Gastric antisecretory activity of telenzepine, a new M1-selective muscarinic antagonist: comparison with pirenzepine.
The new M1-receptor antagonist telenzepine has been studied for its antisecretory effect in different in vitro and in vivo experimental models in comparison with pirenzepine. Telenzepine was found to be from 3 to 10 times more potent than pirenzepine in inhibiting bethanechol-, pentagastrin- and dimaprit-induced acid secretion in the conscious gastric fistula cat. Also, in the lumen-perfused stomach of the anaesthetized rat, telenzepine was more active than pirenzepine as an inhibitor of bethanechol-induced acid secretion; the inhibitory effect of telenzepine lasted more than 3 hr, while that of pirenzepine disappeared within 1 hr. In the isolated gastric fundus from immature rats, telenzepine and pirenzepine did not modify the spontaneous acid secretion, whereas both drugs caused a competitive inhibition of bethanechol-induced acid secretion (pA2 values were 7.96 and 6.81 for telenzepine and pirenzepine, respectively). These data indicate that telenzepine is a potent antisecretory agent both in vitro and in vivo.
Coruzzi
G
G
Institute of Pharmacology, University of Parma, Italy.
Adami
M
M
Bertaccini
G
G
D000758:Anesthesia; D000818:Animals; D002415:Cats; D004305:Dose-Response Relationship, Drug; D005260:Female; D005744:Gastric Acid / Q000378:metabolism*; D066298:In Vitro Techniques; D010276:Parasympatholytics / Q000494:pharmacology*; D010477:Perfusion; D010890:Pirenzepine / Q000031:analogs & derivatives* / Q000494:pharmacology*; D051381:Rats; D011919:Rats, Inbred Strains
D010276:Parasympatholytics; C046338:telenzepine; D010890:Pirenzepine