The effect of a new histamine H2-receptor antagonist derived from the lamtidine molecule and containing a nitric oxide (NO)-donor furoxan moiety (derivative 1) was studied for its gastric antisecretory activity and for a possible gastroprotective effect, in comparison with the analog without the furoxan moiety (derivative 2) The H2-receptor antagonistic activity was also investigated in the isolated guinea pig papillary muscle. Derivative 1 was approximately 10 times less potent than derivative 2 at the H2-receptor level; conversely, t was about 10 times more effective as a gastroprotective agent against ethanol- and 0.6 N HCl- induced gastric lessons The mechanism of the gastroprotection exerted by derivative 1 is probably connected with the release of NO, whose vasodilating action on gastric mucosa vessels is crucial. The combined antisecretory and gastroprotective activity of derivative 1 allows this compound to be considered as a prototype of a new class of antiulcer agents.
Mixed antisecretory and gastroprotective activities of a new H2- antagonist containing a nitric oxide-donor furoxan moiety / G., Sorba; A., Gasco; G., Coruzzi; Adami, Maristella; Pozzoli, Cristina; Morini, Giuseppina; G., Bertaccini. - In: ARZNEIMITTEL-FORSCHUNG. - ISSN 0004-4172. - 47:7(1997), pp. 849-854.
Mixed antisecretory and gastroprotective activities of a new H2- antagonist containing a nitric oxide-donor furoxan moiety
ADAMI, Maristella;POZZOLI, Cristina;MORINI, Giuseppina;
1997-01-01
Abstract
The effect of a new histamine H2-receptor antagonist derived from the lamtidine molecule and containing a nitric oxide (NO)-donor furoxan moiety (derivative 1) was studied for its gastric antisecretory activity and for a possible gastroprotective effect, in comparison with the analog without the furoxan moiety (derivative 2) The H2-receptor antagonistic activity was also investigated in the isolated guinea pig papillary muscle. Derivative 1 was approximately 10 times less potent than derivative 2 at the H2-receptor level; conversely, t was about 10 times more effective as a gastroprotective agent against ethanol- and 0.6 N HCl- induced gastric lessons The mechanism of the gastroprotection exerted by derivative 1 is probably connected with the release of NO, whose vasodilating action on gastric mucosa vessels is crucial. The combined antisecretory and gastroprotective activity of derivative 1 allows this compound to be considered as a prototype of a new class of antiulcer agents.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.