Abstract
Synthesis and pharmacological properties of a group of compounds obtained by coupling the H 3-antagonist SKF 91486 with the NO-donor 3-phenylfuroxan-4-yloxy and 3-benzenesulfonylfuroxan-4-yloxy moieties, as well as with the corresponding furazan analogues, devoid of NO-donating properties, are reported. All the products were tested for their H 3-antagonistic and H 2-agonistic properties on electrically-simulated guinea-pig ileum segments and guinea-pig papillary muscle, respectively. All the synthesised compounds displayed good H 3-antagonistic properties (pA 2 range 7.02–8.49) while behaving only as weak partial H 2-agonists. Derivative 28, the best NO-donor of the series, was able to trigger a dual NO-dependent muscle relaxation and H 3-antagonistic effect on guinea-pig illeum.
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