New sulfamoylphenethylamines, potent alpha 1-adrenoceptor antagonists |
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| Authors: | T Takenaka K Honda T Fujikura K Niigata S Tachikawa N Inukai |
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| Affiliation: | 1. Departments of Pharmacology;2. Chemistry, Central Research Laboratories, Yamanouchi Pharmaceutical Co., Ltd., 1-1-8, Azusawa, Itabashi-ku, Tokyo 174, Japan |
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| Abstract: | The (+)-isomer of amosulalol, a combined alpha- and beta-adrenoceptor antagonist, was one log unit order more potent and less potent than the (-)-isomer in blocking alpha 1- and beta 1-adrenoceptors, respectively, in anaesthetized rats. Nine newly synthesized desoxy compounds derived from amosulalol and its analogues were found to possess potent alpha 1-adrenoceptor blocking activity and to be practically devoid of beta 1-adrenoceptor blocking activity. Among the desoxy derivatives, YM-12617 was more potent than prazosin in blocking alpha 1-adrenoceptors in anaesthetized rats and in reducing blood pressure, total peripheral resistance and left ventricular work in anaesthetized dogs. |
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