Tetranitromethane modification of the muscarinic receptors in bovine adrenal medulla.
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概要
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Muscarinic receptor binding was examined in bovine adrenal medullary microsomes following exposure to tetranitromethane (TNM) that modifies tyrosine and cysteine residues in proteins. The TNM (10-100 μM) treatment of adrenal medullary microsomes caused a concentration-dependent and irreversible reduction in the maximum number of binding sites (B<SUB>max</SUB>) for /-(<SUP>3</SUP>H)quinuclidinyl benzilate (QNB), with a slight increase in the equilibrium dissociation constant (K<SUB>D</SUB>). Typically, about a 36% decrease and a 1.3-fold increase in the corresponding values were obtained at 50 μM of TNM. The alteration in the B<SUB>max</SUB> was partially prevented by atropine but not carbamylcholine, and it was not reversed by subsequent treatment with dithiothreitol, a disulfide reducing agent. The change in the K<SUB>D</SUB> was unaffected by these agents. The TNM (50 μM) treatment also caused a slight decrease in the affinity of atropine and pirenzepine (for both the high and low affinity sites), and it caused a slight decrease in the affinity of carbamylcholine at the high affinity site, with a large loss of the low affinity site. Thus, the results indicate that TNM causes a loss of muscarinic binding sites and a decrease in the binding affinity of muscarinic receptors in bovine adrenal medulla, probably through modifications of functional groups such as tyrosine residues.
- 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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