telenzepine

Telenzepine is a thienobenzodiazepine derivative that acts as a highly selective muscarinic M1 receptor antagonist. It was developed as an antiulcer agent for the treatment of peptic ulcers and functions by inhibiting gastric acid secretion through blockade of M1 receptors in the stomach. Telenzepine is structurally related to pirenzepine but exhibits significantly higher potency and selectivity for M1 receptors, being at least 25 times more potent than pirenzepine in inhibiting gastric acid secretion and up to 50 times more potent in reducing salivary secretion. The drug is atropisomeric, with the (+)-enantiomer displaying much greater activity than the (–)-enantiomer. Clinical development reached preregistration/phase III for peptic ulcer disease but was discontinued before approval; it was also investigated for nocturnal asthma without success[1][2][4][5][6].

Other names

telenzepinetelenzepine dihydrochloride1-methyl-10-[2-(4-methylpiperazin-1-yl)acetyl]-5H-thieno[3,4-b][1,5]benzodiazepin-4-one