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

Stem definition	Drug id	CAS RN
	2162	124-87-8

Description:

Molecule	Description
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

Molecule

Description

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

FDA Adverse Event Reporting System (Geriatric)

None

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
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	D058787	GABA-A Receptor Antagonists
MeSH PA	D018377	Neurotransmitter Agents
MeSH PA	D020011	Protective Agents
CHEBI has role	CHEBI:35337	analeptic
CHEBI has role	CHEBI:65259	GABA antagonists
CHEBI has role	CHEBI:76924	plant metabolites
CHEBI has role	CHEBI:134173	antidote to barbiturate overdose

Drug Use | Suggest Off label Use Form| |View source of the data|

None

🐶 Veterinary Drug Use

None

🐶 Veterinary products

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:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source
Glycine receptor subunit alpha-1	Ion channel	P23415	GLRA1_HUMAN	BLOCKER	IC50	5.20	IUPHAR
Glycine receptor subunit alpha-2	Ion channel	P23416	GLRA2_HUMAN	BLOCKER	IC50	5.60	IUPHAR
Glycine receptor subunit beta	Ion channel	P48167	GLRB_HUMAN	BLOCKER	IC50	4.50	IUPHAR
5-hydroxytryptamine receptor 3A	Ion channel		5HT3A_MOUSE	BLOCKER	IC50	4.50	IUPHAR
GABA-A receptor; anion channel	Ion channel		GBRP_RAT GBRB1_RAT GBRD_RAT GBRG2_RAT GBRA5_RAT GBRA3_RAT GBRG1_RAT GBRA2_RAT GBRA4_RAT GBRG3_RAT GBRA6_RAT GBRA1_RAT GBRB3_RAT GBRB2_RAT Q91ZM7_RAT GBRE_RAT		IC50	5.88	CHEMBL

External reference:

ID	Source
C0031890	UMLSCUI
CHEBI:134126	CHEBI
RI5	PDB_CHEM_ID
CHEMBL1908342	ChEMBL_ID
DB00466	DRUGBANK_ID
D010852	MESH_DESCRIPTOR_UI
31304	PUBCHEM_CID
4051	IUPHAR_LIGAND_ID
ZLT174DL7U	UNII
2539172	RXNORM
001378	NDDF
57979006	SNOMEDCT_US

Pharmaceutical products:

None