[H-3] L-694,247 LABELS THE 5-HT1D-BETA RECEPTOR IN PIG CAUDATE MEMBRANES

被引：11
作者：
HEALD, A [1 ]
STANTON, JA [1 ]
OSBORNE, SA [1 ]
MIDDLEMISS, DN [1 ]
BEER, MS [1 ]
机构：
[1] MERCK SHARP & DOHME LTD,NEUROSCI RES CTR,HARLOW CM20 2QR,ESSEX,ENGLAND
来源：
EUROPEAN JOURNAL OF PHARMACOLOGY | 1994年 / 264卷 / 02期
关键词：
H-3] L-694,247 (2-[5-[3-(4-METHYLSULPHONYLAMINO)BENZYL-1,2,4-OXADIAZOL-5-YL]-1H-INDOLE-3-YL]ETHYLAMINE); CAUDATE NUCLEUS; PIG; 5-HT1D-ALPHA 5-HT(1D-BETA) RECEPTOR;
D O I：
10.1016/0014-2999(94)00527-3
中图分类号：
R9 [药学];
学科分类号：
1007 ;
摘要：
This study, carried out in pig caudate membranes, characterises the radioligand binding site labelled with [H-3]L-694,247 (2-[5-[3-(4-methylsulphonylamino)benzyl-1,2,4-oxadiazol-5-yl]-1H-indole-3-yl]ethylamine). The affinities of 27 standard compounds are consistent with binding to a 5-HT1D recognition site. In addition the results indicate that, under the assay conditions described, [H-3]L-694,247 specifically labels the 5-HT1D beta recognition site since ketanserin and ritanserin display a low affinity consistent with their activities at this subtype of the 5-HT1D receptor.
引用
收藏
页码：213 / 216
页数：4
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