首页> 外国专利> Radiolabeled 1-aryl pyrazoles, the synthesis thereof and the use thereof as pest GABA receptor ligands

Radiolabeled 1-aryl pyrazoles, the synthesis thereof and the use thereof as pest GABA receptor ligands

机译:放射性标记的1-芳基吡唑,其合成及其作为有害GABA受体配体的用途

摘要

The present invention is directed to radiolabeled compounds of Formula I: embedded image;or salts thereof, where;R1 represents R8, R8O, R8SO2, R8SO or R8S in which R8 is tritiated or deuterated methyl;;X is halo, cyano, C1-6 alkoxycarbonyl, C2-6 alkynyl, optionally substituted;C6-14 aryl or an optionally substituted 5- to 7-membered heteroaromatic ring linked to thiazole via a carbon-carbon bond;;R2 is hydrogen or amino; and;R3-R7 are defined in the specification.;The invention is also directed to methods of using such compounds for demonstrating specific insect GABA receptors, qualitatively screening for compounds acting on an insect GABA receptor or quantitatively assaying concentrations of a compound acting on an insect GABA receptor.
机译:本发明涉及式I的放射性标记的化合物:<化学ID =“ CHEM-US-00001”> <图像alt =“嵌入式图像” file =“ US06409988-20020625-C00001.GIF” he =“ 115.92315” imgContent = “未定义” imgFormat =“ GIF” wi =“ 140.19075” /> ;或其盐,其中; R 1 代表R 8 < / Sup>,R 8 O,R 8 SO 2 ,R 8 SO或R 8 S,其中R 8 是tri化或氘代甲基;; X是卤素,氰基,C 1-6 烷氧羰基,C 2-6 < / Sub>炔基,任选取代; C 6-14 芳基或任选取代的5至7元杂芳香环,通过碳-碳键与噻唑连接;; R 2 是氢或氨基;说明书中定义了R 3 -R 7 。本发明还涉及使用此类化合物证明特定昆虫GABA受体的方法,定性筛选化合物作用于昆虫GABA受体的化合物或定量测定作用于昆虫GABA受体的化合物的浓度。

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