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RS 17053 hydrochloride

CAS No. : 169505-93-5

MCE 站：RS 17053 hydrochloride

产品活性：RS 17053 hydrochloride 是一种有效的 α1_A 肾上腺素受体 (α1_A adrenoceptor) 的选择性拮抗剂，其在细胞膜中测得的 pK_i 值为 9.1，功能分析的 pA₂ 值为 9.8。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：Adrenergic Receptor

In Vitro: In several tissues from rat and cloned adrenoceptors, RS 17053 hydrochloride displays high affinity for the α1A-adrenoceptor (pK_i and pA₂ estimates of 9.1-9.9) and a 30-100-fold selectivity over the α1 B and the α1 D-adrenoceptor subtypes (pK_i and pA₂ estimates of 7.7-7.8). However, in isolated smooth muscle preparations from human LUT tissues, RS 17053 hydrochloride antagonizes responses to NE only at high concentrations. Estimates of affinity (pA₂) at α1-adrenoceptors mediating NE-induced contractions are 7.5 in prostatic periurethral longitudinal smooth muscle (compared with 8.6 for prazosin), 6.9 in anterior fibromuscular stroma (prazosin, 8.9), and 7.1 in bladder neck (prazosin, 8.5).

In Vivo: RS 17053 hydrochloride has a rapid onset of action, and a duration of action exceeding 60 min. RS 17053 hydrochloride pretreatment significantly alteres food intake [F(4, 132) 5 6.28, p , 0.0001]. 10 mg/kg RS-17053 significantly suppresses food intake.

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