Target Information

Target General Infomation
Target ID
T44068
Former ID
TTDS00036
Target Name
Beta-1 adrenergic receptor
Gene Name
ADRB1
Synonyms
Beta-1 adrenoceptor; Beta-1 adrenoreceptor; ADRB1
Target Type
Successful
Disease Angina pectoris; Hypertension [ICD9:413, 401; ICD10: I20, I10-I16]
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]
Bronchodilator [ICD9: 493; ICD10: J45]
Coronary artery disease [ICD9: 410-414, 429.2; ICD10: I20-I25]
Cardiac arrhythmias [ICD9: 427; ICD10: I47-I49]
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]
Diabetes [ICD9: 253.5, 588.1; ICD10: E23.2, N25.1]
Glaucoma [ICD9: 365; ICD10: H40-H42]
Heart failure [ICD9: 428; ICD10: I50]
Hypertension; Angina pectoris [ICD9:401, 413; ICD10: I10-I16, I20]
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]
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.
BioChemical Class
GPCR rhodopsin
Target Validation
T44068
UniProt ID
P08588
Sequence
MGAGVLVLGASEPGNLSSAAPLPDGAATAARLLVPASPPASLLPPASESPEPLSQQWTAG
MGLLMALIVLLIVAGNVLVIVAIAKTPRLQTLTNLFIMSLASADLVMGLLVVPFGATIVV
WGRWEYGSFFCELWTSVDVLCVTASIETLCVIALDRYLAITSPFRYQSLLTRARARGLVC
TVWAISALVSFLPILMHWWRAESDEARRCYNDPKCCDFVTNRAYAIASSVVSFYVPLCIM
AFVYLRVFREAQKQVKKIDSCERRFLGGPARPPSPSPSPVPAPAPPPGPPRPAAAAATAP
LANGRAGKRRPSRLVALREQKALKTLGIIMGVFTLCWLPFFLANVVKAFHRELVPDRLFV
FFNWLGYANSAFNPIIYCRSPDFRKAFQRLLCCARRAARRRHATHGDRPRASGCLARPGP
PPSPGAASDDDDDDVVGATPPARLLEPWAGCNGGAAADSDSSLDEPCRPGFASESKV
Structure
2LSQ
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 524493ClinicalTrials.gov (NCT01970501) Genetically Targeted Therapy for the Prevention of Symptomatic Atrial Fibrillation in Patients With Heart Failure. U.S. National Institutes of Health.
Ref 525887Metoprolol: a review of its use in chronic heart failure. Drugs. 2000 Sep;60(3):647-78.
Ref 526432Effect 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 532040Administration 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 533372The 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 533693Antianginal effects of YM-16151-4 in various experimental angina models. J Cardiovasc Pharmacol. 1993 May;21(5):701-8.
Ref 533732Acute effects of the beta 3-adrenoceptor agonist, BRL 35135, on tissue glucose utilisation. Br J Pharmacol. 1995 Feb;114(4):888-94.
Ref 533792Controlled evaluation of the beta adrenoceptor blocking drug oxprenolol in anxiety. Med J Aust. 1976 Jun 12;1(24):909-12.
Ref 534258Biphasic 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 535807Prostaglandin 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 536095New antiarrhythmic agents for atrial fibrillation and atrial flutter. Expert Opin Emerg Drugs. 2005 May;10(2):311-22.
Ref 536116The 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 536361Natural 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 536650Emerging drugs for complications of end-stage liver disease. Expert Opin Emerg Drugs. 2008 Mar;13(1):159-74.
Ref 537619Brinzolamide/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 537669Penbutolol and carteolol: two new beta-adrenergic blockers with partial agonism. J Clin Pharmacol. 1990 May;30(5):412-21.
Ref 537811Antiarrhythmic, 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 538063Report of the Canadian Hypertension Society Consensus Conference: 3. Pharmacologic treatment of hypertensive disorders in pregnancy. CMAJ. 1997 Nov 1;157(9):1245-54.
Ref 538181FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 040455.
Ref 538246FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 072303.
Ref 538260FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 074086.
Ref 538266FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 074229.
Ref 538301FDA Approved Drug Products from FDA Official Website. 2009. Application Number: (ANDA) 075720.
Ref 538499FDA 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 544568Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800000160)
Ref 546489Trusted, scientifically sound profiles of drug programs, clinical trials, safety reports, and company deals, written by scientists. Springer. 2015. Adis Insight (drug id 800008526)
Ref 550707Drug information of Arbutamine, 2008. eduDrugs.
Ref 550781Drug information of Alprenolol, 2008. eduDrugs.
Ref 551871Drugs@FDA. U.S. Food and Drug Administration. U.S. Department of Health & Human Services. 2015
Ref 552007Drug information of Epinephrine, 2008. eduDrugs.
Ref 526033J Med Chem. 2001 Apr 26;44(9):1456-66.(4-Piperidin-1-yl)phenyl amides: potent and selective human beta(3) agonists.
Ref 528842J 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 530558Bioorg 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 530748Bioorg 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 530883Bioorg 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 531079J 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 532040Administration 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 532693Comparison 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 533374J 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 533488Medicinal plants in therapy. Bull World Health Organ. 1985;63(6):965-81.
Ref 533693Antianginal effects of YM-16151-4 in various experimental angina models. J Cardiovasc Pharmacol. 1993 May;21(5):701-8.
Ref 533801J 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 534841Impact 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 534890Inverse agonist activities of beta-adrenoceptor antagonists in rat myocardium. Br J Pharmacol. 1999 Jun;127(4):895-902.
Ref 535001Betaxolol, 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 535096Partial agonistic effects of carteolol on atypical beta-adrenoceptors in the guinea pig gastric fundus. Jpn J Pharmacol. 2000 Nov;84(3):287-92.
Ref 535324TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5.
Ref 535478beta-Adrenergic receptor blockers--a group of chiral drugs: different effects of each enantiomer. Ceska Slov Farm. 2002 May;51(3):121-8.
Ref 535660Knockouts model the 100 best-selling drugs--will they model the next 100? Nat Rev Drug Discov. 2003 Jan;2(1):38-51.
Ref 535807Prostaglandin 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 535812Classification 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 535815Uptake 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 535957Binding 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 536072Blockade 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 536102Invited 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 536152Prediction and experimental validation of acute toxicity of beta-blockers in Ceriodaphnia dubia. Environ Toxicol Chem. 2005 Oct;24(10):2470-6.
Ref 536320Topical dorzolamide 2%/timolol 0.5% ophthalmic solution: a review of its use in the treatment of glaucoma and ocular hypertension. Drugs Aging. 2006;23(12):977-95.
Ref 536398Are we misunderstanding beta-blockers. Int J Cardiol. 2007 Aug 9;120(1):10-27. Epub 2007 Apr 12.
Ref 536628Beta-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.
Ref 536769Antiarrhythmic effect of bisoprolol, a highly selective beta1-blocker, in patients with paroxysmal atrial fibrillation. Int Heart J. 2008 May;49(3):281-93.
Ref 536812Effects of prolonged treatment with beta-adrenoceptor antagonist, carteolol on systemic and regional hemodynamics in stroke-prone spontaneously hypertensive rats. J Pharmacobiodyn. 1991 Feb;14(2):94-100.
Ref 536850Beta-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.
Ref 537023Beta-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.
Ref 537126beta(2)-adrenoceptors are critical for antidepressant treatment of neuropathic pain. Ann Neurol. 2009 Feb;65(2):218-25.
Ref 537316beta-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.
Ref 537327Nitric oxide mechanisms of nebivolol. Ther Adv Cardiovasc Dis. 2009 Aug;3(4):317-27. Epub 2009 May 14.
Ref 537361Adrenergic activation of electrogenic K+ secretion in guinea pig distal colonic epithelium: involvement of beta1- and beta2-adrenergic receptors. Am J Physiol Gastrointest Liver Physiol. 2009 Aug;297(2):G269-77. Epub 2009 May 21.
Ref 537409Beta-blockers in the treatment of hypertension: are there clinically relevant differences? Postgrad Med. 2009 May;121(3):90-8.
Ref 537646Dissociation of autonomic controls of heart rate in weaning-aged borderline hypertensive rats by perinatal NaCl. J Auton Nerv Syst. 1990 Mar;29(3):219-26.
Ref 537649Decrease in penbutolol central response as a cause of changes in its serum protein binding. J Pharm Pharmacol. 1990 Mar;42(3):164-6.
Ref 537704Components of functional sympathetic control of heart rate in neonatal rats. Am J Physiol. 1985 May;248(5 Pt 2):R601-10.
Ref 537779Withdrawal syndromes and the cessation of antihypertensive therapy. Arch Intern Med. 1981 Aug;141(9):1125-7.
Ref 537782Binding of beta-adrenoceptor antagonists to rat and rabbit lung: special reference to levobunolol. Arzneimittelforschung. 1984;34(5):579-84.
Ref 537882Distribution of beta 1- and beta 2-adrenoceptor subtypes in various mouse tissues. Neurosci Lett. 1993 Sep 17;160(1):96-100.
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