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CAS No.: 157066-76-7

SNAP 5089 is a selective antagonist of the subtype α_1A-adrenoceptor. It binds with high affinity to α_1A-adrenoceptor with a Ki value of 0.35 nM.

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描述The α-adrenergic receptors play a pivotal role in the regulation of numerous physiological events. SNAP 5089 is a selective antagonist of the subtype α_1A-adrenoceptor. It binds with high affinity to α_1A-adrenoceptor with a Ki value of 0.35 nM. The Ki values of SNAP 5089 for α_1B-, α_1D-, α_2A-, α_2B-, α_2C-adrenoceptor, and L-type Ca²⁺ channel were 220, 540, 1200, 800, 370 and 540 nM, respectively. SNAP 5089 at 1 μM inhibited norepinephrine-induced liberation of intracellular calcium by 95%, 30%, or 20% in cells transfected with α_1A-, α_1B-, or α_1D-adrenoceptor, respectively^[1]. SNAP 5089 at the concentrations of 10-300 nM produced parallel dextral shifts of E/[A] curves to A-61603 in isolated caudal artery of rat. SNAP 5089 inhibited A-61603-mediated contractions of rat caudal artery with an affinity estimate (pK_b) of 9.4^[2]. The affinity estimate (pK_b) value for SNAP 5089 in rabbit bladder neck was 7.0^[3].
作用机制SNAP 5089 is an α_1A-adrenoceptor antagonist that binds to α_1A-adrenoceptor with high affinity.
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