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首页> 外文期刊>Journal of Medicinal Chemistry >Discovery of 5-(4-Chlorophenyl)-l-(2,4-dichlorophenyl)-3-hexyl-lH-l,2,4-triazole,a Novel in Vivo Cannabinoid Antagonist Containing a 1,2,4-Triazole Motif
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Discovery of 5-(4-Chlorophenyl)-l-(2,4-dichlorophenyl)-3-hexyl-lH-l,2,4-triazole,a Novel in Vivo Cannabinoid Antagonist Containing a 1,2,4-Triazole Motif

机译:发现5-(4-氯苯基)-1-(2,4-二氯苯基)-3-己基-1H-1,2,4-三唑,一种含有1,2,4-三唑基序的体内大麻拮抗剂。

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摘要

A new series of 1,2,4-triazoles have been prepared and the evaluation of their cannabinoid properties have been carried out.Compound 8 showed cannabinoid silent antagonist activity in mouse vas deferens and guinea pig ileum preparations and in vivo assays(cannabinoid tetrad) in mouse.It did not have intrinsic activity in these bioassays,and therefore,it did not behave as a partial agonist or an inverse agonist.
机译:制备了一系列新的1,2,4-三唑并对其大麻素性能进行了评估。化合物8显示了在小鼠输精管和豚鼠回肠制剂中的大麻素沉默拮抗剂活性以及体内测定法(大麻四元)在这些生物测定中,它没有固有的活性,因此,它不具有部分激动剂或反向激动剂的作用。

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