RS 17053 hydrochloride 是一种有效和特异性的 α1A-Adrenergic Receptor 拮抗剂，在功能测定中 pA2 为 9.8，在天然细胞膜中 pKi 为 9.1。

RS 17053 hydrochloride is an effective and selective antagonist of α1A-adrenergic receptor with pA2 of 9.8 in functional assays and pKi of 9.1 in the native cell membrane.

RS 17053 hydrochloride antagonizes responses to NE only at high concentrations in isolated smooth muscle preparations from human LUT tissues. RS 17053 hydrochloride displays a high affinity for the α1A-adrenoceptor (pKi and pA2 estimates of 9.1-9.9) and a 30-100-fold selectivity over the α1 B and the α1 D-adrenoceptor subtypes (pKi and pA2 estimates of 7.7-7.8) in several tissues from rat and cloned adrenoceptors [1].

RS 17053 hydrochloride has a rapid onset of action and a duration of action exceeding 60 min. RS-17053 (10 mg/kg ) significantly suppresses food intake. RS 17053 hydrochloride pretreatment obviously alters food intake [F(4, 132) 5 6.28, p, 0.0001] [2].

169505-93-5

C24H30Cl2N2O2

449.41

RS-17053;RS 17053 hydrochloride

DMSO:125 mg/mL (278.14 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years