Disease relevance of ADRB1

• Superfusion with atenolol (beta 1-adrenoreceptor blocking drug) or butoxamine (beta 2-adrenoreceptor blocking drug) inhibited the pressor response and the tachycardia caused by hypothalamic stimulation [1].

Psychiatry related information on ADRB1

• Polygraphic sleep recordings of 16 h showed that prenalterol (20 and 40 mg/kg i.p.), a beta 1-adrenoceptor-stimulating drug increased paradoxical sleep (PS) in a dose-related manner during 4-12 h [2].

High impact information on ADRB1

• The beta 1-adrenoceptor selectivity of the S-form (about 30) was similar to that of the racemic metoprolol, while the R-form was almost non-selective (3 fold beta 1-selective) [3].
• Histamine bronchoconstriction of the central airways was unmasked by non-selective and beta 2-adrenoceptor blockade but not by beta 1-adrenoceptor blockade [4].
• Both dopexamine and dopamine are weak agonists at the guinea-pig atrial beta 1-adrenoceptor over the concentration range 10(-7) to 10(-4) M, but dopexamine has an intrinsic activity of only 0.16 relative to dopamine [5].
• On the basis of the present data, prenalterol may be characterized as a nonselective beta adrenoceptor ligand with beta-1 adrenoceptor partial agonistic activity [6].
• 4 It is suggested that the effects of D4975 on the myocardium involve both beta 1-adrenoceptor stimulation and inhibition of phosphodiesterase and that the marked and prolonged pressor response is due to resistance to enzymatic breakdown by monoamine oxidase [7].

Biological context of ADRB1

• Furthermore, the expected shift in ocular dominance following monocular deprivation was blocked by a direct cortical infusion of D,L-metoprolol, a selective beta 1-adrenergic receptor antagonist [8].
• The IC50 for CK-4001 at the beta 1-adrenoceptor was 38.1 +/- 8 microM and > 100 microM at the beta 2-adrenoceptor [9].

Anatomical context of ADRB1

• A similar pattern was found in the hippocampus indicating the presence of a beta 1-adrenergic receptor in these two regions [10].
• The comparison between the affinities of a series of beta-adrenergic agonists and antagonists for the beta-adrenergic receptors coupled with an adenylate cyclase in cerebral cortex and cerebellum with their affinities for well characterized beta 2-adrenergic receptors in lung and beta 1-adrenergic receptor in heart substantiated this conclusion [10].
• Qualitative effects of prenalterol and terbutaline on the spontaneous contractile activity in the cat colon strip indicated that the beta 1-adrenoceptor-mediated effects may be related to inhibition of the activity in cholinergic neurons, whereas the beta 2-adrenoceptors may be acting on the smooth muscle cells per se [11].
• Notably, monocular deprivation during the sensitive period of ocular dominance plasticity significantly increased beta1-adrenergic receptor immunoreactivity in the visual cortex ipsilateral to the deprived eye [12].
• These results indicate that the monocular deprivation during the sensitive period of ocular dominance plasticity modified beta1-adrenergic receptor immunoreactivity, including that in glial cells [12].

Associations of ADRB1 with chemical compounds

• At high doses atenolol, a beta 1-adrenoceptor antagonist, inhibited dobutamine's effect on 35S-labelled mucins [13].
• Thus, xamoterol is a partial agonist which displays beta 1-adrenoceptor selectivity [14].
• Extremely long-acting antihypertensive effects of KF-4317, a alpha- and beta 1-adrenoceptor blocker [15].
• Comparison of the Arrhythmogenic Actions of (-)-Isoprenaline, Dobutamine and the selective beta 1-adrenoceptor agonist, (+/-)-(1-[3',4'-dihydroxyphenoxy] -2-hydroxy-[3",4"-dimethoxy phenethylamino]-propane)-oxalate (Ro 363) [16].
• 4. Beta 1-Adrenoreceptor antagonist metoprolol was less potent than beta 2-antagonist H 35/25 in antagonizing the effect of salbutamol; metoprolol was more potent than H 25/35 in antagonizing noradrenaline [17].

Analytical, diagnostic and therapeutic context of ADRB1

• Under normal conditions, these arteries relax because of the predominance of the beta 1-adrenoceptors, whereas constriction prevails in the presence of beta 1-adrenoceptor antagonists [18].

References