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Picrotoxin

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Definition: A noncompetitive antagonist at GABA-A receptors and thus a convulsant. Picrotoxin blocks the GAMMA-AMINOBUTYRIC ACID-activated chloride ionophore. Although it is most often used as a research tool, it has been used as a CNS stimulant and an antidote in poisoning by CNS depressants, especially the barbiturates.     
Pharmacological Action Antidotes; Central Nervous System Stimulants; Convulsants; GABA Antagonists
 
SubstanceCAS Registry & nameCategoriesSourceDrugs*
hyenanchin  3484-46-6   Picrotoxin/*analogs & derivatives. Phytochem Anal 2001 Jan-Feb;12(1):69-72
picrotin  0   Picrotoxin/*analogs & derivatives. Mol Pharmacol 2000 Jul;58(1):11-7
Vertigoheel  0   *Minerals *Picrotoxin *Plant Extracts Drug Combinations. Arzneimittelforsch 1984;34(12):1791
picrotoxinin  17617-45-7 (1aR-(1a alpha,2a beta,3 beta,6 beta,6a beta,8aS*,8b beta,9R*))-hexahydro-2a-hydroxy-8b-methyl-9-(1-methylethenyl)-3,6-methano-8H-1,5,7-trioxa cyclopenta(ij)cycloprop(a)azulene-4,8(3H)-dione  Picrotoxin/*analogs & derivatives.
Pharma Action GABA-A Receptor Antagonists 		Nature 282(5744):298;1980
dihydropicrotoxinin  17617-46-8   Picrotoxin/*analogs & derivatives. Life Sci 22:1643;1978; Mol Pharmacol 14:381;1978
tutin  2571-22-4 (1aS-(1a alpha,1b beta,2 beta,5 beta,6 alpha,6a beta,7 beta,7a alpha,8S*))-hexahydro-1b,6-dihydroxy- 6a-methyl-8-(1-methylethenyl)spiro(2,5-methano-7H- oxireno(3,4)cyclopent(1,2-d)oxepin-7,2'-oxiran)- 3(2 alpha H)-one  *Sesquiterpenes Picrotoxin/*analogs & derivatives GABA Antagonists.
coriamyrtine  2571-86-0   *Picrotoxin. Europ. J. Toxicol. 3(1):191;1970

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Sources: NLM Medical Subject Headings, NIH UMLS, Drugs@FDA, FDA AERS original data copyright United States Government. No endorsement implied. Last modified 6/6/2012
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