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Telenzepine dihydrochloride

Names

[ CAS No. ]:
147416-96-4

[ Name ]:
Telenzepine dihydrochloride

[Synonym ]:
1-methyl-10-[2-(4-methylpiperazin-1-yl)acetyl]-5H-thieno[3,4-b][1,5]benzodiazepin-4-one,dihydrochloride
MFCD00083208

Biological Activity

[Description]:

Telenzepine dihydrochloride is a selective and orally active muscarinic M1 receptor antagonist with a Ki of 0.94 nM. Telenzepine dihydrochloride inhibits gastric acid secretion and has antiulcer effects[1][2][3].

[Related Catalog]:

Signaling Pathways >> Neuronal Signaling >> mAChR
Signaling Pathways >> GPCR/G Protein >> mAChR
Research Areas >> Neurological Disease

[Target]

Ki: 0.94 nM (Muscarinic M1 receptor), 17.8 nM (Muscarinic M2 receptor)[3]


[In Vitro]

At submicromolar concentrations (100 nM), Telenzepine abolishes responses to either muscarine or the muscarinic component of the acetylcholine response. The excitatory effect of muscarine at postsynaptic M1 receptors is dose dependently inhibited by Telenzepine (0.1-1000 nM) at concentrations[2]. The threshold dose of Telenzepine as an antagonist of the muscarinic depolarization in AH/type 2 neurons is in the range of 0.1-1 nM. The IC50 of Telenzepine needed to abolish the response is 8.5 nM[2].

[In Vivo]

Intravenous Telenzepine potently inhibits gastric acid secretion in the Ghosh-Schild rat (carbachol-stimulated), the chronic fistula rat (basal secretion), or, both intravenously and orally, in the modified Shay rat[1]. Telenzepine (2.7 μmol/kg; orally) treatment shows significantly longer duration antiulcer effects in the modified Shay rat[1].

[References]

[1]. R Riedel, et al. Comparison of the gastric antisecretory and antiulcer potencies of telenzepine, pirenzepine, ranitidine and cimetidine in the rat. Digestion. 1988;40(1):25-32.

[2]. F L Christofi, et al. Neuropharmacology of the muscarinic antagonist telenzepine in myenteric ganglia of the guinea-pig small intestine. Eur J Pharmacol. 1991 Apr 3;195(3):333-9.

[3]. M Galvan, et al. Interaction of telenzepine with muscarinic receptors in mammalian sympathetic ganglia. Eur J Pharmacol. 1989 Aug 11;167(1):1-10.

Chemical & Physical Properties

[ Boiling Point ]:
544.7ºC at 760mmHg

[ Molecular Formula ]:
C19H24Cl2N4O2S

[ Molecular Weight ]:
443.39000

[ Flash Point ]:
283.2ºC

[ Exact Mass ]:
442.10000

[ PSA ]:
89.58000

[ LogP ]:
3.78230

[ Vapour Pressure ]:
6.34E-12mmHg at 25°C

MSDS

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Related Compounds