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普通水螅中γ-氨基丁酸(GABA)受体的生化与功能鉴定

Biochemical and functional identification of GABA receptors in Hydra vulgaris.

作者信息

Pierobon P, Concas A, Santoro G, Marino G, Minei R, Pannaccione A, Mostallino M C, Biggio G

机构信息

Istituto di Cibernetica, C.N.R., Arco Felice (Naples), Italy.

出版信息

Life Sci. 1995;56(18):1485-97. doi: 10.1016/0024-3205(95)00111-i.

Abstract

GABA binding sites labelled in vitro with [3H]GABA are present in crude membrane preparations from Hydra vulgaris. [3H]GABA binding is specific (70%), saturable and it is completely displaced by the GABA mimetic muscimol but not by bicuculline or baclofen. Scatchard analysis of saturation data indicates the presence of only one population of binding sites with a Bmax of 4, 75 pmol/mg of protein and a KD of 76 nM. In the living animal GABA and benzodiazepines increase the duration of mouth opening during the glutathione-induced feeding response. Bicuculline prevents the GABA-induced increase of the feeding response. Diazepam activity is enhanced by simultaneous GABA administration and it is suppressed by the specific antagonist flumazenil. In contrast, no [3H]-flunitrazepam binding is detected in membrane preparations. We conclude that a population of GABA receptors is present in Hydra tissues, where they are involved in the modulation of response to chemical stimulation.

摘要

用[3H]GABA在体外标记的GABA结合位点存在于普通水螅的粗膜制剂中。[3H]GABA结合具有特异性(70%)、可饱和性,且能被GABA模拟物蝇蕈醇完全取代,但不能被荷包牡丹碱或巴氯芬取代。对饱和数据进行Scatchard分析表明,仅存在一类结合位点,其最大结合容量(Bmax)为4.75 pmol/mg蛋白质,解离常数(KD)为76 nM。在活体动物中,GABA和苯二氮䓬类药物会增加谷胱甘肽诱导的摄食反应中张口的持续时间。荷包牡丹碱可阻止GABA诱导的摄食反应增强。同时给予GABA可增强地西泮的活性,而其特异性拮抗剂氟马西尼可抑制该活性。相反,在膜制剂中未检测到[3H]氟硝西泮结合。我们得出结论,水螅组织中存在一类GABA受体,它们参与对化学刺激反应的调节。

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