Target Information
Target General Infomation | |||||
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Target ID |
T44068
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Former ID |
TTDS00036
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Target Name |
Beta-1 adrenergic receptor
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Gene Name |
ADRB1
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Synonyms |
Beta-1 adrenoceptor; Beta-1 adrenoreceptor; ADRB1
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Target Type |
Successful
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Disease | Angina pectoris [ICD9: 413; ICD10: I20] | ||||
Acute supraventricular tachycardia [ICD9: 427.0, 427.89; ICD10: I47.1] | |||||
Allergy; Sepsis [ICD9:995.3, 995.91; ICD10: T78.4, A40, A41] | |||||
Angina pectoris; Hypertension [ICD9:413, 401; ICD10: I20, I10-I16] | |||||
Bronchodilator [ICD9: 493; ICD10: J45] | |||||
Chronic open-angle glaucoma [ICD10: H40] | |||||
Chronic open-angle glaucoma; Ocular hypertension [ICD10: H40] | |||||
Central and peripheral nervous diseases [ICD10: G96.9] | |||||
Circulatory disorders [ICD10: I00-I99] | |||||
Coronary artery disease [ICD9: 410-414, 429.2; ICD10: I20-I25] | |||||
Cardiac arrhythmias [ICD9: 427; ICD10: I47-I49] | |||||
Diabetes [ICD9: 253.5, 588.1; ICD10: E23.2, N25.1] | |||||
Glaucoma [ICD9: 365; ICD10: H40-H42] | |||||
Hypertension; Ventricular premature beats [ICD10: I10-I16] | |||||
High blood pressure; Angina [ICD9: 401, 413; ICD10: I10, I11, I12, I13, I15, I20] | |||||
Hypertension [ICD9: 401; ICD10: I10-I16] | |||||
Hypertension; Angina [ICD9: 401, 413; ICD10: I10-I16, I20] | |||||
Hypertension; Heart arrhythmia [ICD9:401; ICD10: I10-I16, I47-I49] | |||||
High blood pressure [ICD9: 401; ICD10: I10-I16] | |||||
Heart failure; Cardiogenic shock [ICD9: 428.0, 785.51; ICD10: I50, R57.0] | |||||
Heart failure [ICD9: 428; ICD10: I50] | |||||
Hypertension; Angina pectoris [ICD9:401, 413; ICD10: I10-I16, I20] | |||||
Maintenance of normal sinus rhythm [ICD9: 427; ICD10: I46-I49] | |||||
Migraine [ICD9: 346; ICD10: G43] | |||||
Obesity [ICD9: 278; ICD10: E66] | |||||
Open-angle glaucoma [ICD9: 365; ICD10: H40-H42] | |||||
Open-angle glaucoma; Ocular hypertension [ICD9: 365, 365.04; ICD10: H40-H42, H40.0] | |||||
Septic shock; Neurogenic shock [ICD9: 785, 785.52; ICD10: R57.8, R65.21] | |||||
Ventricular fibrillation [ICD10: I49.01] | |||||
Function |
Beta-adrenergic receptors mediatethe catecholamine- induced activation of adenylate cyclase through the action of G proteins. This receptor binds epinephrine and norepinephrine with approximately equal affinity. Mediates Ras activation through G(s)-alpha- and cAMP-mediated signaling.
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BioChemical Class |
GPCR rhodopsin
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Target Validation |
T44068
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UniProt ID | |||||
Sequence |
MGAGVLVLGASEPGNLSSAAPLPDGAATAARLLVPASPPASLLPPASESPEPLSQQWTAG
MGLLMALIVLLIVAGNVLVIVAIAKTPRLQTLTNLFIMSLASADLVMGLLVVPFGATIVV WGRWEYGSFFCELWTSVDVLCVTASIETLCVIALDRYLAITSPFRYQSLLTRARARGLVC TVWAISALVSFLPILMHWWRAESDEARRCYNDPKCCDFVTNRAYAIASSVVSFYVPLCIM AFVYLRVFREAQKQVKKIDSCERRFLGGPARPPSPSPSPVPAPAPPPGPPRPAAAAATAP LANGRAGKRRPSRLVALREQKALKTLGIIMGVFTLCWLPFFLANVVKAFHRELVPDRLFV FFNWLGYANSAFNPIIYCRSPDFRKAFQRLLCCARRAARRRHATHGDRPRASGCLARPGP PPSPGAASDDDDDDVVGATPPARLLEPWAGCNGGAAADSDSSLDEPCRPGFASESKV |
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Structure |
2LSQ
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Drugs and Mode of Action | |||||
Drug(s) | Acebutolol | Drug Info | Approved | Hypertension; Ventricular premature beats | [551871] |
Ajmalicine | Drug Info | Approved | Circulatory disorders | [551871] | |
Anisodamine | Drug Info | Approved | Central and peripheral nervous diseases | [551871] | |
Anisodine | Drug Info | Approved | Central and peripheral nervous diseases | [551871] | |
Arbutamine | Drug Info | Approved | Coronary artery disease | [550707] | |
Atenolol | Drug Info | Approved | Hypertension | [538246], [540879] | |
Betaxolol | Drug Info | Approved | Hypertension | [536361], [540888] | |
Bethanidine | Drug Info | Approved | Hypertension; Heart arrhythmia | [537811], [542606], [551871] | |
Bisoprolol | Drug Info | Approved | Hypertension | [536361], [542136] | |
Bretylium | Drug Info | Approved | Ventricular fibrillation | [551871] | |
Carteolol | Drug Info | Approved | Glaucoma | [551871] | |
Dipivefrin | Drug Info | Approved | Chronic open-angle glaucoma | [551871] | |
Dobutamine | Drug Info | Approved | Heart failure; Cardiogenic shock | [538260], [540787] | |
Epinephrine | Drug Info | Approved | Allergy; Sepsis | [468151], [551871], [552007] | |
Esmolol | Drug Info | Approved | Acute supraventricular tachycardia | [536361], [542188] | |
Levobetaxolol | Drug Info | Approved | Chronic open-angle glaucoma; Ocular hypertension | [551871] | |
Levobunolol | Drug Info | Approved | Open-angle glaucoma | [536361], [541042] | |
Metipranolol | Drug Info | Approved | Open-angle glaucoma; Ocular hypertension | [538301], [542255], [551871] | |
Metoprolol | Drug Info | Approved | Angina pectoris; Hypertension | [525887], [536116], [540921] | |
Nadolol | Drug Info | Approved | High blood pressure; Angina | [538266], [540927] | |
Nebivolol | Drug Info | Approved | Hypertension | [536361], [542263] | |
Norepinephrine | Drug Info | Approved | Septic shock; Neurogenic shock | [468140], [538181] | |
Oxprenolol | Drug Info | Approved | Angina pectoris; Hypertension | [533372], [533792], [538499], [542273] | |
Penbutolol | Drug Info | Approved | Hypertension; Angina pectoris | [537669], [542282], [551871] | |
Pindolol | Drug Info | Approved | Hypertension; Angina | [538063], [543300] | |
Practolol | Drug Info | Approved | Cardiac arrhythmias | [535807], [540932] | |
Propranolol | Drug Info | Approved | Migraine | [536650], [542585] | |
Protokylol Hydrochloride | Drug Info | Approved | Bronchodilator | [551871] | |
Sotalol | Drug Info | Approved | Maintenance of normal sinus rhythm | [536095], [542317] | |
Timolol | Drug Info | Approved | High blood pressure | [537619], [540995] | |
BRL 35135 | Drug Info | Phase 2 | Diabetes | [533732], [534258] | |
BUCINDOLOL | Drug Info | Phase 2 | Hypertension | [524493] | |
COR-1 | Drug Info | Phase 2 | Heart failure | [532040] | |
L-796568 | Drug Info | Phase 1 | Obesity | [526432] | |
YM-16151-4 | Drug Info | Phase 1 | Hypertension | [533693] | |
Alprenolol | Drug Info | Withdrawn from market | Hypertension | [540993], [550781] | |
Cetamolol | Drug Info | Terminated | Angina pectoris | [544568] | |
L-755507 | Drug Info | Terminated | Discovery agent | [540554], [546489] | |
Inhibitor | (+/-)-nantenine | Drug Info | [530558] | ||
(R,R)-(-)-fenoterol | Drug Info | [528842] | |||
(R,S)-(-)-fenoterol | Drug Info | [528842] | |||
1-(1H-Indol-4-yloxy)-3-phenethylamino-propan-2-ol | Drug Info | [533374] | |||
1-(2-allylphenoxy)-3-morpholinopropan-2-ol | Drug Info | [530883] | |||
1-(2-isopropylphenoxy)-3-morpholinopropan-2-ol | Drug Info | [530883] | |||
4-(4-butylpiperidin-1-yl)-1-o-tolylbutan-1-one | Drug Info | [531079] | |||
CGP-12177A | Drug Info | [526033] | |||
DICHLOROISOPROTERENOL | Drug Info | [533801] | |||
L-755507 | Drug Info | [526033] | |||
L-796568 | Drug Info | [530748] | |||
Antagonist | Acebutolol | Drug Info | [536152], [538095] | ||
Alprenolol | Drug Info | [534890], [536850] | |||
Atenolol | Drug Info | [536152], [538095] | |||
Betaxolol | Drug Info | [535001], [537316] | |||
Bethanidine | Drug Info | [537779] | |||
Bisoprolol | Drug Info | [536769], [537916] | |||
Bretylium | Drug Info | [537646], [537704] | |||
Cebutolol | Drug Info | [538095] | |||
CGP 20712A | Drug Info | [537882] | |||
CGP 26505 | Drug Info | [535815] | |||
COR-1 | Drug Info | [532040] | |||
Dipivefrin | Drug Info | [537986] | |||
Esmolol | Drug Info | [537023] | |||
Levobetaxolol | Drug Info | [535957] | |||
Levobunolol | Drug Info | [537782] | |||
Metipranolol | Drug Info | [536102] | |||
Metoprolol | Drug Info | [535660], [536152], [538095] | |||
Nebivolol | Drug Info | [537327] | |||
Oxprenolol | Drug Info | [536152] | |||
Penbutolol | Drug Info | [535478], [537649] | |||
Pindolol | Drug Info | [536398] | |||
Practolol | Drug Info | [535324], [535807] | |||
Propranolol | Drug Info | [537409] | |||
Sotalol | Drug Info | [537126] | |||
Timolol | Drug Info | [536072], [536320], [538022] | |||
Modulator | Ajmalicine | Drug Info | [533488] | ||
Anisodamine | Drug Info | [533488] | |||
Anisodine | Drug Info | [533488] | |||
BUCINDOLOL | Drug Info | ||||
Cetamolol | Drug Info | [532040], [532693] | |||
Nadolol | Drug Info | [556264] | |||
Protokylol Hydrochloride | Drug Info | ||||
YM-16151-4 | Drug Info | [533693] | |||
Stimulator | Arbutamine | Drug Info | [537972] | ||
Norepinephrine | Drug Info | [534841] | |||
Agonist | BRL 35135 | Drug Info | [537997] | ||
Carazolol | Drug Info | [538095] | |||
Carteolol | Drug Info | [535096], [536812] | |||
Dobutamine | Drug Info | [536628], [537916] | |||
Epinephrine | Drug Info | [537361] | |||
Isoprenaline | Drug Info | [538095] | |||
Noradrenaline | Drug Info | [535812] | |||
Pathways | |||||
KEGG Pathway | Calcium signaling pathway | ||||
cGMP-PKG signaling pathway | |||||
cAMP signaling pathway | |||||
Neuroactive ligand-receptor interaction | |||||
Endocytosis | |||||
Adrenergic signaling in cardiomyocytes | |||||
Gap junction | |||||
Salivary secretion | |||||
Dilated cardiomyopathy | |||||
PANTHER Pathway | Heterotrimeric G-protein signaling pathway-Gi alpha and Gs alpha mediated pathway | ||||
Beta1 adrenergic receptor signaling pathway | |||||
PathWhiz Pathway | Muscle/Heart Contraction | ||||
Reactome | Adrenoceptors | ||||
G alpha (s) signalling events | |||||
WikiPathways | Monoamine GPCRs | ||||
Calcium Regulation in the Cardiac Cell | |||||
GPCRs, Class A Rhodopsin-like | |||||
Endothelin Pathways | |||||
GPCR ligand binding | |||||
GPCR downstream signaling | |||||
References | |||||
Ref 468140 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 505). | ||||
Ref 468151 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 509). | ||||
Ref 524493 | ClinicalTrials.gov (NCT01970501) Genetically Targeted Therapy for the Prevention of Symptomatic Atrial Fibrillation in Patients With Heart Failure. U.S. National Institutes of Health. | ||||
Ref 526432 | Effect of a 28-d treatment with L-796568, a novel beta(3)-adrenergic receptor agonist, on energy expenditure and body composition in obese men. Am J Clin Nutr. 2002 Oct;76(4):780-8. | ||||
Ref 532040 | Administration of the cyclic peptide COR-1 in humans (phase I study): ex vivo measurements of anti-beta1-adrenergic receptor antibody neutralization and of immune parameters. Eur J Heart Fail. 2012 Nov;14(11):1230-9. | ||||
Ref 533372 | The beta 1- and beta 2-adrenoceptor stimulatory effects of alprenolol, oxprenolol and pindolol: a study in the isolated right atrium and uterus of the rat. Br J Pharmacol. 1986 Apr;87(4):657-64. | ||||
Ref 533693 | Antianginal effects of YM-16151-4 in various experimental angina models. J Cardiovasc Pharmacol. 1993 May;21(5):701-8. | ||||
Ref 533732 | Acute effects of the beta 3-adrenoceptor agonist, BRL 35135, on tissue glucose utilisation. Br J Pharmacol. 1995 Feb;114(4):888-94. | ||||
Ref 533792 | Controlled evaluation of the beta adrenoceptor blocking drug oxprenolol in anxiety. Med J Aust. 1976 Jun 12;1(24):909-12. | ||||
Ref 534258 | Biphasic effects of the beta-adrenoceptor agonist, BRL 37344, on glucose utilization in rat isolated skeletal muscle. Br J Pharmacol. 1996 Mar;117(6):1355-61. | ||||
Ref 535807 | Prostaglandin 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. | ||||
Ref 536095 | New antiarrhythmic agents for atrial fibrillation and atrial flutter. Expert Opin Emerg Drugs. 2005 May;10(2):311-22. | ||||
Ref 536116 | The effect of food on the relative bioavailability of rapidly dissolving immediate-release solid oral products containing highly soluble drugs. Mol Pharm. 2004 Sep-Oct;1(5):357-62. | ||||
Ref 536361 | Natural products as sources of new drugs over the last 25 years. J Nat Prod. 2007 Mar;70(3):461-77. Epub 2007 Feb 20. | ||||
Ref 536650 | Emerging drugs for complications of end-stage liver disease. Expert Opin Emerg Drugs. 2008 Mar;13(1):159-74. | ||||
Ref 537619 | Brinzolamide/timolol fixed combination: a new ocular suspension for the treatment of open-angle glaucoma and ocular hypertension. Expert Opin Pharmacother. 2009 Aug;10(12):2015-24. | ||||
Ref 537669 | Penbutolol and carteolol: two new beta-adrenergic blockers with partial agonism. J Clin Pharmacol. 1990 May;30(5):412-21. | ||||
Ref 537811 | Antiarrhythmic, antifibrillatory, and hemodynamic actions of bethanidine sulfate: an orally effective analog of bretylium for suppression of ventricular tachyarrhythmias. Am J Cardiol. 1982 Oct;50(4):728-34. | ||||
Ref 538063 | Report of the Canadian Hypertension Society Consensus Conference: 3. Pharmacologic treatment of hypertensive disorders in pregnancy. CMAJ. 1997 Nov 1;157(9):1245-54. | ||||
Ref 538181 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 040455. | ||||
Ref 538246 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 072303. | ||||
Ref 538260 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 074086. | ||||
Ref 538266 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 074229. | ||||
Ref 538301 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 075720. | ||||
Ref 538499 | FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (NDA) 018166. | ||||
Ref 540554 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 3931). | ||||
Ref 540787 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 535). | ||||
Ref 540879 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 548). | ||||
Ref 540888 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 549). | ||||
Ref 540921 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 553). | ||||
Ref 540927 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 554). | ||||
Ref 540932 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 555). | ||||
Ref 540993 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 563). | ||||
Ref 540995 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 565). | ||||
Ref 541042 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 570). | ||||
Ref 542136 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7129). | ||||
Ref 542188 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7178). | ||||
Ref 542255 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7239). | ||||
Ref 542263 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7246). | ||||
Ref 542273 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7255). | ||||
Ref 542282 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7263). | ||||
Ref 542317 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7297). | ||||
Ref 542585 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7596). | ||||
Ref 542606 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 7618). | ||||
Ref 543300 | (http://www.guidetopharmacology.org/) Nucleic Acids Res. 2015 Oct 12. pii: gkv1037. The IUPHAR/BPS Guide to PHARMACOLOGY in 2016: towards curated quantitative interactions between 1300 protein targets and 6000 ligands. (Ligand id: 91). | ||||
Ref 544568 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000160) | ||||
Ref 546489 | Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008526) | ||||
Ref 526033 | J Med Chem. 2001 Apr 26;44(9):1456-66.(4-Piperidin-1-yl)phenyl amides: potent and selective human beta(3) agonists. | ||||
Ref 528842 | J 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. | ||||
Ref 530558 | Bioorg 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. | ||||
Ref 530748 | Bioorg 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. | ||||
Ref 530883 | Bioorg Med Chem Lett. 2010 Jun 1;20(11):3399-404. Epub 2010 Apr 9.A vHTS approach for the identification of beta-adrenoceptor ligands. | ||||
Ref 531079 | J 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. | ||||
Ref 532040 | Administration of the cyclic peptide COR-1 in humans (phase I study): ex vivo measurements of anti-beta1-adrenergic receptor antibody neutralization and of immune parameters. Eur J Heart Fail. 2012 Nov;14(11):1230-9. | ||||
Ref 532693 | Comparison of the beta-adrenoceptor affinity and selectivity of cetamolol, atenolol, betaxolol, and ICI-118,551. J Cardiovasc Pharmacol. 1988 Aug;12(2):208-17. | ||||
Ref 533374 | J 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. | ||||
Ref 533693 | Antianginal effects of YM-16151-4 in various experimental angina models. J Cardiovasc Pharmacol. 1993 May;21(5):701-8. | ||||
Ref 533801 | J 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. | ||||
Ref 534841 | Impact of exogenous beta-adrenergic receptor stimulation on hepatosplanchnic oxygen kinetics and metabolic activity in septic shock. Crit Care Med. 1999 Feb;27(2):325-31. | ||||
Ref 534890 | Inverse agonist activities of beta-adrenoceptor antagonists in rat myocardium. Br J Pharmacol. 1999 Jun;127(4):895-902. | ||||
Ref 535001 | Betaxolol, 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. | ||||
Ref 535096 | Partial agonistic effects of carteolol on atypical beta-adrenoceptors in the guinea pig gastric fundus. Jpn J Pharmacol. 2000 Nov;84(3):287-92. | ||||
Ref 535478 | beta-Adrenergic receptor blockers--a group of chiral drugs: different effects of each enantiomer. Ceska Slov Farm. 2002 May;51(3):121-8. | ||||
Ref 535660 | Knockouts model the 100 best-selling drugs--will they model the next 100? Nat Rev Drug Discov. 2003 Jan;2(1):38-51. | ||||
Ref 535807 | Prostaglandin 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. | ||||
Ref 535812 | Classification 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. | ||||
Ref 535815 | Uptake 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. | ||||
Ref 535957 | Binding affinities of ocular hypotensive beta-blockers levobetaxolol, levobunolol, and timolol at endogenous guinea pig beta-adrenoceptors. J Ocul Pharmacol Ther. 2004 Apr;20(2):93-9. | ||||
Ref 536072 | Blockade of beta-adrenergic receptors prevents amphetamine-induced behavioural sensitization in rats: a putative role of the bed nucleus of the stria terminalis. Int J Neuropsychopharmacol. 2005 Dec;8(4):569-81. Epub 2005 Apr 19. | ||||
Ref 536102 | Invited review: Neuroprotective properties of certain beta-adrenoceptor antagonists used for the treatment of glaucoma. J Ocul Pharmacol Ther. 2005 Jun;21(3):175-81. | ||||
Ref 536152 | Prediction and experimental validation of acute toxicity of beta-blockers in Ceriodaphnia dubia. Environ Toxicol Chem. 2005 Oct;24(10):2470-6. | ||||
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