Selective interaction of DG-5128 with a low agonist affinity state of alpha-2 adrenoceptor.
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概要
- 論文の詳細を見る
Using rat cerebral cortex membranes, the inhibitory effect of DG-5128 against (<SUP>3</SUP>H)-clonidine binding was compared between low (α<SUB>2L</SUB>) (in the presence of EDTA) and high (α<SUB>2H</SUB>) affinity states (in the presence of excess magnesium) of alpha<SUB>2</SUB>-adrenoceptor for agonists. The K<SUB>i</SUB> value (pK<SUB>i</SUB>=6.79) of DG-5128 in the α<SUB>2L</SUB> state was 6.4 times higher than the value in the α<SUB>2H</SUB> state. Thus, DG-5128 produces alpha<SUB>2</SUB>-adrenoceptor antagonism through the selective interaction with an α<SUB>2L</SUB> state of the receptor.
- 公益社団法人 日本薬理学会の論文
著者
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Muramatsu Ikunobu
Department Of Pharmacology Faculty Of Medicine Kyoto University And Department Of Zoology And Its Ca
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Kigoshi Shigeru
Department Of Pharmacology Fukui Medical School
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YAMANAKA Kyozo
Department of Pharmacology, Fukui Medical School
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