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194093-42-0

中文名称 7-氧代-N-[3(R)-奎宁环基]-4,7-二氢噻吩并[3,2-B]吡啶-6-甲酰胺盐酸盐
英文名称 N-[(8R)-1-azabicyclo[2.2.2]oct-8-yl]-2-oxo-9-thia-5-azabicyclo[4.3.0]n ona-3,7,10-triene-3-carboxamide hydrochloride
CAS 194093-42-0
分子式 C15H18ClN3O2S
分子量 339.84
MOL 文件 194093-42-0.mol
更新日期 2023/03/20 15:41:27
194093-42-0 结构式 194093-42-0 结构式

基本信息

中文别名
PUMOSETRAG 盐酸盐
7-氧代-N-[3(R)-奎宁环基]-4,7-二氢噻吩并[3,2-B]吡啶-6-甲酰胺盐酸盐
英文别名
DDP733
Pumosetrag
MKC-733 >=98% (HPLC)
Pumosetrag hydrochloride
PuMosetrag hydrochloride MKC-733
7-Oxo-N-[3(R)-quinuclidinyl]-4,7-dihydrothieno[3,2-b]pyridine-6-carboxamide hydrochloride
N-(3R)-1-Azabicyclo[2.2.2]oct-3-yl-4,7-dihydro-7-oxo-thieno[3,2-b]pyridine-6-carboxamide hydrochloride
N-[(8R)-1-azabicyclo[2.2.2]oct-8-yl]-2-oxo-9-thia-5-azabicyclo[4.3.0]n ona-3,7,10-triene-3-carboxamide hydrochloride

物理化学性质

储存条件2-8°C
溶解度H2O:可溶,25mg/mL,澄清
形态粉末
颜色白色至米色
旋光性 (optical activity)[α]/D -15 to -20°, c = 1 in H2O

安全数据

WGK Germany3

常见问题列表

生物活性
Pumosetrag Hydrochloride (MKC-733; DDP-733) 是一种口服可用的 5-HT3 部分激动剂,可用于肠易激综合征和胃食管反流病的研究。
靶点

5-HT 3 Receptor

体内研究

Pumosetrag displays both regional and species specificities. Pumosetrag has a lower efficacy than 5-HT in the rat jejunum, ileum and distal colon; however, it has similar efficacy and potency to 5-HT in the rat proximal colon. The activity profile of Pumosetrag is different in the guinea pig intestine where it exhibits greater potency and efficacy than 5-HT in all regions. Pumosetrag shows little to no response in the regions of the mouse intestine. Responses to Pumosetrag in the rat and guinea pig tissues are inhibited by ondansetron, confirming its action on 5-HT(3) receptors. Pumosetrag delays liquid gastric emptying in association with relaxation of the proximal stomach, stimulates fasting antroduodenal migrating motor complex activity and accelerates small intestinal transit.

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