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  • Title: Mixed antisecretory and gastroprotective activities of a new H2-antagonist containing a nitric oxide-donor furoxan moiety.
    Author: Sorba G, Gasco A, Coruzzi G, Adami M, Pozzoli C, Morini G, Bertaccini G.
    Journal: Arzneimittelforschung; 1997 Jul; 47(7):849-54. PubMed ID: 9272244.
    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, it was about 10 times more effective as a gastroprotective agent against ethanol- and 0.6 N HCl-induced gastric lesions. 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.
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