DC Chemicals Limited
China
Product Name: Telenzepine dihydrochloride
Price: $Inquiry/250mg $Inquiry/100mg $Inquiry/1g
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

147416-96-4

147416-96-4 structure

Name: Telenzepine dihydrochloride
Chemical Name: Telenzepine dihydrochloride hydrate
CAS Number: 147416-96-4
Molecular Formula: C₁₉H₂₄Cl₂N₄O₂S
Molecular Weight: 443.39000
Catalog: Signaling Pathways GPCR/G Protein mAChR
Create Date: 2018-07-14 14:51:07
Modify Date: 2024-01-11 10:05:12
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].

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

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.

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

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