Naftopidil, Novel α_1-Adrenoceptor Antagonist, Displays Selective Inhibition of Canine Prostatic Pressure and High Affinity Binding to Cloned Human α_1-Adrenoceptors
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概要
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The pharmacological profiles of the α1-adrenoceptor antagonists naftopidil, tamsulosin and prazosin were studied in an anesthetized dog model that allowed the simultaneous assessment of their antagonist potency against phenylephrine-mediated increases in prostatic pressure and mean blood pressure. The intravenous administration of each of these compounds dose-dependently inhibited phenylephrineinduced increases in prostatic pressure and mean blood pressure. To further assess the ability of the three compounds to inhibit phenylephrine-induced responses, the doses required to produce a 50% inhibition of the phenylephrine-induced increases in prostatic and mean blood pressure and the selectivity index obtained from the ratio of those two doses were determined for each test compound. Forty minutes after the intravenous administration of naftopidil, the selectivity index was 3.76, and those of tamsulosin and prazosin were 1.23 and 0.61, respectively. These findings demonstrated that naftopidil selectively inhibited the phenylephrine-induced increase in prostatic pressure compared with mean blood pressure in the anesthetized dog model. The selectivity of naftopidil for prostatic pressure was the most potent among the test compounds. In addition, using cloned human α1-adrenoceptor subtypes, naftopidil was selective for the α1d-adrenoceptor with approximately 3- and 17-fold higher affinity than for the α1a- and α1b-adrenoceptor subtypes, respectively. The selectivity of naftopidil for prostatic pressure may be attributable to its high binding affinity for α1a- and α1d-adrenoceptor subtypes.
- 社団法人 日本薬理学会の論文
- 1999-04-01
著者
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TSUJIMOTO Gozoh
Department of Genomic Drug Discovery Science, Kyoto University Graduate School of Pharmaceutical Sci
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Tsujimoto Gozoh
Department Of Genomic Drug Discovery Science Graduate School Of Pharmaceutical Sciences Kyoto Univer
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Tsujimoto Gozoh
Dep. Of Genomic Drug Discovery Sci. Graduate School Of Pharmaceutical Sciences Kyoto Univ. Jpn
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Tsujimoto Gozoh
Department Of Molecular Cell Pharmacology National Research Institute For Child Health And Developme
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Tsujimoto Gozoh
Department Of Molecular And Cellular Pharmacology National Children's Medical Research Center
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Tsujimoto Gozoh
Department Of Molecular Cell Pharmacology National Children 's Medical Research Center
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Takei Ryo-ich
Laboratory For Pharmacology Institute For Life Science Research Asahi Chemical Industry
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Awaji Takeo
Department Of Pharmacology Yamanashi Medical College
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SHIBATA Katsushi
Department of Molecular, Cell Pharmacology, National Children 's Medical Research Center
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Asano Toshio
Laboratory For Pharmacology Asahi Chemical Industry
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Ikegaki Ichiro
Institute Of Life Science Research Asahi Kasei Corporation
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Ikegaki Ichiro
Laboratory For Pharmacology Asahi Chemical Industry
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Shibata Katsushi
Department Of Molecular Cell Pharmacology National Children 's Medical Research Center
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Tsujimoto Gozoh
Department Of Genomic Drug Discovery Science Graduate School Of Pharmaceutical Sciences Kyoto Univer
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Tsujimoto Gozoh
Department Of Genomic Drug Discovery Science Graduate School Of Pharmaceutical Sciences Kyoto Univer
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Ikegaki Ichiro
Laboratory For Pharmacology Institute For Life Science Research Asahi Chemical Industry
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ASANO Toshio
Laboratory for Pharmacology, Institute for Life Science Research, Asahi Chemical Industry
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