奴文西平
- CAS号:96487-37-5
- 英文名:Nuvenzepine
- 中文名:奴文西平
- CBNumber:CB41118339
- 分子式:C19H20N4O2
- 分子量:336.39
- MOL File:96487-37-5.mol
- 沸点 :522.3±50.0 °C(Predicted)
- 密度 :1.267±0.06 g/cm3(Predicted)
- 储存条件 :Store at -20°C
- 溶解度 :Soluble in DMSO
- 形态 :Solid
- 酸度系数(pKa) :10.99±0.20(Predicted)
- 颜色 :White to off-white
奴文西平性质、用途与生产工艺
- 生物活性 Nuvenzepine是 mAChR 的拮抗剂,有潜力用于胃痉挛的研究。
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靶点
mAChR
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体外研究
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.
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体内研究
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.
- 更新日期:2024/08/19
- 产品编号:HY-U00119
- 产品名称:奴文西平 Nuvenzepine
- CAS编号:96487-37-5
- 包装:1mg
- 价格:1800元
- 更新日期:2024/08/19
- 产品编号:HY-U00119
- 产品名称:奴文西平 Nuvenzepine
- CAS编号:96487-37-5
- 包装:5mg
- 价格:4000元
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