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Description: ICI-118551 HCl, the hydrochloride salt of ICI-118551, is a novel, potent and highly selective beta2 adrenergic receptor antagonist, with Kis of 0.7, 49.5 and 611 nM for beta2, beta1 and beta3 receptors, respectively. beta(2)-adrenoceptors are important modulators of vascular tone, particularly in the pulmonary circulation. ICI 118551 binding directs the beta(2)AR to a G(i)-coupled form and away from the G(s)-coupled form (ligand-directed trafficking). ICI 118, 551 effectively acts as an agonist at the G(i)-coupled beta(2)AR, producing a direct negative inotropic effect. Conditions where beta(2)ARs are present and G(i) is raised (failing human heart, TGbeta(2) mouse heart) predispose to the appearance of the negative inotropic effect.
References: Circulation. 2002 May 28; 105(21):2497-503; Hypertension. 2009 Jul; 54(1):157-63.
Related CAS #: 72795-01-8 (HCl) 72795-26-7 (free base) 91021-57-7 (racemic)
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