Nipradilol Displays a Unique Pharmacological Profile of Affinities for the Different α<SUB>1</SUB>-Adrenoceptor Subtypes
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概要
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The selectivity of antagonistic effects of nipradilol, its four isomers and denitronipradilol, a major metabolite of nipradilol, on α<SIB>1</SUB>-adrenoceptor subtypes in rat heart, brain and spleen were examined by radioligand binding assay with [<SUP>3</SUP>H]-prazosin. Pharmacological characteristics of these compounds were determined in isolated aortae from rats and guinea pigs. The order of the pK<SIB>i</SUB> values for α<SUB>1High</SUB>-affinity sites in the heart, spleen and brain was SR 〉> nipradilol ≥ RR ≥ SS ≈ RS » denitronipradilol, but the order of the pKi values for the α<SUB>1LOW</SUB> -affinity sites was different in the heart and brain. There were good correlations between the pK<SUB>i</SUB> values of these compounds for the α<SUB>1High</SUB> -affinity sites and the pA<SUB>2</SUB> values for the contractile inhibition of the phenylephrine-induced response in rat aorta. There was no correlation between the pK<SUB>i</SUB> values of these compounds for the α<SUB>1LOW</SUB> -affinity sites and the pA<SUB>2</SUB> values. These results indicate that: 1) α<SUB>1High</SUB> -Affinity sites are related to vasoconstriction mediated by α<SUB>1</SUB>- adrenoceptors; 2)Nipradilol and its isomers possess low affinity to α<SUB>1</SUB> -adrenoceptors; and 3)The nitroxy group in nipradilol is important for its α1-blocking activity.
著者
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Kinami Junji
Department Of Pharmacology Niigata College Of Pharmacy
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Nagatomo Takafumi
Department Of Pharmacology Faculty Of Pharmaceutical Sciences Niigata University Of Pharmacy And App
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Tsuchihashi Hiroshi
Department Of Pharmacology Niigata College Of Pharmacy
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Sasaki Keiko
Department Of Earth Resources Engineering Faculty Of Engineering Kyushu University
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Maruyama Keiko
Department Of Clinical Laboratory Science Kanazawa University Graduate School Kanazawa University
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Kinami Junji
Department of Pharmacology, Niigata College of Pharmacy
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