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

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

Stem definition	Drug id	CAS RN
ergot alkaloid derivatives	1588	18016-80-3

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: lisuride hydrogen maleate lisuride maleate lisuride lisurid lysuride mesorgydine methylergol carbamide methylergol carbamide maleate	An ergot derivative that acts as an agonist at dopamine D2 receptors (DOPAMINE AGONISTS). It may also act as an antagonist at dopamine D1 receptors, and as an agonist at some serotonin receptors (SEROTONIN RECEPTOR AGONISTS). Molecular weight: 338.46 Formula: C20H26N4O CLOGP: 2.67 LIPINSKI: 0 HAC: 5 HDO: 2 TPSA: 51.37 ALOGS: -3.38 ROTB: 3

Drug dosage:

Dose	Unit	Route
0.60	mg	O

ADMET properties:

Property	Value	Reference
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.25 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability)	14 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution)	1.73 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	13.30 mL/min/kg	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	1.80 hours	Lombardo F, Berellini G, Obach RS

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
ATC	G02CB02	GENITO URINARY SYSTEM AND SEX HORMONES OTHER GYNECOLOGICALS OTHER GYNECOLOGICALS Prolactine inhibitors
ATC	N02CA07	NERVOUS SYSTEM ANALGESICS ANTIMIGRAINE PREPARATIONS Ergot alkaloids
MeSH PA	D018726	Anti-Dyskinesia Agents
MeSH PA	D000978	Antiparkinson Agents
MeSH PA	D002491	Central Nervous System Agents
MeSH PA	D015259	Dopamine Agents
MeSH PA	D018491	Dopamine Agonists
MeSH PA	D018377	Neurotransmitter Agents
MeSH PA	D018490	Serotonin Agents
MeSH PA	D017366	Serotonin Receptor Agonists
CHEBI has role	CHEBI:35941	serotonin agonists
CHEBI has role	CHEBI:48407	antiparkinson agent
CHEBI has role	CHEBI:51065	Dopamine receptor agonist
CHEBI has role	CHEBI:66956	antidyskinetic agent

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

Disease	Relation	SNOMED_ID	DOID
Amenorrhea	indication	14302001	DOID:13938
Migraine	indication	37796009	DOID:6364
Acromegaly	indication	74107003	DOID:2449

🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	12.8	acidic
pKa2	13.36	acidic
pKa3	6.95	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
5-hydroxytryptamine receptor 2B	GPCR	P41595	5HT2B_HUMAN	ANTAGONIST	Ki	8.49		DRUG MATRIX	DRUG LABEL
Beta-1 adrenergic receptor	GPCR	P08588	ADRB1_HUMAN		Ki	6.49		DRUG MATRIX
Beta-2 adrenergic receptor	GPCR	P07550	ADRB2_HUMAN		Ki	7.54		DRUG MATRIX
D(1A) dopamine receptor	GPCR	P21728	DRD1_HUMAN		Ki	7.11		CHEMBL
Alpha-2A adrenergic receptor	GPCR	P08913	ADA2A_HUMAN		Ki	9.94		DRUG MATRIX
5-hydroxytryptamine receptor 1A	GPCR	P08908	5HT1A_HUMAN		Ki	9.40		CHEMBL
5-hydroxytryptamine receptor 2A	GPCR	P28223	5HT2A_HUMAN		Ki	9.06		DRUG MATRIX
5-hydroxytryptamine receptor 2C	GPCR	P28335	5HT2C_HUMAN	AGONIST	Ki	8.30		IUPHAR
5-hydroxytryptamine receptor 6	GPCR	P50406	5HT6R_HUMAN		Ki	8.26		DRUG MATRIX
Alpha-1A adrenergic receptor	GPCR	P35348	ADA1A_HUMAN	ANTAGONIST	Ki	8.30		IUPHAR
Alpha-2B adrenergic receptor	GPCR	P18089	ADA2B_HUMAN		Ki	9.63		DRUG MATRIX
D(3) dopamine receptor	GPCR	P35462	DRD3_HUMAN		Ki	8.77		CHEMBL
D(1B) dopamine receptor	GPCR	P21918	DRD5_HUMAN	AGONIST	Ki	8.50		IUPHAR
Histamine H1 receptor	GPCR	P35367	HRH1_HUMAN		Ki	7.72		DRUG MATRIX
Histamine H2 receptor	GPCR	P25021	HRH2_HUMAN		Ki	5.99		DRUG MATRIX
D(2) dopamine receptor	GPCR	P14416	DRD2_HUMAN		Ki	9.30		CHEMBL
5-hydroxytryptamine receptor 1D	GPCR	P28221	5HT1D_HUMAN	AGONIST	Ki	9		IUPHAR
Alpha-2C adrenergic receptor	GPCR	P18825	ADA2C_HUMAN		Ki	9.20		DRUG MATRIX
Cytochrome P450 2D6	Enzyme	P10635	CP2D6_HUMAN		IC50	7.80		DRUG MATRIX
D(4) dopamine receptor	GPCR	P21917	DRD4_HUMAN	AGONIST	Ki	8.30		IUPHAR
Alpha-1D adrenergic receptor	GPCR	P25100	ADA1D_HUMAN		Ki	8.04		DRUG MATRIX
Alpha-1B adrenergic receptor	GPCR	P35368	ADA1B_HUMAN		Ki	7.78		PDSP
5-hydroxytryptamine receptor 1B	GPCR	P28222	5HT1B_HUMAN	AGONIST	Ki	7.70		IUPHAR
Alpha-1B adrenergic receptor	GPCR		ADA1B_RAT		Ki	7.17		DRUG MATRIX
5-hydroxytryptamine receptor 1B	GPCR		5HT1B_RAT		Ki	8.34		DRUG MATRIX
Alpha-1A adrenergic receptor	GPCR		ADA1A_RAT		IC50	7.64		CHEMBL
D(2) dopamine receptor	GPCR		DRD2_RAT		Kd	9.52		CHEMBL
5-hydroxytryptamine receptor 1A	GPCR		5HT1A_RAT		IC50	9.33		CHEMBL
5-hydroxytryptamine receptor 7	GPCR		5HT7R_RAT	AGONIST	Ki	9.30		IUPHAR
5-hydroxytryptamine receptor 6	GPCR		5HT6R_RAT	AGONIST	Ki	8.30		IUPHAR

External reference:

ID	Source
D01462	KEGG_DRUG
19875-60-6	SECONDARY_CAS_RN
C0023863	UMLSCUI
CHEBI:51164	CHEBI
H8G	PDB_CHEM_ID
CHEMBL157138	ChEMBL_ID
DB00589	DRUGBANK_ID
D008090	MESH_DESCRIPTOR_UI
28864	PUBCHEM_CID
43	IUPHAR_LIGAND_ID
3065	INN_ID
E0QN3D755O	UNII
6446	RXNORM
003989	NDDF
003990	NDDF
323159002	SNOMEDCT_US
349894007	SNOMEDCT_US
395770007	SNOMEDCT_US

Pharmaceutical products:

None