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96487-37-5

中文名稱 奴文西平
英文名稱 Nuvenzepine
CAS 96487-37-5
分子式 C19H20N4O2
分子量 336.39
MOL 文件 96487-37-5.mol
96487-37-5 結構式 96487-37-5 結構式

基本信息

中文別名
奴文西平
英文別名
K-545
Nuvenzepine
11-(1-methylpiperidine-4-carbonyl)-6H-pyrido[3,2-c][1,5]benzodiazepin-5-one
6,11-Dihydro-11-[(1-methyl-4-piperidinyl)carbonyl]-5H-pyrido[2,3-b][1,5]benzodiazepin-5-one
5H-Pyrido[2,3-b][1,5]benzodiazepin-5-one, 6,11-dihydro-11-[(1-methyl-4-piperidinyl)carbonyl]-

物理化學性質

沸點522.3±50.0 °C(Predicted)
密度1.267±0.06 g/cm3(Predicted)
儲存條件-20°C儲存
溶解度溶于二甲基亞砜
酸度系數(shù)(pKa)10.99±0.20(Predicted)
形態(tài)Solid
顏色White to off-white
奴文西平價格(試劑級)
報價日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價格
2024/11/08HY-U00119奴文西平
Nuvenzepine
96487-37-51mg1800元
2024/11/08HY-U00119奴文西平
Nuvenzepine
96487-37-55mg4000元
2024/08/19HY-U00119奴文西平
Nuvenzepine
96487-37-510mg6800元

常見問題列表

生物活性
Nuvenzepine是 mAChR 的拮抗劑,有潛力用于胃痙攣的研究。
靶點

mAChR

體外研究

Nuvenzepine shows a four-fold higher affinity than pirenzepine in competitively antagonizing acetylcholine-induced contractions on isolated ileal musculature and on longitudinal ileum dispersed cells. Nuvenzepine is almost equipotent to pirenzepine in competitively preventing bethanechol-induced gall-bladder contractions and it displays a four-fold higher potency than pirenzepine in blocking vagal-stimulated tracheal constrictions.

體內研究

Intraduodenally administration of Nuvenzepine displays a long-lasting and dose-dependent inhibition of neostigmine-induced intestinal motility in anaesthetized cats. On ileal motor activity, Nuvenzepine shows a potency 10 times greater than that of pirenzepine. Nuvenzepine is also active, unlike pirenzepine, on colonic stimulated motility. Furthermore, in conscious cats, Nuvenzepine inhibits pentagastrin-stimulated gastric acid secretion resulting 25-30 times more potent than pirenzepine. Nuvenzepine has been found to be very active in inhibiting gastric acid secretion and intestinal hypermotility in rats, with very slight atropine-like side effects. The oral absorption rate is relatively slow, that the absolute bioavailability is 30 to 40%, that the elimination rate is slow and there is no accumulation in the body, and that there is very little metabolism.

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