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首页> 外文期刊>Parasitology >Characterization of two classes of benzodiazepine binding sites in Schistosoma mansoni.
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Characterization of two classes of benzodiazepine binding sites in Schistosoma mansoni.

机译：曼氏血吸虫中两类苯并二氮杂结合位点的表征。

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摘要

As we have recently shown that GABA should be considered a putative neurotransmitter in Schistosoma mansoni, the present work aimed to search for GABAA receptors in adult worms using [3H]-flunitrazepam to label the allosteric benzodiazepine binding site which is classically present on GABAA receptor complexes. We detected a large population (Bmax=8.25+/-1.1 pmol x mg protein(-1)) of high affinity (Kd=33.6+/-1.5 nM) binding sites for flunitrazepam. These sites harboured a singular pharmacological modulation that does not fit well with a mammalian central benzodiazepine receptor, mainly due to a very high affinity for Ro5-4864 and a very low affinity for clonazepam. We also detected a second population of benzodiazepine binding sites labelled with high affinity (IC50=85 nM) by [3H]-PK11195, a selective ligand of the mammalian peripheral benzodiazepine receptor. In conclusion, this work describes the pharmacological properties of a large population of central-like benzodiazepine receptors supporting theirstudy as putative new targets for the development of anti-parasitic agents. We also describe, for the first time, the presence of peripheral benzodiazepine receptors in this parasite.
机译：正如我们最近显示的那样，在曼氏血吸虫中应将GABA视为推定的神经递质，本研究旨在使用[3H]-氟硝西m标记通常位于GABAA受体复合物上的变构苯并二氮杂结合位点来寻找成虫中GABAA受体。 。我们检测到大量的氟尼西epa具有高亲和力（Kd = 33.6 +/- 1.5 nM）结合位点（Bmax = 8.25 +/- 1.1 pmol x mg蛋白（-1））。这些位点具有单一的药理学调节，与哺乳动物的中央苯并二氮杂receptor受体不太吻合，这主要是由于对Ro5-4864的亲和力非常高，而对氯硝西am的亲和力很低。我们还检测到第二批苯并二氮杂卓结合位点，并被[3H] -PK11195（哺乳动物外围苯并二氮杂卓受体的选择性配体）标记为高亲和力（IC50 = 85 nM）。总之，这项工作描述了支持其研究的大量中央样苯并二氮杂receptor受体的药理学性质，这些受体是开发抗寄生虫药的推定新靶标。我们还首次描述了该寄生虫中周围苯并二氮杂receptor受体的存在。

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