Synthesis and pharmacological properties of a group of compounds obtained by coupling the H3-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 H3-antagonistic and H2-agonistic properties on electrically-simulated guinea-pig ileum segments and guinea-pig papillary muscle, respectively. All the synthesised compounds displayed good H3-antagonistic properties (pA2 range 7.02/8.49) while behaving only as weak partial H2-agonists. Derivative 28, the best NO-donor of the series, was able to trigger a dual NO-dependent muscle relaxation and H3-antagonistic effect on guinea-pig illeum
H3 Receptor Ligands: New Imidazole H3-antagonists Endowed with NO-Donor Properties
BERTINARIA, Massimo
2002-01-01
Abstract
Synthesis and pharmacological properties of a group of compounds obtained by coupling the H3-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 H3-antagonistic and H2-agonistic properties on electrically-simulated guinea-pig ileum segments and guinea-pig papillary muscle, respectively. All the synthesised compounds displayed good H3-antagonistic properties (pA2 range 7.02/8.49) while behaving only as weak partial H2-agonists. Derivative 28, the best NO-donor of the series, was able to trigger a dual NO-dependent muscle relaxation and H3-antagonistic effect on guinea-pig illeum
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