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

Stem definition	Drug id	CAS RN
	1443	26844-12-2

Description:

Molecule

Description

Molfile Inchi Smiles

Synonyms:

Wy21901
Wy 21901
Wy-21901
indoramin
indoramine

An alpha-1 adrenergic antagonist that is commonly used as an antihypertensive agent.

Molecular weight: 347.46
Formula: C22H25N3O
CLOGP: 2.84
LIPINSKI: 0
HAC: 4
HDO: 2
TPSA: 48.13
ALOGS: -4.60
ROTB: 5

Drug dosage:

None

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	5 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	8.22 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability)	18 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution)	4.90 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	20 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.15 %	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	4.30 hours	Lombardo F, Berellini G, Obach RS

Approvals:

Date	Agency	Company	Orphan
Jan. 1, 1981	YEAR INTRODUCED

FDA Adverse Event Reporting System (Female)

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
Lower urinary tract symptoms	38.07	31.50	3	3	46	63488970

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	C02CA02	CARDIOVASCULAR SYSTEM ANTIHYPERTENSIVES ANTIADRENERGIC AGENTS, PERIPHERALLY ACTING Alpha-adrenoreceptor antagonists
MeSH PA	D018663	Adrenergic Agents
MeSH PA	D058668	Adrenergic alpha-1 Receptor Antagonists
MeSH PA	D000317	Adrenergic alpha-Antagonists
MeSH PA	D018674	Adrenergic Antagonists
MeSH PA	D000959	Antihypertensive Agents
MeSH PA	D002317	Cardiovascular Agents
MeSH PA	D018377	Neurotransmitter Agents

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

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	12.08	acidic
pKa2	13.42	acidic
pKa3	7.43	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
Alpha-2A adrenergic receptor	GPCR	P08913	ADA2A_HUMAN		Ki	5.65		CHEMBL
Alpha-1A adrenergic receptor	GPCR	P35348	ADA1A_HUMAN		Ki	8.43		CHEMBL
Alpha-2B adrenergic receptor	GPCR	P18089	ADA2B_HUMAN		Ki	6.28		CHEMBL
Alpha-2C adrenergic receptor	GPCR	P18825	ADA2C_HUMAN		Ki	6.32		CHEMBL
D(4) dopamine receptor	GPCR	P21917	DRD4_HUMAN		Ki	7.75		WOMBAT-PK
Alpha-1D adrenergic receptor	GPCR	P25100	ADA1D_HUMAN		Ki	6.96		CHEMBL
Alpha-1B adrenergic receptor	GPCR	P35368	ADA1B_HUMAN		Ki	7.60		CHEMBL
Alpha-1D adrenergic receptor	GPCR		ADA1D_RAT		Ki	6.21		CHEMBL
Alpha-1A adrenergic receptor	GPCR		ADA1A_BOVIN		Ki	7.92		CHEMBL
Adrenergic receptor alpha-2	GPCR		ADA2B_RAT ADA2C_RAT ADA2A_RAT		Ki	4.92		CHEMBL
Adrenergic receptor alpha-1	GPCR		ADA1B_RAT ADA1D_RAT ADA1A_RAT		Ki	7.61		CHEMBL

External reference:

ID	Source
N0000167199	NUI
D04531	KEGG_DRUG
C0021252	UMLSCUI
CHEBI:135470	CHEBI
CHEMBL279516	ChEMBL_ID
DB08950	DRUGBANK_ID
D007217	MESH_DESCRIPTOR_UI
33625	PUBCHEM_CID
501	IUPHAR_LIGAND_ID
3064	INN_ID
0Z802HMY7H	UNII
5784	RXNORM
003737	NDDF
349913001	SNOMEDCT_US
395748009	SNOMEDCT_US

Pharmaceutical products:

None