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
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
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 |
---|---|---|---|
Target ID: P08588 Gene ID: 153.0 Gene Symbol: ADRB1 Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/41147 |
0.15 nM [Ki] | ||
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 |
0.15 nM [Ki] |
PubMed
Title | Date | PubMed |
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Carazolol: a potent, selective beta 3-adrenoceptor agonist. | 1995 Nov 30 |
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Multiresidue analysis of tranquilizers and the beta-blocker Carazolol in meat by liquid chromatography/tandem mass spectrometry. | 2001 |
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Separation of carvedilol enantiomers in very small volumes of human plasma by capillary electrophoresis with laser-induced fluorescence. | 2001 May 5 |
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Integrated acquisition of analytical and biopharmaceutical screening data for beta-adrenergic-drugs employing diversified macrocycle supported potentiometric detection in HPLC systems. | 2002 Aug |
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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 |
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Effect of carazolol on the oestrous behaviour and concentrations of luteinising hormone and steroids in lactating cows during the periovulatory period. | 2007 Jun 9 |
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Biochemistry. Signaling across the cell membrane. | 2007 Nov 23 |
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High-resolution crystal structure of an engineered human beta2-adrenergic G protein-coupled receptor. | 2007 Nov 23 |
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GPCR engineering yields high-resolution structural insights into beta2-adrenergic receptor function. | 2007 Nov 23 |
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Comprehensive screening and quantification of veterinary drugs in milk using UPLC-ToF-MS. | 2008 Jul |
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Active state-like conformational elements in the beta2-AR and a photoactivated intermediate of rhodopsin identified by dynamic properties of GPCRs. | 2008 Jul 15 |
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Structure of a beta1-adrenergic G-protein-coupled receptor. | 2008 Jul 24 |
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Crystallizing thinking about the beta2-adrenergic receptor. | 2008 May |
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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 |
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Use of the X-ray structure of the beta2-adrenergic receptor for drug discovery. Part 2: Identification of active compounds. | 2008 Oct 15 |
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Structural basis for ligand binding and specificity in adrenergic receptors: implications for GPCR-targeted drug discovery. | 2008 Oct 21 |
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Virtual screening of GPCRs: an in silico chemogenomics approach. | 2008 Sep 6 |
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Computing highly correlated positions using mutual information and graph theory for G protein-coupled receptors. | 2009 |
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Rapid method for the determination of tranquilizers and a beta-blocker in porcine and bovine kidney by liquid chromatography with tandem mass spectrometry. | 2009 Apr 1 |
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Chiral separation of beta-adrenergic blockers on CelluCoat column by HPLC. | 2009 Apr 30 |
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Analysis of full and partial agonists binding to beta2-adrenergic receptor suggests a role of transmembrane helix V in agonist-specific conformational changes. | 2009 Jul-Aug |
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Allosteric modulation of adenosine receptors. | 2009 Mar |
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Identifying conformational changes of the beta(2) adrenoceptor that enable accurate prediction of ligand/receptor interactions and screening for GPCR modulators. | 2009 May |
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Ligand-regulated oligomerization of beta(2)-adrenoceptors in a model lipid bilayer. | 2009 Nov 4 |
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FoldGPCR: structure prediction protocol for the transmembrane domain of G protein-coupled receptors from class A. | 2010 Aug 1 |
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Dynamics of the beta2-adrenergic G-protein coupled receptor revealed by hydrogen-deuterium exchange. | 2010 Feb 1 |
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Forced unbinding of GPR17 ligands from wild type and R255I mutant receptor models through a computational approach. | 2010 Mar 16 |
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QC07AA90
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C29576
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260-945-1
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20192
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m3050
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71739
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DTXSID00866648
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CHEMBL324665
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Carazolol
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569
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100000081608
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57775-29-8
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C77941
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SUB06086MIG
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487
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C014382
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ACTIVE MOIETY