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Zenidolol hydrochloride

CAS No. : 72795-01-8

產品活性：Zenidolol (ICI-118551) hydrochloride is a highly selective β2 adrenergic receptor antagonist, with K_is of 0.7, 49.5 and 611 nM for β2, β1 and β3 receptors, respectively.

研究領域：GPCR/G Protein  |  Neuronal Signaling

作用靶點：Adrenergic Receptor

In Vitro: Zenidolol (ICI-118551) hydrochloride inhibits cAMP accumulation with IC₅₀ of 1.7 μM in IMCD cells. Zenidolol (ICI-118551; 10 μM) hydrochloride induces a prominent vasorelaxation of norepinephrine (NE)-precontracted PA but not AO. 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).

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.

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