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[异吲哚酮:在利钠肽与单胺功能相互作用中的可能作用]

[Isatin: possible role in functional interaction of natriuretic peptides and monoamines].

作者信息

Glover V, Medvedev A E, Sandler M

机构信息

Queen Charlotte's and Chelsea Hospital, London UK.

出版信息

Vopr Med Khim. 1997 Nov-Dec;43(6):515-21.

PMID:9503568
Abstract

Isatin is an endogenous compound recently discovered in mammalian tissues and body fluids. It has a distinct distribution in rat brain, with a highest concentration, in the hippocampus, of 0.1 microgram/g. Its origin and metabolic pathways remain unclear. In vitro, isatin selectively inhibits monoamine oxidase (MAO) B (IC50 3-8 microM, Ki approximately 20 microM) and, more potently, atrial natriuretic peptide(ANP) binding (IC50, 0.4 microM). Convulsant doses of pentylene tetrazole result in increased isatin level in the brain. Small amounts of isatin are anxiogenic in rodent models, but higher doses cause sedation and possess anticonvulsant action. Isatin administration also increases monoamine levels in the brain and reduces daily urine output.

摘要

异吲哚酮是最近在哺乳动物组织和体液中发现的一种内源性化合物。它在大鼠脑中具有独特的分布,在海马体中的浓度最高,为0.1微克/克。其来源和代谢途径尚不清楚。在体外,异吲哚酮选择性抑制单胺氧化酶(MAO)B(IC50为3-8微摩尔,Ki约为20微摩尔),更有效地抑制心房利钠肽(ANP)结合(IC50为0.4微摩尔)。惊厥剂量的戊四氮会导致脑中异吲哚酮水平升高。在啮齿动物模型中,少量异吲哚酮具有致焦虑作用,但高剂量会导致镇静并具有抗惊厥作用。给予异吲哚酮还会增加脑中的单胺水平并减少每日尿量。

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