Several analogues of idazoxan 1 and fenmetazole 2 were prepared as potential alpha-adrenoreceptor antagonists.Their blocking activity and selectivity on al- and a,-adrenoreceptors were evaluated in isolated rat vas deferens. Althoughall 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 / M., Pigini; Brasili, Livio; A., Cassinelli; D., Giardina; U., Gulini; W., Quaglia; C., Melchiorre. - In: EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY. - ISSN 0223-5234. - STAMPA. - 22:(1987), pp. 273-276.
Synthesis and alpha blocking activity of some analogues of idazoxan
BRASILI, Livio;
1987
Abstract
Several analogues of idazoxan 1 and fenmetazole 2 were prepared as potential alpha-adrenoreceptor antagonists.Their blocking activity and selectivity on al- and a,-adrenoreceptors were evaluated in isolated rat vas deferens. Althoughall 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.Pubblicazioni consigliate
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