Nuvenzepine 

Nuvenzepine is an mAChR antagonist, has the potential for gastrospasm treatment.

mAChR^[1]

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

336.39

C₁₉H₂₀N₄O₂

96487-37-5

Solid

White to off-white

O=C1C2=CC=CN=C2N(C(C3CCN(C)CC3)=O)C4=CC=CC=C4N1

Room temperature in continental US; may vary elsewhere.

• [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.  [Content Brief]

  [2]. Barocelli E, et al. Gastrointestinal activities of a new pirenzepine-analog, nuvenzepine, in the cat. Farmaco. 1990 Oct;45(10):1089-99.  [Content Brief]

  [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.  [Content Brief]