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首页> 外文期刊>Bioorganic and medicinal chemistry >A novel synthesis and pharmacological evaluation of a potential dopamine D1/D2 agonist: 1-propyl-1,2,3,4,4a,5,10,10a-octahydrobenzo(g)quinoline-6,7-diol.
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A novel synthesis and pharmacological evaluation of a potential dopamine D1/D2 agonist: 1-propyl-1,2,3,4,4a,5,10,10a-octahydrobenzo(g)quinoline-6,7-diol.

机译:潜在的多巴胺D1 / D2激动剂的新型合成和药理评估:1-丙基-1,2,3,4,4a,5,10,10a-八氢苯并(g)喹啉-6,7-二醇。

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摘要

Previously, we have demonstrated that enone prodrugs of dopaminergic catecholamines represent a new type of dopamine (DA) agonist. Trans-1-propyl-1,2,3,4,4a,5,10,10a-octahydrobenzo[g]quinoline-6,7-diol (TL-334), the active form of trans-1-propyl-2,3,4,4a,5,7,8,9,10,10a-decahydro-1H-benzo[g]quinolin-6-one (GMC-6650), in vivo showed an extremely potent dopaminergic activity. Here, we report a novel synthesis and a pharmacological evaluation of TL-334 by means of microdialysis.
机译:以前,我们已经证明多巴胺能儿茶酚胺的烯酮前药代表一种新型的多巴胺(DA)激动剂。反式-1-丙基-1,2,3,4,4a,5,10,10a-八氢苯并[g]喹啉-6,7-二醇(TL-334),反式-1-丙基-2的活性形式,3,4,4a,5,7,8,9,10,10a-十氢-1H-苯并[g]喹啉-6-一(GMC-6650),在体内表现出极强的多巴胺能活性。在这里,我们报告通过微透析的TL-334的新型合成和药理评价。

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