Telenzepine (dihydrochloride)

Telenzepine dihydrochloride is a selective and orally active muscarinic M1 receptor antagonist with a K_i of 0.94 nM. Telenzepine dihydrochloride inhibits gastric acid secretion and has antiulcer effects^[1][2][3]. IC50 & 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].