All FDA-approved EMA-approved PMDA-approved
Target Card Uniprot Example: P23975

piribedil 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | BioActivity |

Stem definition	Drug id	CAS RN
vasodilators	2202	3605-01-4

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: piribedil methanesulfonate piribedil maleate ET-495 piribedil trivastal trivastan piribedil hydrochloride piribedil HCl EU 4200 EU-4200	A dopamine D2 agonist. It is used in the treatment of parkinson disease, particularly for alleviation of tremor. It has also been used for circulatory disorders and in other applications as a D2 agonist. Molecular weight: 298.35 Formula: C16H18N4O2 CLOGP: 2.38 LIPINSKI: 0 HAC: 6 HDO: 0 TPSA: 50.72 ALOGS: -2.28 ROTB: 3

Drug dosage:

Dose	Unit	Route
0.20	g	O

ADMET properties:

Property	Value	Reference
BA (Bioavailability)	8 %

Predicted pharmacokinetic/toxicological properties (PK-AZ):

Property	Description	Value	Unit	Confidence	Similarity
azlogd74	LogD at pH 7.4	2.613		Moderate	0.72
caco2-efflux	Caco-2 efflux ratio (BA/AB)	0.348		Moderate	0.72
caco2-intrinsic-papp	Caco-2 intrinsic apparent permeability	50.234	10^-6 cm/s	Moderate	0.72
dh-clint	Dog hepatocyte intrinsic clearance	18.072	uL/min/10^6 cells	Moderate	0.72
dppb	Dog plasma protein binding (% unbound)	11.620	%	Moderate	0.72
fcs-ppb	Fetal calf serum protein binding (% unbound)	21.020	%	Moderate	0.72
herg	hERG pIC50	5.185	pIC50	Moderate	0.72
hh-clint	Human hepatocyte intrinsic clearance	9.863	uL/min/10^6 cells	Moderate	0.72
hlm-clint	Human liver microsomal intrinsic clearance	49.204	uL/min/mg protein	Moderate	0.72
hppb	Human plasma protein binding (% unbound)	7.530	%	Moderate	0.72
kinase-safety-class	ACVR2A,ACVR2B,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,FLT3,GRK2,ITK,JAK2,MAP3K21,MAP3K7,MAPK7,MAPK9,MAPKAPK2,MTOR,NTRK2,PDK2,PDK4,PIK3CB,PRKCD,PRKDC,SIK2,SIK3,STK33,TEK,TTK	35
kinase-selectivity-class	AXL,BRAF	2
mdck-mdr1-efflux	MDCK-MDR1 efflux ratio	0.122		Moderate	0.72
mh-clint	Mouse hepatocyte intrinsic clearance	119.124		Moderate	0.72
mppb	Mouse plasma protein binding (% unbound)	12.200		Moderate	0.72
nih-mdck-mdr1-efflux	NIH MDCK-MDR1 efflux ratio	0.356		Moderate	0.72
pfas-class	PFAS structural alert (1 = True, 0 = False)	0
pppb	Pig plasma protein binding (% unbound)	23.650	%	Moderate	0.72
rh-clint	Rat hepatocyte intrinsic clearance	134.586	uL/min/10^6 cells	Moderate	0.72
rh-fuinc	Rat hepatocyte fraction unbound in incubation	69.420	%	Moderate	0.72
rppb	Rat plasma protein binding (% unbound)	9.960	%	Moderate	0.72
solubility-dd	Solubility at pH 7.4 in DMSO	401.791	uM	Moderate	0.72

Approvals:

None

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Gambling disorder	69.24	61.08	12	325	1764	42619234

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Gambling disorder	77.07	47.38	13	637	2178	110586471
Fall	59.04	47.38	39	611	603443	109985206

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	N04BC08	NERVOUS SYSTEM ANTI-PARKINSON DRUGS DOPAMINERGIC AGENTS Dopamine agonists
MeSH PA	D000978	Antiparkinson Agents
MeSH PA	D015259	Dopamine Agents
MeSH PA	D018377	Neurotransmitter Agents
MeSH PA	D018491	Dopamine Agonists
MeSH PA	D018726	Anti-Dyskinesia Agents

Related Drugs by ATC class:

N04BC Dopamine agonists 8 drugs

apomorphinebromocriptinecabergolinedihydroergocryptinepergolidepramipexoleropinirolerotigotine

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

Disease	Relation	SNOMED_ID	DOID
Parkinsonism	indication	32798002

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	6.95	Basic
pKa2	2.23	Basic

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])	Mechanism action	Bioact source	MoA source
D(2) dopamine receptor	GPCR	P14416	DRD2_HUMAN	AGONIST	Ki	6.90		IUPHAR	SCIENTIFIC LITERATURE
5-hydroxytryptamine receptor 1A	GPCR	P08908	5HT1A_HUMAN	AGONIST	Ki	6.40		IUPHAR
5-hydroxytryptamine receptor 2B	GPCR	P41595	5HT2B_HUMAN	ANTAGONIST	Ki	5.90		IUPHAR
Alpha-1A adrenergic receptor	GPCR	P35348	ADA1A_HUMAN	ANTAGONIST	Ki	6.10		IUPHAR
Alpha-2B adrenergic receptor	GPCR	P18089	ADA2B_HUMAN		Ki	6.54		PDSP
Alpha-2A adrenergic receptor	GPCR	P08913	ADA2A_HUMAN	ANTAGONIST	Ki	7.10		IUPHAR
Alpha-2C adrenergic receptor	GPCR	P18825	ADA2C_HUMAN	ANTAGONIST	Ki	7.20		IUPHAR
D(4) dopamine receptor	GPCR	P21917	DRD4_HUMAN	ANTAGONIST	Ki	6.50		IUPHAR
Alpha-1D adrenergic receptor	GPCR	P25100	ADA1D_HUMAN		Ki	6.66		PDSP
Alpha-1B adrenergic receptor	GPCR	P35368	ADA1B_HUMAN		Ki	5.21		PDSP
D(3) dopamine receptor	GPCR	P35462	DRD3_HUMAN	AGONIST	Ki	6.60		IUPHAR

External reference:

ID	Source
N0000167119	NUI
D07305	KEGG_DRUG
C0031979	UMLSCUI
CHEBI:92833	CHEBI
CHEMBL1371770	ChEMBL_ID
CHEMBL1256997	ChEMBL_ID
DB12478	DRUGBANK_ID
D010891	MESH_DESCRIPTOR_UI
4850	PUBCHEM_CID
49	IUPHAR_LIGAND_ID
2569	INN_ID
DO22K1PRDJ	UNII
8353	RXNORM
005711	NDDF
1173977003	SNOMEDCT_US
713435009	SNOMEDCT_US
DO22K1PRDJ	INXIGHT DRUGS

Pharmaceutical products:

None