169505-93-5

中文名称 (N-[2-(2-CYCLOPROPYLMETHOXYPHENOXY)ETHYL]-5-CHLORO-ALPHA,ALPHA-DIMETHYL-1H-INDOLE-3-ETHANAMINE) HYDROCHLORIDE

英文名称 (N-[2-(2-CYCLOPROPYLMETHOXYPHENOXY)ETHYL]-5-CHLORO-ALPHA,ALPHA-DIMETHYL-1H-INDOLE-3-ETHANAMINE) HYDROCHLORIDE

CAS 169505-93-5

分子式 C24H30Cl2N2O2

分子量 449.41

MOL 文件 169505-93-5.mol

更新日期 2023/03/20 15:41:25

169505-93-5 结构式

基本信息物理化学性质图谱信息 (N-[2-(2-CYCLOPROPYLMETHOXYPHENOXY)ETHYL]-5-CHLORO-ALPHA,ALPHA-DIMETHYL-1H-INDOLE-3-ETHANAMINE) HYDROCHLORIDE价格(试剂级) 常见问题列表

基本信息

中文别名

化合物 T16798
化合物RS 17053 HYDROCHLORIDE

英文别名

RS-17053
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

生物活性

RS 17053 hydrochloride 是一种有效的 α1A 肾上腺素受体 (α1A adrenoceptor) 的选择性拮抗剂，其在细胞膜中测得的 pKi 值为 9.1，功能分析的 pA2 值为 9.8。

靶点

pKi: 9.1 (α1 _A adrenoceptor in native cell membrane)
pA2: 9.8 (α1 _A adrenoceptor).

体外研究

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).

体内研究

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.