(N-[2-(2-CYCLOPROPYLMETHOXYPHENOXY)ETHYL]-5-CHLORO-ALPHA,ALPHA-DIMETHYL-1H-INDOLE-3-ETHANAMINE) HYDROCHLORIDE
- CAS号:169505-93-5
- 英文名:(N-[2-(2-CYCLOPROPYLMETHOXYPHENOXY)ETHYL]-5-CHLORO-ALPHA,ALPHA-DIMETHYL-1H-INDOLE-3-ETHANAMINE) HYDROCHLORIDE
- 中文名:(N-[2-(2-CYCLOPROPYLMETHOXYPHENOXY)ETHYL]-5-CHLORO-ALPHA,ALPHA-DIMETHYL-1H-INDOLE-3-ETHANAMINE) HYDROCHLORIDE
- CBNumber:CB5417674
- 分子式:C24H30Cl2N2O2
- 分子量:449.42
- MOL File:169505-93-5.mol
- 储存条件 :Store at RT
- 溶解度 :insoluble in ethanol; <22.47mg/ml in DMSO
- 形态 :solid
- 颜色 :White
(N-[2-(2-CYCLOPROPYLMETHOXYPHENOXY)ETHYL]-5-CHLORO-ALPHA,ALPHA-DIMETHYL-1H-INDOLE-3-ETHANAMINE) HYDROCHLORIDE性质、用途与生产工艺
- 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.
- 更新日期:2024/04/30
- 产品编号:HY-101336
- 产品名称:(N-[2-(2-CYCLOPROPYLMETHOXYPHENOXY)ETHYL]-5-CHLORO-ALPHA,ALPHA-DIMETHYL-1H-INDOLE-3-ETHANAMINE) HYDROCHLORIDE RS 17053 hydrochloride
- CAS编号:169505-93-5
- 包装:5mg
- 价格:850元
- 更新日期:2024/04/30
- 产品编号:HY-101336
- 产品名称:(N-[2-(2-CYCLOPROPYLMETHOXYPHENOXY)ETHYL]-5-CHLORO-ALPHA,ALPHA-DIMETHYL-1H-INDOLE-3-ETHANAMINE) HYDROCHLORIDE RS 17053 hydrochloride
- CAS编号:169505-93-5
- 包装:10mM * 1mLin DMSO
- 价格:935元
- 公司名称:TOCRIS-US
- 联系电话:--
- 电子邮件:customerservice@tocris.co.uk
- 国家:英国
- 产品数:5729
- 优势度:77
- 公司名称:MOLEKULA
- 联系电话:--
- 电子邮件:kevinbanks@molekula.com
- 国家:英国
- 产品数:6152
- 优势度:66