Several analogues of idazoxan 1 and fenmetazole 2 were prepared as potential alpha2-adrenoreceptor antagonists. Their blocking activity and selectivity on alpha1- and alpha2-adrenoreceptors were evaluated in isolated rat vas deferens. Although all the drugs displayed a significantly lower activity compared to the parent compounds 1 and 2, with 3 being the only exception, the present results might help in elucidating the role of ring oxygens of 1 in drug—receptor interaction.
Synthesis and alpha-blocking activity of some analogues of idazoxan
PIGINI, Maria;QUAGLIA, Wilma;
1987-01-01
Abstract
Several analogues of idazoxan 1 and fenmetazole 2 were prepared as potential alpha2-adrenoreceptor antagonists. Their blocking activity and selectivity on alpha1- and alpha2-adrenoreceptors were evaluated in isolated rat vas deferens. Although all the drugs displayed a significantly lower activity compared to the parent compounds 1 and 2, with 3 being the only exception, the present results might help in elucidating the role of ring oxygens of 1 in drug—receptor interaction.File in questo prodotto:
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