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
Strutture eterocicliche nella ricerca farmaceutica
Palermo
19-22 Maggio 2002
ATTI del X Meeting Strutture Eterocicliche Nella Ricerca Farmaceutica
Zangara editore
189
198
M. BERTINARIA
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/2318/17427
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