alpha(2)-Adrenoceptor subtypes in the human brain: A pharmacological delineation of [H-3]RX-821002 binding to membranes and tissue sections

被引:50
作者
Grijalba, B
Callado, LF
Meana, JJ
GarciaSevilla, JA
Pazos, A
机构
[1] UNIV CANTABRIA,DEPT PHYSIOL & PHARMACOL,E-39005 SANTANDER,SPAIN
[2] UNIV BASQUE COUNTRY,DEPT PHARMACOL,LEIOA,BIZKAIA,SPAIN
[3] UNIV BALEARIC ISL,NEUROPHARMACOL LAB,PALMA DE MALLORCA,SPAIN
关键词
alpha(2)-adrenoceptor subtype; brain; human; RX; 821002; autoradiography; frontal cortex; hippocampus;
D O I
10.1016/0014-2999(96)00381-0
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
In order to study the characterization and localization of [H-3]RX-821002 (2-methoxy-idazoxan) binding to alpha(2)-adrenoceptor subtypes in several regions of the human brain, we have carried out competition studies using both autoradiography and membrane binding assays. The alpha(2A)-adrenoceptor subtype was found to be predominant in the different layers of the frontal cortex, cerebellum and hippocampal formation, while in the neostriatum it was the non-alpha(2A)- (alpha(2B)- and alpha(2C)-) adrenoceptor subtype. In the frontal cortex, in addition to binding to the alpha(2A)-adrenoceptor subtype, [H-3]RX-821002 bound also to a small portion of alpha(2B)- and alpha(2C)-adrenoceptors in layer III, and labelled in the dentate gyrus and the CA(1) field, together with 5-HT1A receptors. 5-HT1A receptors were labelled predominantly in the stratum pyramidale layer. These results, in addition to delineate the relative presence of alpha(2)-adrenoceptor subtypes, indicate that caution is needed when analyzing RX 821002 binding to human brain tissue.
引用
收藏
页码:83 / 93
页数:11
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