Assessment of Antihistaminic and Antimuscarinic Effects of Optical Isomers of Ephedrine and Methylephedrine by Receptor Binding Assay in Guinea Pig Ileal Muscle
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概要
- 論文の詳細を見る
Effects of optical isomers of ephedrine (EPH) and methylephedrine (MEP) on histamine H_1-receptors and muscarinic receptors in guinea pig ileal muscle were investigated by radioligand binding assay and by measuring the mechanical response to histamine and acetylcholine. EPH and MEP inhibited the specific binding of [^3H]mepyramine and [^3H]quinuclidinyl benzilate (QNB) to microsomal fractions prepared from this tissue. The rank order of inhibitory potency of [^3H]mepyramine and [^3H]QNB binding was d->l-isomer and l->d-isomer, respectively. Furthermore, the rank order of antagonistic potency in the mechanical response was the same as that in the binding study. d-MEP competitively antagonized histamine-induced contration (pA_2 value; 5.14). These results suggest that each isomer of EPH and MEP has a distinct affinity for histamine H_1-receptors and muscarinic receptors in guinea pig ileal muscle. The antihistaminic and antimuscarinic activity of these compounds may be largely attributed to competition at receptor sites. In addition, it is suggested that d-MEP exhibits a competitive antagonist activity for the histamine H_1-receptor.
- 公益社団法人日本薬学会の論文
- 1996-10-15
著者
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KOIKE Katsuo
Department of Chemical Pharmacology, Toho University School of Pharmaceutical Sciences
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Koike K
Department Of Chemical Pharmacology Toho University School Of Pharmaceutical Sciences
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Koike Katsuo
Department Of Chemical Pharmacology Toho University Faculty Of Pharmaceutical Sciences
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Saito Haruo
Department Of Pharmaceutical Research Lead Chemical Co. Ltd.
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Saito H
Toyama Prefectural Institute For Pharmaceutical Research
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KAWASUJI Toru
Toyama Prefectural Institute for Pharmaceutical Research
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SAITO Haruo
Toyama Prefectural Institute for Pharmaceutical Research
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Saito H
Department Of Chemical Pharmacology Faculty Of Pharmaceutical Sciences The University Of Tokyo
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Kawasuji T
Toyama Prefectural Institute For Pharmaceutical Research
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