ICI 118,551 (hydrochloride)

72795-01-8

C17H28ClNO2

H2O : 12.5 mg/mL (39.83 mM; Need ultrasonic); DMSO : 25 mg/mL (79.65 mM; Need ultrasonic)

GPCR/G Protein; Neuronal Signaling

ICI 118, 551 (hydrochloride) is a highly selective beta2 adrenergic receptor antagonist, with K_is of 0.7, 49.5 and 611 nM for beta2, beta1 and beta3 receptors, respectively. IC50 & Target: Ki: 0.7nM (beta2 receptor), 49.5 nM (beta1 receptor), 611 nM (beta3 receptor)^[4] In Vitro: ICI 118551 inhibits cAMP accumulation with IC₅₀ of 1.7 uM in IMCD cells^[1]. ICI 118551 (10 uM) induces a prominent vasorelaxation of norepinephrine (NE)-precontracted PA but not AO^[2]. In failing human heart, ICI 118551 has significant effects on beat duration, with time-to-peak contraction and time-to-90% relaxation reduced compared with basal contraction. Negative Inotropic Effect of ICI 118551 Is Not cAMP-Related. Overexpression of beta2AR in rabbit myocytes enhances negative inotropic effects of ICI 118551^[3]. In Vivo: ICI 118551 (0.2 mg/kg) injected into the jugular vein of the mice, reduces systolic pressure in the pulmonary circuit but not systemic arterial pressure^[2].