CARAZOLOL

Possibly Marketed Outside US

Details

Stereochemistry	RACEMIC
Molecular Formula	C18H22N2O2
Molecular Weight	298.3795
Optical Activity	( + / - )
Defined Stereocenters	0 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CC(C)NCC(O)COC1=CC=CC2=C1C3=CC=CC=C3N2

InChI

InChIKey=BQXQGZPYHWWCEB-UHFFFAOYSA-N

InChI=1S/C18H22N2O2/c1-12(2)19-10-13(21)11-22-17-9-5-8-16-18(17)14-6-3-4-7-15(14)20-16/h3-9,12-13,19-21H,10-11H2,1-2H3

HIDE SMILES / InChI

Molecular Formula	C18H22N2O2
Molecular Weight	298.3795
Charge	0
Count

Stereochemistry	RACEMIC
Additional Stereochemistry	No
Defined Stereocenters	0 / 1
E/Z Centers	0
Optical Activity	( + / - )

Description
Sources: https://www.ncbi.nlm.nih.gov/pubmed/41147 | http://www.inchem.org/documents/jecfa/jecmono/v43jec02.htm | http://europroxima.com/products/contaminants-and-residues/tranquilizers/carazol-elisa/

Carazolol is a beta1/beta2 adrenoreceptor blocking agent. Activity and safety of the drug were evaluated in clinical trials that were conducted in healthy subjects and in patients suffering from either chronic bronchitis or asthma. The drug, however, was not developed for human use. Instead, carazolol is used in to reduce stress in animals during transportation. In veterinary medicine, carazolol is given by intramuscular injection to pigs is indicated in stress-inducing situations. In cattle, carazolol is intended to be used for the prevention of shipment stress caused by transportation and formation of new herds.

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Beta-1 adrenergic receptor 158 Target ID: P08588 Gene ID: 153.0 Gene Symbol: ADRB1 Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/41147	Antagonist 2778		0.15 nM [Ki]
Beta-2 adrenergic receptor 203 Target ID: P07550\|\|\|Q53GA6\|\|\|Q9UCZ3 Gene ID: 154.0 Gene Symbol: ADRB2 Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/41147	Antagonist 2778		0.15 nM [Ki]

PubMed

Title	Date	PubMed
Carazolol, an extremely potent beta-adrenergic blocker: binding to beta-receptors in brain membranes.	1979 Jun 11	41147
Carazolol: a potent, selective beta 3-adrenoceptor agonist.	1995 Nov 30	8719421
Multiresidue analysis of tranquilizers and the beta-blocker Carazolol in meat by liquid chromatography/tandem mass spectrometry.	2001	11555876
Evidence for the binding of beta-adrenoceptor blockers to microsomal Na+/K+-ATPase in guinea pig heart preparations.	2001 Jan	11201505
Separation of carvedilol enantiomers in very small volumes of human plasma by capillary electrophoresis with laser-induced fluorescence.	2001 May 5	11393694
Development of a rapid screening test for veterinary sedatives and the beta-blocker carazolol in porcine kidney by ELISA.	2004 Feb	14752562
Screening for library-assisted identification and fully validated quantification of 22 beta-blockers in blood plasma by liquid chromatography-mass spectrometry with atmospheric pressure chemical ionization.	2004 Nov 26	15595665
Influence of supplemental magnesium, tryptophan, vitamin C, and vitamin E on stress responses of pigs to vibration.	2005 Jul	15956466
Adrenergic stimulation and blocking of hormonal secretion activity of cultured cow granulosa cells.	2006 Nov	17242478
Selective structure-based virtual screening for full and partial agonists of the beta2 adrenergic receptor.	2008 Aug 28	18680279
Structure of a beta1-adrenergic G-protein-coupled receptor.	2008 Jul 24	18594507
Crystallizing thinking about the beta2-adrenergic receptor.	2008 May	18239031
On the applicability of GPCR homology models to computer-aided drug discovery: a comparison between in silico and crystal structures of the beta2-adrenergic receptor.	2008 May 22	18442228
Structural constraints for the binding of short peptides to claudin-4 revealed by surface plasmon resonance.	2008 Nov 7	18782762
Use of the X-ray structure of the beta2-adrenergic receptor for drug discovery. Part 2: Identification of active compounds.	2008 Oct 15	18829308
Structural basis for ligand binding and specificity in adrenergic receptors: implications for GPCR-targeted drug discovery.	2008 Oct 21	18821775
Virtual screening of GPCRs: an in silico chemogenomics approach.	2008 Sep 6	18775075
Ligand-specific regulation of the extracellular surface of a G-protein-coupled receptor.	2010 Jan 7	20054398
Predicting drug-target interaction networks based on functional groups and biological features.	2010 Mar 11	20300175
Cell distribution after intracoronary bone marrow stem cell delivery in damaged and undamaged myocardium: implications for clinical trials.	2010 Mar 15	20504285
Structure-based discovery of A2A adenosine receptor ligands.	2010 May 13	20405927

Substance Class	Chemical Created by `admin` on `Fri Dec 15 16:33:13 GMT 2023` Edited by `admin` on `Fri Dec 15 16:33:13 GMT 2023`
Record UNII	29PW75S82A
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

CARAZOLOL

Official Name

English

SUACRON

Brand Name

English

carazolol [INN]

Common Name

English

CARAZOLOL [MART.]

Common Name

English

CONDUCTON

Brand Name

English

BM-51052

Code

English

1-(CARBAZOL-4-YLOXY)-3-(ISOPROPYLAMINO)-2-PROPANOL

Systematic Name

English

Carazolol [WHO-DD]

Common Name

English

BM 51052

Code

English

CARAZOLOL [MI]

Common Name

English

Classification Tree Code System Code

WHO-VATC

QC07AA90