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首页> 外文期刊>European Journal of Medicinal Chemistry: Chimie Therapeutique >Dopamine/serotonin receptor ligands. Part VIII((1)):the dopamine receptor antagonist LE300 - modelled and X-ray structure plus further pharmacological characterization, including serotonin receptor binding, biogenic amine transporter testing and in v
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Dopamine/serotonin receptor ligands. Part VIII((1)):the dopamine receptor antagonist LE300 - modelled and X-ray structure plus further pharmacological characterization, including serotonin receptor binding, biogenic amine transporter testing and in v

机译：多巴胺/ 5-羟色胺受体配体。第VIII（（1）部分）：多巴胺受体拮抗剂LE300-建模和X射线结构，以及进一步的药理学表征，包括血清素受体结合，生物胺转运蛋白测试和体内

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摘要

-LE300, a benz[d]indolo[2,3-g]azecine with nanomolar affinities to the hD(1) receptor family, has been further pharmacologically characterized and its modelled structure was compared to its X-ray structure in order to explain NMR data, that was not in accordance to the X-ray structure. Moderate affinity at the hD(3) receptor was determined, nanomolar affinities were found at the 5-HT(2A) and 5-HT(2C) receptors, micromolar affinity at the 5-HT(1A) receptor using binding assays. Functional studies indicate moderate antagonist activity at the 5-HT(2A) site. No activity was found at dopamine, serotonin and norepinephrine transporters. These results suggested the use of LE300 for cocaine addiction treatment. High activities were found using in vivo testing: LE300 suppressed spontanous locomotor activity with an ID(50) of 1.24 mg/kg and attenuated locomotor activity induced by 20 mg/kg cocaine with an AD(50) of 1.50 mg/kg. It failed to substitute for the discriminative stimulus effects produced by cocaine.
机译：-LE300是与hD（1）受体家族具有纳摩尔摩尔亲和力的苯并[d]吲哚并[2,3-g] a嗪，已在药理上作了进一步表征，并将其建模结构与X射线结构进行了比较，以说明NMR数据，与X射线结构不一致。确定了在hD（3）受体的适度亲和力，在5-HT（2A）和5-HT（2C）受体发现了纳摩尔亲和力，使用结合试验在5-HT（1A）受体发现了微摩尔亲和力。功能研究表明在5-HT（2A）站点适度的拮抗剂活性。在多巴胺，5-羟色胺和去甲肾上腺素转运蛋白上未发现活性。这些结果表明LE300用于可卡因成瘾治疗。使用体内测试发现了高活性：LE300抑制了自发运动能力，ID（50）为1.24 mg / kg，减弱了20 mg / kg可卡因诱导的运动能力，AD（50）为1.50 mg / kg。它不能替代可卡因产生的歧视性刺激作用。

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