Binding characteristics of 3H-dihydroalprenolol to .BETA.-adrenergic receptors of rat brain: Influence of exo- and endoglycosidases and glycopeptidase.
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概要
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The significance of carbohydrate moieties containing the β-adrenoceptor molecule in the rat brain was examined using radioligand binding assay methods. Thus, this experiment was designed to assess the effects of exoglycosidase (α-D-mannosidase and neuraminidase), endoglycosidase (endoglycosidase D and endoglycosidase H), and glycopeptidase A on the affinity of β-adrenoceptor. The main reason why five kinds of enzymes were used in the present study is that they can hydrolyze different carbohydrate molecules from cell membranes. Rat brain was used and β-adrenoceptor binding assay was carried out using <SUP>3</SUP>H-dihydroalprenolol (<SUP>3</SUP>H-DHA) as a ligand. <SUP>3</SUP>H-DHA binding to β-adrenoceptors was sensitive to very low concentration of endoglycosidase H and glycopeptidase A, thus indicating that the treatments with these enzymes of rat brain membrane appear to decrease the number of β-receptor binding sites. On the other hand, the treatment with neuraminidase, endoglycosidase H, and glycopeptidase A of the membrane induced lower values of the dissociation constant (K<SUB>d</SUB>) than those of the control. α-D-mannosidase and endoglycosidase D are without effect in spite of the removal of hexose contents and total carbohydrate contents with these treatments, respectively. These results imply that complex type N-linked acidic carbohydrate chains containing neuraminic acid and high mannose type N-linked carbohydrate chains, which are hydrolyzed with endoglycosidase H and glycopeptidase A, of the rat brain membrane containing β-adrenoceptor molecules play a crucial role in the drug-receptor interaction.
- 公益社団法人 日本薬理学会の論文
著者
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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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