Shanghai Nianxing Industrial Co., Ltd
China
Product Name: Nuvenzepine
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Purity: 99.0%
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Dayang Chem (Hangzhou) Co., Ltd.
China
Product Name: Nuvenzepine
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Purity: 98.0%
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96487-37-5

96487-37-5 structure

96487-37-5 structure

Name: Nuvenzepine
Chemical Name: 11-(1-methylpiperidine-4-carbonyl)-6H-pyrido[3,2-c][1,5]benzodiazepin-5-one
CAS Number: 96487-37-5
Molecular Formula: C₁₉H₂₀N₄O₂
Molecular Weight: 336.38800
Catalog: Signaling Pathways GPCR/G Protein mAChR
Create Date: 2018-06-13 17:58:15
Modify Date: 2025-08-25 18:42:09
Nuvenzepine is an mAChR antagonist previously in phase I clinical trials for the treatment of gastrospasm.

Name	11-(1-methylpiperidine-4-carbonyl)-6H-pyrido[3,2-c][1,5]benzodiazepin-5-one
Synonyms	Nuvenzepinum UNII-8OMO7K4W74 Nuvenzepina [INN-Spanish] Nuvenzepina Nuvenzepine Nuvenzepinum [INN-Latin] Nuvenzepine [INN]

Description	Nuvenzepine is an mAChR antagonist previously in phase I clinical trials for the treatment of gastrospasm.
Related Catalog	Signaling Pathways >> GPCR/G Protein >> mAChR Signaling Pathways >> Neuronal Signaling >> mAChR Research Areas >> Cardiovascular Disease
Target	mAChR[1]
In Vitro	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[1].
In Vivo	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[2]. 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[3].
References	[1]. Barocelli E, et al. Functional comparison between nuvenzepine and pirenzepine on different guinea pig isolated smooth muscle preparations. Pharmacol Res. 1994 Aug-Sep;30(2):161-70. [2]. Barocelli E, et al. Gastrointestinal activities of a new pirenzepine-analog, nuvenzepine, in the cat. Farmaco. 1990 Oct;45(10):1089-99. [3]. Caselli G, et al. Determination of nuvenzepine in human plasma by a sensitive [3H]pirenzepine radioreceptor binding assay. J Pharm Sci. 1991 Feb;80(2):173-7.

Density	1.267g/cm3
Boiling Point	522.3ºC at 760mmHg
Molecular Formula	C₁₉H₂₀N₄O₂
Molecular Weight	336.38800
Flash Point	269.7ºC
Exact Mass	336.15900
PSA	70.99000
LogP	2.35990
Index of Refraction	1.616
Storage condition	2-8℃

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