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

Stem definition	Drug id	CAS RN
beta-adrenoreceptor antagonists	137	13655-52-2

Description:

Molecule

Description

Molfile Inchi Smiles

Synonyms:

alprenolol
alpheprol
dl-Alprenolol
(RS)-Alprenolol
(+/-)-Alprenolol
alprenoxime hydrochloride
alprenolol hydrochloride
alprenoxime HCl
alprenolol HCl

One of the ADRENERGIC BETA-ANTAGONISTS used as an antihypertensive, anti-anginal, and anti-arrhythmic agent.

Molecular weight: 249.35
Formula: C15H23NO2
CLOGP: 2.65
LIPINSKI: 0
HAC: 3
HDO: 2
TPSA: 41.49
ALOGS: -3.12
ROTB: 8

Drug dosage:

Dose	Unit	Route
0.40	g	O
0.40	g	P

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	50 mg/mL	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	0.50 %	Benet LZ, Broccatelli F, Oprea TI
BA (Bioavailability)	8 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution)	3.20 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	15 mL/min/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.18 %	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	2.50 hours	Lombardo F, Berellini G, Obach RS

Approvals:

Date	Agency	Company	Orphan
Jan. 1, 1966	YEAR INTRODUCED

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	C07AA01	CARDIOVASCULAR SYSTEM BETA BLOCKING AGENTS BETA BLOCKING AGENTS Beta blocking agents, non-selective
MeSH PA	D018663	Adrenergic Agents
MeSH PA	D018674	Adrenergic Antagonists
MeSH PA	D000319	Adrenergic beta-Antagonists
MeSH PA	D000889	Anti-Arrhythmia Agents
MeSH PA	D000959	Antihypertensive Agents
MeSH PA	D002317	Cardiovascular Agents
MeSH PA	D018377	Neurotransmitter Agents
MeSH PA	D018373	Peripheral Nervous System Agents
MeSH PA	D013565	Sympatholytics
CHEBI has role	CHEBI:35530	beta-adrenergic blockers
CHEBI has role	CHEBI:35674	antihypertensive drugs
CHEBI has role	CHEBI:38070	antiarrhythmic agent
CHEBI has role	CHEBI:66991	sympatholytic drug

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	9.19	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
Beta-1 adrenergic receptor	GPCR	P08588	ADRB1_HUMAN	ANTAGONIST	Kd	9.68		SCIENTIFIC LITERATURE	KEGG DRUG
Beta-2 adrenergic receptor	GPCR	P07550	ADRB2_HUMAN	ANTAGONIST	Kd	9.66		SCIENTIFIC LITERATURE	IUPHAR
Beta-3 adrenergic receptor	GPCR	P13945	ADRB3_HUMAN		Kd	6.86		CHEMBL
5-hydroxytryptamine receptor 1A	GPCR	P08908	5HT1A_HUMAN		Ki	7.67		CHEMBL
5-hydroxytryptamine receptor 2A	GPCR	P28223	5HT2A_HUMAN		Ki	5.29		PDSP
5-hydroxytryptamine receptor 1A	GPCR		5HT1A_RAT		Ki	6.93		CHEMBL
Beta-2 adrenergic receptor	GPCR		ADRB2_BOVIN		IC50	8.53		CHEMBL
Squalene synthase	Enzyme		FDFT_RAT		IC50	5.38		CHEMBL

External reference:

ID	Source
N0000166828	NUI
D01182	KEGG_DRUG
597	RXNORM
C0002334	UMLSCUI
CHEBI:51211	CHEBI
CHEMBL266195	ChEMBL_ID
DB00866	DRUGBANK_ID
D000526	MESH_DESCRIPTOR_UI
2119	PUBCHEM_CID
563	IUPHAR_LIGAND_ID
2461	INN_ID
121009-30-1	SECONDARY_CAS_RN
13707-88-5	SECONDARY_CAS_RN
877K5MQ27W	UNII
96294004	SNOMEDCT_US
CHEMBL2448147	ChEMBL_ID
CHEMBL1256179	ChEMBL_ID
005225	NDDF
006317	NDDF

Pharmaceutical products:

None