Disease relevance of ICI118551

• However, at the dose tested ICI118551 was the more effective antagonist of the muscle growth response, and when given alone, ICI118551 caused significant muscle atrophy [1].
• During hypoxia, heart rate was further reduced by 31% in the presence of a beta(1)AR antagonist, CGP20712A, at 100 nM, but not with a beta2 (ICI118551)- or a beta3 (SR59230A)-specific antagonist at 100 nM [2].

High impact information on ICI118551

• The role of beta-arrestin was further confirmed by showing that transfection of beta-arrestin 2 in these knockout cells restored ICI118551 promoted ERK1/2 activation [3].
• Displacement with ICI118551 in the bladder base and urethra best fitted a 2-site model with 20% and 28% high affinity sites (beta2), respectively [4].
• (-)-Isoprenaline mediated relaxation of ileum was antagonized weakly by ICI118551 (100 nM) (beta(2)-AR antagonist) [5].
• A beta2 antagonist, ICI118551, impaired the PRL but not the VP or OT response to fear or novel environmental stimuli [6].
• Neither the phasic nature nor the EC50 of the norepinephrine-induced vasoconstrictions was altered in the presence of the beta2-adrenergic receptor antagonist 10(-5) M ICI118551 or the nitric oxide synthase inhibitor 10(-4) M NOARG [7].

Biological context of ICI118551

• For both rat strains, only half of the displaceable [125I]CYP binding sites displayed high affinity for CGP12177 (IC50 = 6.8 to 7.5 nM), and competition binding studies with CGP20712 and ICI118551 indicated that they represent beta 1- and beta 2-adrenoceptors [8].
• On calf adipocyte membranes, competition binding curves with CGP12177 displayed one high affinity binding site (IC50 = 4.7 nM), whereas the curves for CGP20712 (beta 1-selective antagonist) and ICI118551 (beta 2-selective antagonist) were biphasic [8].

Anatomical context of ICI118551

• In adipose tissue, an equal number of beta1- and beta2-AR was identified through the binding of clenbuterol and CGP20712A, whereas ICI118551 could not discriminate between these sites [9].

Associations of ICI118551 with other chemical compounds

• The beta-2-selective antagonist ICI118551 was a more potent inhibitor of acid production than both the beta-1 antagonist practolol and the H2-receptor antagonist cimetidine [10].

Gene context of ICI118551

• The affinity of ICI118551, a ligand selective for beta2-AR in other species, was uncharacteristically low in porcine LM (Kd = 441 nM), but was consistent with a value reported for the cloned porcine beta2-AR [9].

References