ICI 118,551 hydrochloride 是高度选择性的β2 Adrenergic Receptor拮抗剂，能够结合 β2 肾上腺素能受体 (Ki=0.7 nM)、β1 肾上腺素能受体 (Ki=49.5 nM) 和 β3 肾上腺素能受体 (Ki=611 nM)。

ICI 118,551 is a highly selective β2 adrenergic receptor antagonist (Kis: 0.7, 49.5, and 611 nM for β2, β1, and β3 receptors).

ICI 118551 (10 μM) induces a prominent vasorelaxation of norepinephrine (NE)-precontracted PA but not AO [2]. ICI 118551 inhibits cAMP accumulation in IMCD cells (IC50: 1.7 μM) [1]. In the 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 β2AR in rabbit myocytes enhances the negative inotropic effects of ICI 118551 [3].

ICI 118551 (0.2 mg/kg) injected into the jugular vein of the mice, strongly reduces systolic pressure in the pulmonary circuit but not systemic arterial pressure in vivo[2].

72795-01-8

C17H28ClNO2

313.86

ICI 118551 hydrochloride;ICI 118,551 hydrochloride

DMSO:20 mg/mL (63.72 mM),Need ultrasonic
H2O:11 mg/mL (35.05 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years