Binding characteristics of (3H)quinupramine to rat brain membrane fractions.
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概要
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The binding characteristics of [<SUP>3</SUP>H]quinupramine to rat brain membrane fractions were studied. The specific binding of [<SUP>3</SUP>H]quinupramine to rat brain membrane fractions was stable, reversible and saturable. Scatchard analysis of the data from saturation experiments indicated that the specific binding was a single population with an affinity (K<SUB>D</SUB>) of 3.04 nM, a maximal binding site number (B<SUB>max</SUB>) of 714 fmol/mg protein, and a Hill coefficent (n<SUB>H</SUB>) of 1.08. Compounds known to inhibit muscarinic cholinergic receptors such as atropine and quinuclidinyl benzilate were the most potent competitors of [<SUP>3</SUP>H]quinupramine binding. When the drug potencies in inhibiting [<SUP>3</SUP>H]quinupramine binding were tested in the presence of 10 nM atropine, mianserin was the most potent competitor. Studies of the subcellular fractions showed that there was an enrichment of [<SUP>3</SUP>H]quinupramine binding sites in the synaptosome fraction. The regional distribution study revealed the highest densities of binding sites in the cerebral cortex and the lowest in the cerebellum. Thus, the specific binding of [<SUP>3</SUP>H]quinupramine observed here can be accounted for by both muscarinic cholinergic and serotonin S<SUB>2</SUB> receptors.
- 公益社団法人 日本薬理学会の論文
著者
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Ohata Katsuya
Department Of Pharmacology Kyoto Pharmaceutical University:department Of Pneumology Ogaki Municipal
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NISHIMOTO Takashi
Department of Thoracic Surgery, OSAKA MEDICAL COLLEGE, Takatsuki, JAPAN
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Kohno Shigekatsu
Department Of Pharmacology Division Of Pathological Sciences Kyoto Pharmaceutical University
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Tatsumi Hiroshi
Research Laboratories Dainippon Pharmaceutical Co. Ltd.
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SAKAMOTO Hirohiko
Department of Pharmacology, Kyoto Pharmaceutical University
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YOKOYAMA Nobuharu
Department of Pharmacology, Kyoto Pharmaceutical University
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MURAI Kazuyuki
Research Laboratories, Nippon Shoji Kaisha, Ltd.
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NISHIMOTO Takashi
Department of Pharmacology, Kyoto Pharmaceutical University
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