Therapeutic Targets Database
BIDD Pharmainformatics Databases


TTD Target ID: TTDS00036

Target Information
NameBeta-1 adrenergic receptor    
Type of targetSuccessful target    
SynonymsBeta-1 adrenoceptor    
Beta-1 adrenoreceptor    
DiseaseAnxiety disorder, unspecified
[ICD9: 300   ICD10: F40-F42]
[ICD9: 493   ICD10: J45]
Cardiac arrhythmias
[ICD9: 427   ICD10: I47-I49]
Cardiovascular disease, unspecified
[ICD9: 390-459   ICD10: I00-I99]
Coronary heart disease
[ICD9: 414.0   ICD10: I25.1]
Dilated cardiomyopathy
[ICD9: 425.4   ICD10: I42.0]
[ICD9: 365   ICD10: H40-H42]
[ICD9: 401   ICD10: I10, I11, I12, I13, I15]
AjmalicineApprovedCirculatory disorders[6][7][8]
DobutamineApprovedHeart failure and cardiogenic shock[13][3]
EsmololApprovedAcute supraventricular tachycardia[14]
PractololApprovedCardiac arrhythmias[18][19]
SotalolApprovedMaintenance of normal sinus rhythm[20]
BioChemical ClassG-protein coupled receptor (rhodopsin family)    
UniProt IDP08588
PDB Structure2LSQ.    
FunctionBeta-adrenergic receptors mediate the catecholamine- induced activation of adenylate cyclase through the action of G proteins. This receptor binds epinephrine and norepinephrine with approximatively equal affinity.    
Target ValidationClick to Find Target Validation Information.    
Inhibitor (+/-)-nantenine[21]
1- (1H-Indol-4-yloxy)-3-phenethylamino-propan-2-ol[23]
1- (2-allylphenoxy)-3-morpholinopropan-2-ol[24]
1- (2-isopropylphenoxy)-3-morpholinopropan-2-ol[24]
4- (4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one[25]
CGP 20712A[32]
CGP 26505[33]
Cross References 3D Structure
Related Literature
On-Line Medical Dictionary
Ref 1Current therapeutic uses and potential of beta-adrenoceptor agonists and antagonists. Eur J Clin Pharmacol. 1998 Feb;53(6):389-404. To Reference
Ref 2Probing the immunological properties of the extracellular domains of the human beta(1)-adrenoceptor. J Autoimmun. 1999 Sep;13(2):179-86. To Reference
Ref 3Autoimmunity in idiopathic dilated cardiomyopathy. Characterization of antibodies against the beta 1-adrenoceptor with positive chronotropic effect. Circulation. 1994 Jun;89(6):2760-7. To Reference
Ref 4Betaxolol, a beta(1)-adrenoceptor antagonist, reduces Na(+) influx into cortical synaptosomes by direct interaction with Na(+) channels: comparison with other beta-adrenoceptor antagonists. Br J Pharmacol. 2000 Jun;130(4):759-66. To Reference
Ref 5Prediction and experimental validation of acute toxicity of beta-blockers in Ceriodaphnia dubia. Environ Toxicol Chem. 2005 Oct;24(10):2470-6. To Reference
Ref 63879679 To Reference
Ref 7Needs for new plant-derived pharmaceuticals in the post-genome era an industrial view in drug research and development, 2008 by Ying Wang To Reference
Ref 8Plant Based Drugs and Medicines, by Leslie Taylor, in Raintree Nutrition, Inc., on October 13, 2000 To Reference
Ref 9Beta-blockers alprenolol and carvedilol stimulate beta-arrestin-mediated EGFR transactivation. Proc Natl Acad Sci U S A. 2008 Sep 23;105(38):14555-60. Epub 2008 Sep 11. To Reference
Ref 10Inverse agonist activities of beta-adrenoceptor antagonists in rat myocardium. Br J Pharmacol. 1999 Jun;127(4):895-902. To Reference
Ref 11beta-adrenergic enhancement of brain kynurenic acid production mediated via cAMP-related protein kinase A signaling. Prog Neuropsychopharmacol Biol Psychiatry. 2009 Apr 30;33(3):519-29. Epub 2009 Feb 12. To Reference
Ref 12Antiarrhythmic effect of bisoprolol, a highly selective beta1-blocker, in patients with paroxysmal atrial fibrillation. Int Heart J. 2008 May;49(3):281-93. To Reference
Ref 13Beta-adrenoceptor alterations coupled with secretory response and experimental periodontitis in rat submandibular glands. Arch Oral Biol. 2008 Jun;53(6):509-16. Epub 2008 Feb 13. To Reference
Ref 14Beta-1 selective adrenergic antagonist landiolol and esmolol can be safely used in patients with airway hyperreactivity. Heart Lung. 2009 Jan-Feb;38(1):48-55. Epub 2008 Sep 11. To Reference
Ref 15J Ocul Pharmacol Ther. 2004 Apr;20(2):93-9.Binding affinities of ocular hypotensive beta-blockers levobetaxolol, levobunolol, and timolol at endogenous guinea pig beta-adrenoceptors. To Reference
Ref 16Nat Rev Drug Discov. 2003 Jan;2(1):38-51.Knockouts model the 100 best-selling drugs--will they model the next 100? To Reference
Ref 17Nitric oxide mechanisms of nebivolol. Ther Adv Cardiovasc Dis. 2009 Aug;3(4):317-27. Epub 2009 May 14. To Reference
Ref 18Prostaglandin E2 synthesis elicited by adrenergic stimuli in guinea pig trachea is mediated primarily via activation of beta 2 adrenergic receptors. Prostaglandins. 1992 Nov;44(5):399-412. To Reference
Ref 19TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. To Reference
Ref 20beta(2)-adrenoceptors are critical for antidepressant treatment of neuropathic pain. Ann Neurol. 2009 Feb;65(2):218-25. To Reference
Ref 21Bioorg Med Chem Lett. 2010 Jan 15;20(2):628-31. Epub 2009 Nov 20.Synthetic studies and pharmacological evaluations on the MDMA ('Ecstasy') antagonist nantenine. To Reference
Ref 22J Med Chem. 2007 Jun 14;50(12):2903-15. Epub 2007 May 17.Comparative molecular field analysis of the binding of the stereoisomers of fenoterol and fenoterol derivatives to the beta2 adrenergic receptor. To Reference
Ref 23J Med Chem. 1986 Aug;29(8):1524-7.Synthesis and beta-adrenergic receptor blocking potency of 1-(substituted amino)-3-(4-indolyloxy)propan-2-ols. To Reference
Ref 24Bioorg Med Chem Lett. 2010 Jun 1;20(11):3399-404. Epub 2010 Apr 9.A vHTS approach for the identification of beta-adrenoceptor ligands. To Reference
Ref 25J Med Chem. 2010 Sep 9;53(17):6386-97.Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential. To Reference
Ref 26Bioorg. Med. Chem. Lett. 7(12):1583-1588 (1997) To Reference
Ref 27J Med Chem. 1980 Mar;23(3):285-9.Antihypertensive indole derivatives of phenoxypropanolamines with beta-adrenergic receptor antagonist and vasodilating activity. To Reference
Ref 28J Med Chem. 2001 Apr 26;44(9):1456-66.(4-Piperidin-1-yl)phenyl amides: potent and selective human beta(3) agonists. To Reference
Ref 29J Med Chem. 1994 May 13;37(10):1518-25.The [(methyloxy)imino]methyl moiety as a bioisoster of aryl. A novel class of completely aliphatic beta-adrenergic receptor antagonists. To Reference
Ref 30Bioorg Med Chem Lett. 2010 Mar 15;20(6):1895-9. Epub 2010 Feb 4.Heterocyclic acetamide and benzamide derivatives as potent and selective beta3-adrenergic receptor agonists with improved rodent pharmacokinetic profiles. To Reference
Ref 31Classification of the beta-adrenoceptor subtype in the rat portal vein: effect of altered thyroid hormone levels. Eur J Pharmacol. 1992 Mar 3;212(2-3):201-7. To Reference
Ref 32Distribution of beta 1- and beta 2-adrenoceptor subtypes in various mouse tissues. Neurosci Lett. 1993 Sep 17;160(1):96-100. To Reference
Ref 33Uptake of radioligands by rat heart and lung in vivo: CGP 12177 does and CGP 26505 does not reflect binding to beta-adrenoceptors. Eur J Pharmacol. 1992 Nov 3;222(1):107-12. To Reference


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