Nuvenzepine - CAS 96487-37-5
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C19H20N4O2
Molecular Weight:
336.39
COA:
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Targets:
mAChR
Description:
Nuvenzepine, a new pirenzepine-analog, is an mAChR antagonist, administered intraduodenally, displayed a long-lasting and dose-dependent inhibition of neostigmine-induced intestinal motility in anaesthetized cats.
Synonyms:
11-(1-methylpiperidine-4-carbonyl)-6H-pyrido[3,2-c][1,5]benzodiazepin-5-one; 11-(N-methylisonipecotyl)-6,11-dihydro-5H-pyrido(2,3-b)(1,5)benzodiazepin-5-one; DF 545; DF-545; nuvenzepine
Storage:
Store in a cool and dry place (or refer to the Certificate of Analysis).
MSDS:
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Boiling Point:
522.3±50.0 ℃ at 760 Torr
Density:
1.267±0.06 g/cm3
InChIKey:
HPKYRXAEGNUARA-UHFFFAOYSA-N
InChI:
1S/C19H20N4O2/c1-22-11-8-13(9-12-22)19(25)23-16-7-3-2-6-15(16)21-18(24)14-5-4-10-20-17(14)23/h2-7,10,13H,8-9,11-12H2,1H3,(H,21,24)
Canonical SMILES:
CN1CCC(CC1)C(=O)N2C3=CC=CC=C3NC(=O)C4=C2N=CC=C4
1.Regional differences in motor responsiveness to antimuscarinic drugs in rabbit isolated small and large intestine.
Barocelli E;Ballabeni V;Chiavarini M;Caretta A;Molina E;Impicciatore M Pharmacol Res. 1995 Jan;31(1):43-8.
The pirenzepine-related analogue, nuvenzepine, and the antagonists selective for the three muscarinic receptor subtypes 4-DAMP (M1 and M3 receptors), pirenzepine (M1 receptors), methoctramine (M2 receptors) have been tested on rabbit isolated small and large intestinal regions provided with spontaneous motor activity. The employed drugs differently affected intestinal motility patterns. The ileum pendular movements as well as the proximal colon and taenia coli tone, spike amplitude and frequency were concentration-dependently inhibited by the compounds here employed. Their pIC50 values followed the rank order of potency generally reported for the involvement of the M3 muscarinic receptors (4-DAMP > or = atropine > nuvenzepine > or = pirenzepine > methoctramine). Unlike nuvenzepine and the other antimuscarinics assayed, the M1 selective antagonist pirenzepine, at nanomolar concentrations, was able to enhance the proximal taenia coli motility patterns suggesting that a M1-inhibitory pathway might operate in the physiological modulation of taenia coli motility. At variance with longitudinal ileum and colon contractile activity, proximal circular colon motility was resistant to muscarinic as well as to alpha 1-, H1-, 5-HT-blockade indicating that NANC neuronal mechanisms could act at this level.
2.Functional comparison between nuvenzepine and pirenzepine on different guinea pig isolated smooth muscle preparations.
Barocelli E;Ballabeni V;Chiavarini M;Molina E;Impicciatore M Pharmacol Res. 1994 Aug-Sep;30(2):161-70.
The antimuscarinic agents nuvenzepine and pirenzepine were tested on four guinea pig isolated smooth muscle preparations in order to better investigate the existence of differences in the functional activities of such antagonists, as suggested by previous reports. The effects of both compounds were compared to those of atropine. Nuvenzepine showed a four-fold higher affinity than pirenzepine in competitively antagonizing acetylcholine-induced contractions on isolated ileal musculature (pA2 = 7.08 +/- 0.15) and on longitudinal ileum dispersed cells (pA2 = 7.11 +/- 0.19). By contrast, unlike pirenzepine which was ineffective, nuvenzepine inhibited histamine-induced ileal motor activity in a dualistic manner, behaving as an irreversible competitive H1 antagonist (pA2 = 5.02 +/- 0.11). Nuvenzepine was almost equipotent to pirenzepine in competitively preventing bethanechol-induced gall-bladder contractions (pA2 = 7.23 +/- 0.16) and it displayed a four-fold higher potency than pirenzepine in blocking vagal-stimulated tracheal constrictions (pIC50 = 6.77 +/- 0.06). Both compounds were definitely less potent than atropine. On the whole, these findings indicate that, on the selected preparations, nuvenzepine substantially shares the antimuscarinic properties of pirenzepine but it is also endowed with a (weak) H1-blocking action.
3.Quinolizidinyl derivatives of 5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one as ligands for muscarinic receptors.
Novelli F;Sparatore A;Tasso B;Sparatore F Bioorg Med Chem Lett. 1999 Oct 18;9(20):3031-4.
Quinolizidinyl derivatives of the tricyclic systems characterizing pirenzepine and nuvenzepine, were prepared and tested as ligands for muscarinic M1, M2 and M3 receptors; 5,11-dihydro-11-[(S-lupinyl)-thioacetyl]-6H-pyrido[2,3-b][1, 4]benzodiazepin-6-one exhibited IC50 = 10 nM for M1 and 760 nM for both M2 and M3 subtypes. During the synthesis some interesting side compounds were isolated and characterized.
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CAS 96487-37-5 Nuvenzepine

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