Telenzepine dihydrochloride

Modify Date: 2024-01-11 10:05:12

Telenzepine dihydrochloride Structure
Telenzepine dihydrochloride structure
Common Name Telenzepine dihydrochloride
CAS Number 147416-96-4 Molecular Weight 443.39000
Density N/A Boiling Point 544.7ºC at 760mmHg
Molecular Formula C19H24Cl2N4O2S Melting Point N/A
MSDS Chinese USA Flash Point 283.2ºC

 Use of Telenzepine dihydrochloride


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].

 Names

Name Telenzepine dihydrochloride hydrate
Synonym More Synonyms

 Telenzepine dihydrochloride 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
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

 Synonyms

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