Characteristics of binding of a new anti-inflammatory glucocorticoid, hydrocortisone 17-butyrate 21-propionate (HBP), to glucocorticoid receptors of rat liver.
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概要
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Characteristics of the specific binding of hydrocortisone 17-butyrate 21-propionate (HBP) to the cytoplasmic fraction from rat liver were investigated. The inhibition constant (K<SUB>i</SUB>) of HBP for the site of <SUP>3</SUP>H-dexamethasone (<SUP>3</SUP>H-DM) binding was approximately equal to the value of DM and significantly smaller than that of hydrocortisone (HC). The maximum number of binding sites (B<SUB>max</SUB>) and dissociation constant (K<SUB>d</SUB>) for <SUP>3</SUP>H-HBP were also approximately equal to those for <SUP>3</SUP>H-DM . The Scatchard and Hofstee plots analyses of <SUP>3</SUP>H-HC binding indicated that the HC binding sites consisted of three components with different affinity, while that of <SUP>3</SUP>H-DM had only one site with an intermediate affinity. HBP and hydrocortisone 17-butyrate (HB) bound to other binding sites of HC in addition to the site for DM. The IC50 value for synthetic glucocorticoids determined from the inhibition curves of <SUP>3</SUP>H-HC binding in the first phase agreed with the values determined by the displacement study of <SUP>3</SUP>H-DM binding. Furthermore, the first phase of HBP in the inhibition curve of <SUP>3</SUP>H-HC binding disappeared from the curve, and only the second phase remained following the addition of DM. These results indicate that the esterification of C-17 and C-21 OH increases the affinity of the binding site for synthetic glucocorticoid and attenuates the affinity for the other binding sites of HC.
- 公益社団法人 日本薬理学会の論文
著者
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Kuriyama Kinya
Department Of Health Promoting Acupuncture And Moxibution Meiji University Of Oriental Medicine
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Aihara Hironaka
Research Center Taisho Pharmaceutical Co. Ltd.
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Muramatsu Makoto
Research Center Taisho Pharmaceutical Co. Ltd.
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KURIYAMA Kinya
Department of Pharmacology, Kyoto Prefectual University of Medicine
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TANAKA Makoto
Research Center, Taisho Pharmaceutical Co., Ltd
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MURAMATSU Makoto
Research Center, Taisho Pharmaceutical Co., Ltd
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OTOMO Susumu
Research Center, Taisho Pharmaceutical Co., Ltd
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