picrotoxin Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
2162 124-87-8

Description:

MoleculeDescription

Synonyms:

  • picrotoxin
  • cocculin
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.
  • Molecular weight: 602.59
  • Formula: C30H34O13
  • CLOGP:
  • LIPINSKI: None
  • HAC: None
  • HDO: None
  • TPSA: 105.59
  • ALOGS:
  • ROTB: None

Drug dosage:

None

ADMET properties:

None

Approvals:

None

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

None

Pharmacologic Action:

SourceCodeDescription
CHEBI has role CHEBI:35337 central nervous system stimulant
CHEBI has role CHEBI:134173 antidote to barbiturate poisoning
CHEBI has role CHEBI:65259 GABA antagonist
MeSH PA D000931 Antidotes
MeSH PA D002491 Central Nervous System Agents
MeSH PA D000697 Central Nervous System Stimulants
MeSH PA D003292 Convulsants
MeSH PA D018682 GABA Agents
MeSH PA D018756 GABA Antagonists
MeSH PA D018377 Neurotransmitter Agents
MeSH PA D020011 Protective Agents

Drug Use (View source of the data)

None

Acid dissociation constants calculated using MoKa v3.0.0

None

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Glycine receptor subunit beta Ion channel BLOCKER IC50 4.50 IUPHAR
Glycine receptor subunit alpha-1 Ion channel BLOCKER IC50 5.20 IUPHAR
Glycine receptor subunit alpha-2 Ion channel BLOCKER IC50 5.60 IUPHAR
5-hydroxytryptamine receptor 3A Ion channel BLOCKER IC50 4.50 IUPHAR
GABA-A receptor; anion channel Ion channel IC50 5.88 CHEMBL

External reference:

IDSource
57979006 SNOMEDCT_US
001378 NDDF
CHEBI:134126 CHEBI
DB00466 DRUGBANK_ID
RI5 PDB_CHEM_ID
ZLT174DL7U UNII
31304 PUBCHEM_CID
D010852 MESH_DESCRIPTOR_UI
CHEMBL1908342 ChEMBL_ID
4051 IUPHAR_LIGAND_ID

Pharmaceutical products:

None