Dunwiddie T V, Basile A S, Palmer M R
Life Sci. 1984 Jan 2;34(1):37-47. doi: 10.1016/0024-3205(84)90328-x.
Adenosine has profound depressant effects upon the electrophysiological activity of the brain, but the adenosine receptor subtypes which mediate these responses are uncertain. In order to resolve this question, we have characterized the effects of two adenosine analogs which differ in their relative potencies at adenosine A1 and A2 receptors. The effects of these adenosine analogs were examined on spontaneous firing rate of Purkinje neurons in the rat cerebellum in situ, in cerebellar brain slices in vitro, and on synaptic transmission in the rat hippocampus in vitro. Although the A2 agonist appeared to be more potent with local drug application techniques in situ, our in vitro results suggest that the A1 receptor subtype is involved in the electrophysiological actions of these drugs in both rat cerebellum and hippocampus. Furthermore, these data indicate that the physical properties of some adenosine analogs may reduce apparent drug potencies when they are studied with local application techniques.
腺苷对大脑的电生理活动具有显著的抑制作用,但其介导这些反应的腺苷受体亚型尚不确定。为了解决这个问题,我们对两种腺苷类似物的作用进行了表征,这两种类似物在腺苷A1和A2受体上的相对效力有所不同。研究了这些腺苷类似物对大鼠原位小脑浦肯野神经元的自发放电频率、体外小脑脑片以及体外大鼠海马体突触传递的影响。尽管在原位局部给药技术中,A2激动剂似乎更有效,但我们的体外实验结果表明,A1受体亚型参与了这些药物在大鼠小脑和海马体中的电生理作用。此外,这些数据表明,当使用局部给药技术研究某些腺苷类似物时,其物理性质可能会降低表观药物效力。