CAS 96487-37-5|Nuvenzepine
Introduction：Basic information about CAS 96487-37-5|Nuvenzepine, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
| 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 | / |
| MSDS | / | Flash Point | 269.7ºC |
Names
| Name | 11-(1-methylpiperidine-4-carbonyl)-6H-pyrido[3,2-c][1,5]benzodiazepin-5-one |
|---|---|
| Synonym | More Synonyms |
Nuvenzepine BiologicalActivity
| Description | Nuvenzepine is an mAChR antagonist previously in phase I clinical trials for the treatment of gastrospasm. |
|---|---|
| Related Catalog | Signaling Pathways >>GPCR/G Protein >>mAChRSignaling Pathways >>Neuronal Signaling >>mAChRResearch 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. |
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 |
| InChIKey | HPKYRXAEGNUARA-UHFFFAOYSA-N |
| SMILES | CN1CCC(C(=O)N2c3ccccc3NC(=O)c3cccnc32)CC1 |
| Storage condition | 2-8℃ |
Synonyms
| Nuvenzepinum |
| UNII-8OMO7K4W74 |
| Nuvenzepina [INN-Spanish] |
| Nuvenzepina |
| Nuvenzepine |
| Nuvenzepinum [INN-Latin] |
| Nuvenzepine [INN] |
