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肌苷和次黄嘌呤作为脑内苯二氮䓬结合位点内源性配体的鉴定。

Identification of inosine and hypoxanthine as endogenous ligands for the brain benzodiazepine-binding sites.

作者信息

Asano T, Spector S

出版信息

Proc Natl Acad Sci U S A. 1979 Feb;76(2):977-81. doi: 10.1073/pnas.76.2.977.

Abstract

Two endogenous ligands for the brain benzodiazepine-binding sites were isolated from bovine brain through gel filtration, paper electrophoresis, and paper chromatography. These ligands were identified as inosine and hypoxanthine, and both had a higher affinity for the brain benzodiazepine-binding sites than for benzodiazepine sites in some peripheral tissues. They did not bind to any other receptors tested, such as the opiate, muscarinic cholinergic, gamma-aminobutyric acid, and beta-adrenergic receptors. Both inosine and hypoxanthine competitively inhibited the binding of [3H]diazepam to the brain binding site.

摘要

通过凝胶过滤、纸电泳和纸色谱法,从牛脑中分离出两种脑苯二氮䓬结合位点的内源性配体。这些配体被鉴定为肌苷和次黄嘌呤,并且它们对脑苯二氮䓬结合位点的亲和力高于某些外周组织中的苯二氮䓬位点。它们不与任何其他测试受体结合,如阿片、毒蕈碱胆碱能、γ-氨基丁酸和β-肾上腺素能受体。肌苷和次黄嘌呤均竞争性抑制[3H]地西泮与脑结合位点的结合。

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