266-271H,13-14,22-35,42-49,58-85,88-99,207-213H2,1-12H3,(H2,214,272)(H2,215,273)(H2,216,274)(H2,217,275)(H2,218,276)(H2,219,277)(H,225,288)(H,226,289)(H,227,317)(H,228,287)(H,229,301)(H,230,278)(H,231,279)(H,232,280)(H,233,285)(H,234,291)(H,235,293)(H,236,299)(H,237,292)(H,238,303)(H,239,297)(H,240,308)(H,241,307)(H,242,312)(H,243,316)(H,244,286)(H,245,302)(H,246,305)(H,247,309)(H,248,290)(H,249,294)(H,250,304)(H,251,298)(H,252,318)(H,253,306)(H,254,295)(H,255,310)(H,256,311)(H,257,313)(H,258,314)(H,259,296)(H,260,315)(H,261,320)(H,262,300)(H,263,319)(H,264,321)(H,281,282)(H,283,284)(H,323,324)(H4,220,221,222)/t101-,102-,103-,104-,105+,106+,107+,117-,120-,121-,122-,123-,124-,125-,126-,127-,128-,129-,130-,131-,132-,133-,134-,135-,136-,137-,138-,139-,140-,141-,142-,143-,144-,145-,146-,147-,148-,149-,150-,162-,163-,164-,165-,166-/m0/s1 |
| Canonical SMILES | CCC(C)C1C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NCC(=O)NC(C(=O)NC2CSSCC3C(=O)NC4CSSCC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(CSSCC(C(=O)N1)NC(=O)C(NC(=O)C(NC(=O)C5CCCN5C(=O)C(CSSCC(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)CNC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC(=O)C(NC2=O)CCC(=O)N)C(C)O)C(C)O)C(C)CC)C(C)O)CC(C)C)CC6=CC=CC=C6)CCCCN)CCCCN)C(=O)O)NC4=O)CCSC)CCCCN)C(=O)NCC(=O)NC(C(=O)NC(C(=O)NC(C(=O)NC(C(=O)N3)CC(=O)O)CCC(=O)O)CC(=O)N)CCCCN)CC7=CNC8=CC=CC=C87)CC(=O)N)CCCNC(=N)N)CCCCN)CCCCN)C)N)CO)CCC(=O)N)CCC(=O)N)CC(=O)N)CC9=CC=C(C=C9)O)CC1=CNC2=CC=CC=C21)C)CC1=CC=C(C=C1)O |
| Isomeric SMILES | CC[C@H](C)[C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)NCC(=O)N[C@H](C(=O)N[C@H]2CSSC[C@H]3C(=O)N[C@H]4CSSC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CSSC[C@@H](C(=O)N1)NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H]5CCCN5C(=O)[C@H](CSSC[C@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)CNC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC(=O)[C@@H](NC2=O)CCC(=O)N)[C@@H](C)O)[C@@H](C)O)[C@@H](C)CC)[C@@H](C)O)CC(C)C)CC6=CC=CC=C6)CCCCN)CCCCN)C(=O)O)NC4=O)CCSC)CCCCN)C(=O)NCC(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N3)CC(=O)O)CCC(=O)O)CC(=O)N)CCCCN)CC7=CNC8=CC=CC=C87)CC(=O)N)CCCNC(=N)N)CCCCN)CCCCN)C)N)CO)CCC(=O)N)CCC(=O)N)CC(=O)N)CC9=CC=C(C=C9)O)CC1=CNC2=CC=CC=C21)C)CC1=CC=C(C=C1)O |
| Synonyms |
Robustoxin
91728-12-0
|
| Classifies |
Animal Toxin
|
| Update Date | Nov 13, 2018 17:07 |
Chemical Taxonomy
| Kingdom | Organic compounds |
| Superclass | Organic Polymers |
| Class | Polypeptides |
| Subclass | Not available |
| Intermediate Tree Nodes | Not available |
| Direct Parent | Polypeptides |
| Alternative Parents |
|
| Molecular Framework | Aromatic heteropolycyclic compounds |
| Substituents | Polypeptide - Cyclic alpha peptide - Alpha-amino acid amide - Alpha-amino acid or derivatives - 3-alkylindole - Indole - Indole or derivatives - Tricarboxylic acid or derivatives - 1-hydroxy-2-unsubstituted benzenoid - Phenol - Monocyclic benzene moiety - Fatty amide - Substituted pyrrole - Fatty acyl - Benzenoid - Tertiary carboxylic acid amide - Pyrrolidine - Pyrrole - Heteroaromatic compound - Amino acid or derivatives - Carboxamide group - Guanidine - Amino acid - Secondary carboxylic acid amide - Secondary alcohol - Primary carboxylic acid amide - Lactam - Organic disulfide - Dialkylthioether - Carboximidamide - Organoheterocyclic compound - Sulfenyl compound - Azacycle - Carboxylic acid derivative - Carboxylic acid - Thioether - Imine - Carbonyl group - Organic nitrogen compound - Organic oxide - Alcohol - Amine - Organic oxygen compound - Hydrocarbon derivative - Primary amine - Primary aliphatic amine - Primary alcohol - Organonitrogen compound - Organooxygen compound - Organosulfur compound - Aromatic heteropolycyclic compound |
| Description | This compound belongs to the class of organic compounds known as polypeptides. These are peptides containing ten or more amino acid residues. |
Properties
| Property Name | Property Value |
|---|---|
| Molecular Weight | 4848.664 |
| Hydrogen Bond Donor Count | 67 |
| Hydrogen Bond Acceptor Count | 76 |
| Rotatable Bond Count | 73 |
| Complexity | 11700 |
| Monoisotopic Mass | 4845.079 |
| Exact Mass | 4847.086 |
| XLogP | -20.2 |
| Formal Charge | 0 |
| Heavy Atom Count | 333 |
| Defined Atom Stereocenter Count | 44 |
| 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- | 0.9867 |
| Human Intestinal Absorption | HIA+ | 0.9028 |
| Caco-2 Permeability | Caco2- | 0.7476 |
| P-glycoprotein Substrate | Substrate | 0.9229 |
| P-glycoprotein Inhibitor | Non-inhibitor | 0.8103 |
| Non-inhibitor | 0.9824 | |
| Renal Organic Cation Transporter | Non-inhibitor | 0.8263 |
| Distribution | ||
| Subcellular localization | Mitochondria | 0.3802 |
| Metabolism | ||
| CYP450 2C9 Substrate | Non-substrate | 0.7479 |
| CYP450 2D6 Substrate | Non-substrate | 0.7925 |
| CYP450 3A4 Substrate | Substrate | 0.5769 |
| CYP450 1A2 Inhibitor | Non-inhibitor | 0.7917 |
| CYP450 2C9 Inhibitor | Non-inhibitor | 0.7549 |
| CYP450 2D6 Inhibitor | Non-inhibitor | 0.8652 |
| CYP450 2C19 Inhibitor | Non-inhibitor | 0.7545 |
| CYP450 3A4 Inhibitor | Non-inhibitor | 0.7882 |
| CYP Inhibitory Promiscuity | Low CYP Inhibitory Promiscuity | 0.9128 |
| Excretion | ||
| Toxicity | ||
| Human Ether-a-go-go-Related Gene Inhibition | Weak inhibitor | 0.9044 |
| Inhibitor | 0.5737 | |
| AMES Toxicity | Non AMES toxic | 0.7066 |
| Carcinogens | Non-carcinogens | 0.8015 |
| Fish Toxicity | High FHMT | 0.9960 |
| Tetrahymena Pyriformis Toxicity | High TPT | 0.9665 |
| Honey Bee Toxicity | Low HBT | 0.6458 |
| Biodegradation | Not ready biodegradable | 0.9929 |
| Acute Oral Toxicity | III | 0.5334 |
| Carcinogenicity (Three-class) | Non-required | 0.5731 |
| Model | Value | Unit |
|---|---|---|
| Absorption | ||
| Aqueous solubility | -3.4083 | LogS |
| Caco-2 Permeability | -0.2952 | LogPapp, cm/s |
| Distribution | ||
| Metabolism | ||
| Excretion | ||
| Toxicity | ||
| Rat Acute Toxicity | 2.9776 | LD50, mol/kg |
| Fish Toxicity | 1.3725 | pLC50, mg/L |
| Tetrahymena Pyriformis Toxicity | 0.5001 | pIGC50, ug/L |
Targets
- 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:
- Robustoxin inhibits both insect and mammalian voltage-gated sodium channels. It binds to site 3 in tetrodotoxin-sensitive sodium channels, which slows their inactivation and causes a prolongation of action potential duration resulting in repetitive firing in autonomic and motor nerve fibres.
References
- Armas LA, Hollis BW, Heaney RP: Vitamin D2 is much less effective than vitamin D3 in humans. J Clin Endocrinol Metab. 2004 Nov;89(11):5387-91. [15531486 ]
- 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:
- Robustoxin inhibits both insect and mammalian voltage-gated sodium channels. It binds to site 3 in tetrodotoxin-sensitive sodium channels, which slows their inactivation and causes a prolongation of action potential duration resulting in repetitive firing in autonomic and motor nerve fibres.
References
- Armas LA, Hollis BW, Heaney RP: Vitamin D2 is much less effective than vitamin D3 in humans. J Clin Endocrinol Metab. 2004 Nov;89(11):5387-91. [15531486 ]
- 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:
- Robustoxin inhibits both insect and mammalian voltage-gated sodium channels. It binds to site 3 in tetrodotoxin-sensitive sodium channels, which slows their inactivation and causes a prolongation of action potential duration resulting in repetitive firing in autonomic and motor nerve fibres.
References
- Armas LA, Hollis BW, Heaney RP: Vitamin D2 is much less effective than vitamin D3 in humans. J Clin Endocrinol Metab. 2004 Nov;89(11):5387-91. [15531486 ]
- 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:
- Robustoxin inhibits both insect and mammalian voltage-gated sodium channels. It binds to site 3 in tetrodotoxin-sensitive sodium channels, which slows their inactivation and causes a prolongation of action potential duration resulting in repetitive firing in autonomic and motor nerve fibres.
References
- Armas LA, Hollis BW, Heaney RP: Vitamin D2 is much less effective than vitamin D3 in humans. J Clin Endocrinol Metab. 2004 Nov;89(11):5387-91. [15531486 ]
- 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:
- Robustoxin inhibits both insect and mammalian voltage-gated sodium channels. It binds to site 3 in tetrodotoxin-sensitive sodium channels, which slows their inactivation and causes a prolongation of action potential duration resulting in repetitive firing in autonomic and motor nerve fibres.
References
- Armas LA, Hollis BW, Heaney RP: Vitamin D2 is much less effective than vitamin D3 in humans. J Clin Endocrinol Metab. 2004 Nov;89(11):5387-91. [15531486 ]
- 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:
- Robustoxin inhibits both insect and mammalian voltage-gated sodium channels. It binds to site 3 in tetrodotoxin-sensitive sodium channels, which slows their inactivation and causes a prolongation of action potential duration resulting in repetitive firing in autonomic and motor nerve fibres.
References
- Armas LA, Hollis BW, Heaney RP: Vitamin D2 is much less effective than vitamin D3 in humans. J Clin Endocrinol Metab. 2004 Nov;89(11):5387-91. [15531486 ]
- 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:
- Robustoxin inhibits both insect and mammalian voltage-gated sodium channels. It binds to site 3 in tetrodotoxin-sensitive sodium channels, which slows their inactivation and causes a prolongation of action potential duration resulting in repetitive firing in autonomic and motor nerve fibres.
References
- Armas LA, Hollis BW, Heaney RP: Vitamin D2 is much less effective than vitamin D3 in humans. J Clin Endocrinol Metab. 2004 Nov;89(11):5387-91. [15531486 ]
- 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:
- Robustoxin inhibits both insect and mammalian voltage-gated sodium channels. It binds to site 3 in tetrodotoxin-sensitive sodium channels, which slows their inactivation and causes a prolongation of action potential duration resulting in repetitive firing in autonomic and motor nerve fibres.
References
- Armas LA, Hollis BW, Heaney RP: Vitamin D2 is much less effective than vitamin D3 in humans. J Clin Endocrinol Metab. 2004 Nov;89(11):5387-91. [15531486 ]
- 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:
- Robustoxin inhibits both insect and mammalian voltage-gated sodium channels. It binds to site 3 in tetrodotoxin-sensitive sodium channels, which slows their inactivation and causes a prolongation of action potential duration resulting in repetitive firing in autonomic and motor nerve fibres.
References
- Armas LA, Hollis BW, Heaney RP: Vitamin D2 is much less effective than vitamin D3 in humans. J Clin Endocrinol Metab. 2004 Nov;89(11):5387-91. [15531486 ]
- 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:
- Robustoxin inhibits both insect and mammalian voltage-gated sodium channels. It binds to site 3 in tetrodotoxin-sensitive sodium channels, which slows their inactivation and causes a prolongation of action potential duration resulting in repetitive firing in autonomic and motor nerve fibres.
References
- Armas LA, Hollis BW, Heaney RP: Vitamin D2 is much less effective than vitamin D3 in humans. J Clin Endocrinol Metab. 2004 Nov;89(11):5387-91. [15531486 ]
- 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:
- Robustoxin inhibits both insect and mammalian voltage-gated sodium channels. It binds to site 3 in tetrodotoxin-sensitive sodium channels, which slows their inactivation and causes a prolongation of action potential duration resulting in repetitive firing in autonomic and motor nerve fibres.
References
- Armas LA, Hollis BW, Heaney RP: Vitamin D2 is much less effective than vitamin D3 in humans. J Clin Endocrinol Metab. 2004 Nov;89(11):5387-91. [15531486 ]
- 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:
- Robustoxin inhibits both insect and mammalian voltage-gated sodium channels. It binds to site 3 in tetrodotoxin-sensitive sodium channels, which slows their inactivation and causes a prolongation of action potential duration resulting in repetitive firing in autonomic and motor nerve fibres.
References
- Armas LA, Hollis BW, Heaney RP: Vitamin D2 is much less effective than vitamin D3 in humans. J Clin Endocrinol Metab. 2004 Nov;89(11):5387-91. [15531486 ]
- 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:
- Robustoxin inhibits both insect and mammalian voltage-gated sodium channels. It binds to site 3 in tetrodotoxin-sensitive sodium channels, which slows their inactivation and causes a prolongation of action potential duration resulting in repetitive firing in autonomic and motor nerve fibres.
References
- Armas LA, Hollis BW, Heaney RP: Vitamin D2 is much less effective than vitamin D3 in humans. J Clin Endocrinol Metab. 2004 Nov;89(11):5387-91. [15531486 ]
- 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:
- Robustoxin inhibits both insect and mammalian voltage-gated sodium channels. It binds to site 3 in tetrodotoxin-sensitive sodium channels, which slows their inactivation and causes a prolongation of action potential duration resulting in repetitive firing in autonomic and motor nerve fibres.
References
- Armas LA, Hollis BW, Heaney RP: Vitamin D2 is much less effective than vitamin D3 in humans. J Clin Endocrinol Metab. 2004 Nov;89(11):5387-91. [15531486 ]