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首页> 外文期刊>Life sciences >ADAPTIVE CHANGES IN ADENOSINE RECEPTORS FOLLOWING LONG-TERM TREATMENT WITH THE ADENOSINE RECEPTOR AGONIST R-PHENYLISOPROPYL ADENOSINE
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ADAPTIVE CHANGES IN ADENOSINE RECEPTORS FOLLOWING LONG-TERM TREATMENT WITH THE ADENOSINE RECEPTOR AGONIST R-PHENYLISOPROPYL ADENOSINE

机译：腺嘌呤受体激动剂R-苯异丙基腺嘌呤长期治疗后腺苷受体的适应性变化

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Changes in brain A(1) and A(2A) receptors and in the corresponding mRNA were studied using quantitative receptor autoradiography and in situ hybridisation. [H-3]-DPCPX was used as an antagonist ligand at A(1) receptors and [H-3]-CGS 21680 as an agonist ligand at A(2A) receptors. Treatment of rats with the relatively A(1) receptor selective adenosine analogue R-PIA (0.3 mg/kg) for 7 days in the presence of the peripherally acting antagonist 8-p-sulfophenyltheophylline (8-PST; 10 mg/kg) caused a decrease in the binding of the A(1) receptor ligand, but not in that of the A(2A) receptor ligand. The effect on A(1) receptors was also seen in the presence of 100 mu M GTP that decreases agonist binding to insignificant levels. There was no change in either A(1) or A(2A) receptor mRNA. No significant changes were detected following administration of either R-PIA or 8-PST alone. These results thus demonstrate an effect on brain A(1) receptors after systemic administration of R-PIA in the presence of a peripherally acting adenosine antagonist, demonstrating that, under these conditions, the agonist reaches receptors in significant amounts. [References: 25]
机译：使用定量受体放射自显影和原位杂交研究了大脑A（1）和A（2A）受体以及相应mRNA中的变化。 [H-3] -DPCPX用作A（1）受体的拮抗剂配体，[H-3] -CGS 21680用作A（2A）受体的激动剂配体。在存在作用于周围的拮抗剂8-p-磺基苯基茶碱（8-PST; 10 mg / kg）的情况下，用相对A（1）受体选择性腺苷类似物R-PIA（0.3 mg / kg）治疗大鼠7天减少A（1）受体配体的结合，但不减少A（2A）受体配体的结合。在100μMGTP的存在下也可以看到对A（1）受体的影响，GTP减少了激动剂与微不足道水平的结合。 A（1）或A（2A）受体mRNA均无变化。单独施用R-PIA或8-PST后未检测到明显变化。因此，这些结果证明了在存在外围作用的腺苷拮抗剂的情况下全身性施用R-PIA后对大脑A（1）受体的影响，表明在这些条件下，激动剂可以大量到达受体。 [参考：25]

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