565446-60-8Relevant academic research and scientific papers
H3 receptor ligands: New imidazole H3-antagonists endowed with NO-donor properties
Bertinaria, Massimo
, p. 279 - 283 (2007/10/03)
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.
[3-(1H-Imidazol-4-yl)propyl]guanidines containing furoxan moieties: A new class of H3-antagonists endowed with NO-donor properties
Bertinaria, Massimo,Di Stilo, Antonella,Tosco, Paolo,Sorba, Giovanni,Poli, Enzo,Pozzoli, Cristina,Coruzzi, Gabriella,Fruttero, Roberta,Gasco, Alberto
, p. 1197 - 1205 (2007/10/03)
Synthesis and pharmacological characterisation of a series of products obtained by coupling the H3-antagonist SKF 91486 through appropriate spacers with the NO-donor 3-phenylfuroxan-4-yloxy and 3-benzenesulfonylfuroxan-4-yloxy moieties, as well as with the corresponding furazan substructures, devoid of NO-donating properties, are reported. All the products were tested for their H3-antagonistic and H2-agonistic properties on electrically-stimulated guinea-pig ileum segments and guinea-pig papillary muscle, respectively. The whole series of compounds displayed good H3-antagonist behaviour and feeble partial H2-agonist activity. Among furoxan derivatives, the benzenesulfonyl hybrid 28, a good NO-donor, triggered a dual NO-dependent muscle relaxation and H3-antagonistic effect on guinea-pig intestine.
