Zenidolol hydrochloride

CAS: 72795-01-8 F: C17H28ClNO2 W: 313.86

Zenidolol (ICI-118551) hydrochloride is a highly selective β2 adrenergic receptor antagonist, with Kis of 0.7, 49.5 and

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Bioactivity	Zenidolol (ICI-118551) hydrochloride is a highly selective β2 adrenergic receptor antagonist, with Kis of 0.7, 49.5 and 611 nM for β2, β1 and β3 receptors, respectively.
Invitro	Zenidolol (ICI-118551) hydrochloride inhibits cAMP accumulation with IC50 of 1.7 μM in IMCD cells[1]. Zenidolol (ICI-118551; 10 μM) hydrochloride induces a prominent vasorelaxation of norepinephrine (NE)-precontracted PA but not AO[2]. In failing human heart, Zenidolol (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 Zenidolol (ICI-118551) Is Not cAMP-Related. Overexpression of β2AR in rabbit myocytes enhances negative inotropic effects of Zenidolol (ICI-118551)[3].
In Vivo	Zenidolol (ICI-118551; 0.2 mg/kg) hydrochloride injected into the jugular vein of the mice, reduces systolic pressure in the pulmonary circuit but not systemic arterial pressure[2].
Name	Zenidolol hydrochloride
CAS	72795-01-8
Formula	C17H28ClNO2
Molar Mass	313.86
Appearance	Solid
Transport	Room temperature in continental US; may vary elsewhere.
Storage	4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Reference	[1]. Yasuda G, et al. The beta 1- and beta 2-adrenoceptor subtypes in cultured rat inner medullary collecting duct cells. Am J Physiol. 1996 Sep;271(3 Pt 2):F762-9. [2]. Wenzel D, et al. beta(2)-adrenoceptor antagonist ICI 118,551 decreases pulmonary vascular tone in mice via a G(i/o) protein/nitric oxide-coupled pathway. Hypertension. 2009 Jul;54(1):157-63. [3]. Gong H, et al. Specific beta(2)AR blocker ICI 118,551 actively decreases contraction through a G(i)-coupled form of the beta(2)AR in myocytes from failing human heart. Circulation. 2002 May 28;105(21):2497-503. [4]. Hoffmann C, et al. Comparative pharmacology of human beta-adrenergic receptor subtypes--characterization of stably transfected receptors in CHO cells. Naunyn Schmiedebergs Arch Pharmacol. 2004 Feb;369(2):151-9.