Nuvenzepine

Modify Date: 2024-01-02 18:36:49

Nuvenzepine Structure
Nuvenzepine structure
Common Name Nuvenzepine
CAS Number 96487-37-5 Molecular Weight 336.38800
Density 1.267g/cm3 Boiling Point 522.3ºC at 760mmHg
Molecular Formula C19H20N4O2 Melting Point N/A
MSDS N/A Flash Point 269.7ºC

 Use of Nuvenzepine


Nuvenzepine is an mAChR antagonist previously in phase I clinical trials for the treatment of gastrospasm.

 Names

Name 11-(1-methylpiperidine-4-carbonyl)-6H-pyrido[3,2-c][1,5]benzodiazepin-5-one
Synonym More Synonyms

 Nuvenzepine Biological Activity

Description Nuvenzepine is an mAChR antagonist previously in phase I clinical trials for the treatment of gastrospasm.
Related Catalog
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.

 Chemical & Physical Properties

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℃

 Synonyms

Nuvenzepinum
UNII-8OMO7K4W74
Nuvenzepina [INN-Spanish]
Nuvenzepina
Nuvenzepine
Nuvenzepinum [INN-Latin]
Nuvenzepine [INN]