POTENTIAL USE OF DPCPX AS PROBE FOR INVIVO LOCALIZATION OF BRAIN-A1 ADENOSINE RECEPTORS

被引:23
作者
BISSERBE, JC
PASCAL, O
DECKERT, J
MAZIERE, B
机构
[1] NIH,NEUROCHEM UNIT,BETHESDA,MD 20892
[2] INSERM,SERV HOSP FREDERIC JOLIOT,ORSAY,FRANCE
关键词
DPCPX; ADENOSINE-A1; RECEPTOR; EXVIVO AUTORADIOGRAPHY; RAT;
D O I
10.1016/0006-8993(92)90845-Z
中图分类号
Q189 [神经科学];
学科分类号
071006 ;
摘要
The suitability of (H-3)DPCPX (8-cyclopentyl-1,3-dipropylxanthine), a xanthine derivative, as an vivo probe for labelling adenosine A1 receptors was studied in rats. [H-3]DPCPX (nM) penetrated largely into the brain (0.8% of the injected dose per gram of brain tissue 5 min after injection). Brain concentrations stayed at a plateau level from 5 to 15 min after the injection. The distribution in the different brain regions was heterogeneous with the highest amount of [H-3]DPCPX in cerebellum and hippocampus and the lowest concentrations in hypothalamus and brain stem. Displacement (45-70% of total radioactivity) was obtained by the injection of 250 nM of cold DPCPX or cyclopentylxanthine, an analog of DPCPX. The ex vivo autoradiographic distribution of [H-3]DPCPX was similar to the in vitro autoradiographic distribution of tritiated A1 adenosine receptor ligand as [H-3]CHA. These results suggest the potential use of DPCPX for further in vivo investigation of A1 adenosine receptors with techniques such as positron emission tomography.
引用
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页码:6 / 12
页数:7
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