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作 者:MUSTAFA Mohd Rais ACHIKE Francis Ifejika
出 处:《Acta Pharmacologica Sinica》2000年第12期110-113,共4页中国药理学报(英文版)
摘 要:AIM: Dicentrine is a known α1-adrenoceptor antagonist, but its 1α-adrenoceptor subtype selectivity has not yet been determined. We therefore, investigated the putative α1-adrenoceptor subtype selectivity of this agent. METHODS : Graded isometric contractile responses of rat aortic rings and spleen to phenylephrine were observed in the absence or presence of various concentrations of dicentrine. The pA2 values for dicentrine were determined. RESULTS: Aortic tissues were more sensitive to phenylephrine-induced contraction than the spleen tissues. Dicentrine was approximately 100 times more potent as an antagonist to the aortic contraction, than it was to the splenic contractions. CONCLUSION: Dicentrine is an α1-adrenoceptor antagonist which is more selective towards the putative α1D-adrenoceptor subtype of the rat aorta than the α1B-adrenoceptor of the spleen.AIM: Dicentrine is a known α1-adrenoceptor antagonist, but its 1α-adrenoceptor subtype selectivity has not yet been determined. We therefore, investigated the putative α1-adrenoceptor subtype selectivity of this agent. METHODS : Graded isometric contractile responses of rat aortic rings and spleen to phenylephrine were observed in the absence or presence of various concentrations of dicentrine. The pA2 values for dicentrine were determined. RESULTS: Aortic tissues were more sensitive to phenylephrine-induced contraction than the spleen tissues. Dicentrine was approximately 100 times more potent as an antagonist to the aortic contraction, than it was to the splenic contractions. CONCLUSION: Dicentrine is an α1-adrenoceptor antagonist which is more selective towards the putative α1D-adrenoceptor subtype of the rat aorta than the α1B-adrenoceptor of the spleen.
关 键 词:LINDERA megaphylla dicentrine apor-phines ADRENERGIC alpha-antagonists AORTA spleen
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