Nuvenzepine - CAS 96487-37-5
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
Molecular Weight:
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.
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
Store in a cool and dry place (or refer to the Certificate of Analysis).
Boiling Point:
522.3±50.0 ℃ at 760 Torr
1.267±0.06 g/cm3
Canonical SMILES:
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.
Molecular Weight Calculator Molarity Calculator Solution Dilution Calculator

Related mAChR Products

CAS 139886-04-7 Milameline hydrochloride

Milameline hydrochloride
(CAS: 139886-04-7)

Milameline is a non-selective muscarinic acetylcholine receptor partial agonist at all receptor subtypes (Ki values are 2.3, 2.4, 3.6, 3.8 and 4.3 μM for hM1, h...

Desfesoterodine fumarate
(CAS: 380636-50-0)

Desfesoterodine is the active metabolite of fesoterodine as its isobutyrate ester.

CAS 62-51-1 Methacholine chloride

Methacholine chloride
(CAS: 62-51-1)

Methacholine chloride, a synthetic choline ester, is pharmaceutical agent acting as a β2-adrenergic agonist used in the treatment of pulmonary and respiratory d...

CAS 148-72-1 pilocarpine nitrate

pilocarpine nitrate
(CAS: 148-72-1)

pilocarpine nitrate is a non-selective muscarinic receptor agonist that can be used to treat glaucoma.

CAS 242478-38-2 Solifenacin succinate

Solifenacin succinate
(CAS: 242478-38-2)

Solifenacin is a competitive cholinergic receptor antagonist.Solifenacin succinate is a urinary antispasmodic of the antimuscarinic class.

CAS 1135243-19-4 VU 0255035

VU 0255035
(CAS: 1135243-19-4)

VU 0255035 is a highly selective M1 muscarinic acetylcholine receptor antagonist (Ki = 14.87 nM) with 75-fold greater selectivity for the M1 orthosteric site ov...

CAS 300-08-3 Arecoline hydrobromide

Arecoline hydrobromide
(CAS: 300-08-3)

Arecoline is a muscarinic acetylcholine receptor agonist.

CAS 133099-04-4 Darifenacin

(CAS: 133099-04-4)

Darifenacin hydrobromide is an antispasmodic muscarinic antagonist, selective for blocking the M3 muscarinic acetylcholine receptor, which is primarily responsi...

CAS 385367-47-5 Tarafenacin

(CAS: 385367-47-5)

Tarafenacin is a highly selective M3 muscarinic receptor antagonist. It was the most potent in inhibiting carbachol-induced bladder contractions of the anti-ch...

CAS 133099-07-7 Darifenacin hydrobromide

Darifenacin hydrobromide
(CAS: 133099-07-7)

Darifenacin exerts non-parallel rightward displacement of the agonist curve and also significant depression of the maximum response (+)-cis-Dioxolane produced c...

CAS 131780-48-8 DAU 5884 hydrochloride

DAU 5884 hydrochloride
(CAS: 131780-48-8)

DAU 5884 hydrochloride is a selective muscarinic M3 receptor antagonist. It inhibits methacholine-dependent effects on cell proliferation and muscle contractili...

CAS 257603-40-0 J 104129 fumarate

J 104129 fumarate
(CAS: 257603-40-0)

The fumarate salt form of J 104129, which has been found to be a muscarinic M3 receptor antagonist with high selectivity.

CAS 127308-82-1 Zamifenacin

(CAS: 127308-82-1)

Zamifenacin is a Muscarinic M3 receptor antagonist originated by Pfizer. pKi value is 8.52 for M3 receptor, 7.93 for M2 receptor, 7.90 for M1 receptor and 7.78 ...

CAS 113-69-9 Benzquinamide Hydrochloride

Benzquinamide Hydrochloride
(CAS: 113-69-9)

Benzquinamide hydrochloride is an antiemetic compound with antihistaminic, anticholinergic and sedative properties. The mechanism of action is not quite sure an...

CAS 52-49-3 Benzhexol HCl

Benzhexol HCl
(CAS: 52-49-3)

Benzhexol HCl is an anticholinergic tertiary amine used to treat parkinsonism and the extrapyramidal side effects of anti-psychotic drugs.

CAS 10049-83-9 Pyrithioxin dihydrochloride

Pyrithioxin dihydrochloride
(CAS: 10049-83-9)

Pyrithioxin dihydrochloride, a pyridine thiol derivative, is a nootropic which could be used in the treatment of sequelae of brain trauma, encephalitis and meni...

CAS 101-31-5 Hyoscyamine

(CAS: 101-31-5)

Hyoscyamine is an AChR inhibitor with IC50 of 7.5 nM.

CAS 5633-14-7 Benzetimide hydrochloride

Benzetimide hydrochloride
(CAS: 5633-14-7)

Benzetimide hydrochloride is a muscarinic acetylcholine receptor antagonist that has anticholinergic properties and could block pilocarpine-induced lacrimation.

CAS 201939-40-4 PTAC oxalate

PTAC oxalate
(CAS: 201939-40-4)

PTAC oxalate is a muscarinic receptor ligand, which shows partial agonist activity at the M2 and M4 receptors, with minor antagonistic activity at m1, m3, m5 re...

CAS 98636-73-8 Nitrocaramiphen hydrochloride

Nitrocaramiphen hydrochloride
(CAS: 98636-73-8)

Nitrocaramiphen hydrochloride is a mAChR M1 selective muscarinic antagonist, which exhibits 71-fold selectivity for M1 over M2.

Chemical Structure

CAS 96487-37-5 Nuvenzepine

Quick Inquiry

Verification code

Featured Items