169505-93-5
基本信息
化合物RS 17053 HYDROCHLORIDE
RS17053HCl
RS 17053 HYDROCHLORIDE
RS 17053 hydrochloride (RS-17053)
RS 17053 hydrochloride (Synonyms: RS-17053)
(N-[2-(2-Cyclopropylmethoxyphenoxy)ethyl]-5-chloro-α,α-dimethyl-1H-indole-3-ethanamine)hydrochloride
(N-(2-(2-Cyclopropylmethoxyphenoxy)ethyl)-5-chloro-(a,a)-dimethyl-(1H)-indole-3-ethanamine)hydrochloride
(N-[2-(2-CYCLOPROPYLMETHOXYPHENOXY)ETHYL]-5-CHLORO-ALPHA,ALPHA-DIMETHYL-1H-INDOLE-3-ETHANAMINE) HYDROCHLORIDE
物理化学性质
| 储存条件 | Store at RT |
| 溶解度 | insoluble in ethanol; <22.47mg/ml in DMSO |
| 形态 | 固体 |
| 颜色 | 白色 |
图谱信息
(N-[2-(2-CYCLOPROPYLMETHOXYPHENOXY)ETHYL]-5-CHLORO-ALPHA,ALPHA-DIMETHYL-1H-INDOLE-3-ETHANAMINE) HYDROCHLORIDE(169505-93-5)核磁图(1HNMR)常见问题列表
pKi: 9.1 (α1
A
adrenoceptor in native cell membrane)
pA2: 9.8 (α1
A
adrenoceptor).
In several tissues from rat and cloned adrenoceptors, RS 17053 hydrochloride displays high affinity for the α1A-adrenoceptor (pK i and pA 2 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 pA 2 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 (pA 2 ) 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).
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.