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异吲哚酮:与纯化的内源性单胺氧化酶抑制剂刺蒺藜素一致。

Isatin: identity with the purified endogenous monoamine oxidase inhibitor tribulin.

作者信息

Glover V, Halket J M, Watkins P J, Clow A, Goodwin B L, Sandler M

机构信息

Department of Chemical Pathology, Queen Charlotte's Hospital, London, England.

出版信息

J Neurochem. 1988 Aug;51(2):656-9. doi: 10.1111/j.1471-4159.1988.tb01089.x.

Abstract

Purified tribulin, an endogenous monoamine oxidase (MAO) inhibitor, has been identified by direct probe insertion mass spectrometry as the indole-2,3-dione, isatin. A gas chromatographic-mass spectrometric assay for isatin has been developed and used to measure its relatively high concentrations in unpurified human urine, and in rat heart and brain. Isatin is a known compound with a broad range of biological activity; this is the first report of its presence in the animal body. Isatin is a potent inhibitor of MAO, particularly of MAO B (IC50, 3 microM), and also binds to central benzodiazepine receptors (IC50 against clonazepam, 123 microM).

摘要

纯化的色氨酸,一种内源性单胺氧化酶(MAO)抑制剂,已通过直接探针插入质谱法鉴定为吲哚-2,3-二酮,即异吲哚酮。已开发出一种用于测定异吲哚酮的气相色谱-质谱分析法,并用于测量其在未纯化的人尿、大鼠心脏和大脑中的相对高浓度。异吲哚酮是一种已知的具有广泛生物活性的化合物;这是其在动物体内存在的首次报道。异吲哚酮是MAO的有效抑制剂,尤其是MAO B(IC50,3 microM),并且还与中枢苯二氮䓬受体结合(对氯硝西泮的IC50,123 microM)。

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