Disease relevance of ADRB1

• SSR149744C, which has no or low affinity for alpha 1 and beta 1 adrenergic and angiotensin II AT1 receptors, reduced isoproterenol-induced tachycardia and phenylephrine- or angiotensin II-induced hypertension in anaesthetized dogs [1].

High impact information on ADRB1

• Fat cell beta 1-adrenergic receptors display Mr = 67,000 under reducing conditions and Mr = 54,000 under nonreducing conditions, as previously reported (Moxham, C. P., and Malbon, C. C. (1985) Biochemistry 24, 6072-6077) [2].
• Peptide maps of beta 1-adrenergic receptors from the myocardial tissue of different species (pig versus rat) yield slightly different maps while the maps derived from the beta 2-adrenergic receptors of hamster lung and rat lung or erythrocytes reveal no interspecies differences [3].
• The affinity of the 2-fluoro analogue for beta 1-adrenergic receptors (inhibition of the specific binding of [3H]dihydroalprenolol, rat cerebral cortical membranes) was 2 times greater, while the 6-fluoro analogue was 1450 times less than the parent [4].
• The effects of tulobuterol in the saphenous vein (but not in the coronary artery) were antagonized by the selective beta-2 adrenergic blocker ICI 118,551 but were not affected by the selective beta-1 adrenergic inhibitor metoprolol [5].
• Effects of the new selectively beta 1-adrenergic cardiotonic drug denopamine (TA-064), (-)-(R)-1-(p-hydroxyphenyl)-2-[(3,4-dimethoxyphenethyl)amino]ethanol, on the adenylate cyclase-adenosine-3',5'-monophosphate (c-AMP) system of various tissues and cells in rats and guinea pigs were investigated in comparison with those of isoproterenol [6].

Biological context of ADRB1

• The CCAAT/enhancer binding proteins beta and alpha, adipocyte fatty acid binding protein, hormone-sensitive lipase, and the beta1-adrenergic receptor transcript concentrations tended (P < . 10) to be greater in adipose tissue from obese than in that from lean pigs [7].
• Infusion of purported beta 1- and beta 2-adrenergic antagonists suggested control of lipolysis in vivo predominantly by beta 1-adrenergic receptors; however, because the results in vitro do not indicate this specificity, differential pharmacodynamics of the antagonists are suggested rather than designation of receptor subtypes [8].

Anatomical context of ADRB1

• These compounds have been tested for beta 1-adrenergic receptors antagonism on guinea pig atria, beta 2-adrenergic receptor antagonism on guinea pig trachea and alpha-adrenergic blocking activity on rat aorta [9].
• These studies disclosed predominantly beta 1-adrenergic receptors on pig luteal membranes [10].
• Bovine anterior descending coronary artery possesses a homogeneous population of beta-1 adrenergic receptors [11].
• With that respect, 2 groups of proteins can be distinguished: (1) the group formed by the calcium-activated adenosine triphosphatase (Ca2(+)-ATPase) of the sarcoplasmic reticulum, the beta 1-adrenergic and muscarinic receptors and the low affinity isoform of the Na+K(+)-ATPase [12].
• Isoeugenolol: a selective beta1-adrenergic antagonist with tracheal and vascular smooth muscle relaxant properties [13].

Associations of ADRB1 with chemical compounds

• All the changes in Isc and Gt induced by higenamine were suppressed by the non-selective beta-adrenergic receptor antagonist propranolol and by the beta2-adrenergic receptor antagonist ICI-118,551, but not by the beta1-adrenergic-receptor-selective antagonist atenolol or by the alpha-antagonists phentolamine, prazosin and yohimbine [14].
• Beta 1-adrenergic selectivity of the new cardiotonic agent denopamine in its stimulating effects on adenylate cyclase [6].
• 1-[4-(2-Cyclopropylmethoxyethyl)phenoxy]-3-[1-p-(bromoacetamidophe nyl) -2-methyl-2-propylamine]-2-propranol (8), which is a derivative of the beta 1-adrenergic agent betaxolol, was synthesized [15].
• Metoprolol, a purported beta 1-adrenergic specific antagonist, was bound to the receptor with a Ki of approximately 300 nM when the radioligands were CGP or ICP but with a Ki of approximately 1,000 nM when the radioligand was DHA [16].
• The affinity constants (KA) of arbutamine and isoproterenol for cardiac beta1-adrenergic receptors, as determined by competition binding assays, were found to be 7.32 and 6.04, respectively [17].

Regulatory relationships of ADRB1

• These results suggest that PKC promotes coupling of cardiac beta1-adrenergic and H2 histamine receptors to Gi/o mediated inhibitory responses [18].

Other interactions of ADRB1

• The effect of protein kinase C (PKC) activation on beta1-adrenergic receptor (beta1-AR) regulation of the cardiac L-type Ca2+ current (ICa,L) was studied using the whole-cell patch clamp technique [18].

References