Lin Y, Phillis J W
Department of Physiology, Wayne State University School of Medicine, Detroit, MI 48201.
Brain Res. 1991 Feb 1;540(1-2):307-10. doi: 10.1016/0006-8993(91)90525-z.
The identity of the receptors involved in mediating the depressant actions of adenosine and its analogs on the spontaneous firing of rat cerebral cortical neurons was elucidated by evaluating the effects of selective A1 and A2 receptor agonists and antagonists. The A1 agonist N6-cyclopentyladenosine (CPA) and the A2 agonist CGS 21680 both depressed cortical neuronal firing. At low doses (0.001-0.01 mg/kg) the A1 antagonist DPCPX blocked the effects of CPA, but not those of CGS 21680. At higher doses, it antagonized both agonists. The A2 antagonist CGS 15943 (0.01-0.1 mg/kg) selectively blocked the actions of CGS 21680. At 1 mg/kg it also antagonized the responses of some neurons to CPA. These results suggest that the depressant actions of adenosinergic agonists on the firing of rat cerebral cortical neurons involve both A1 and A2 receptors.
通过评估选择性A1和A2受体激动剂及拮抗剂的作用，阐明了介导腺苷及其类似物对大鼠大脑皮质神经元自发放电的抑制作用的受体特性。A1激动剂N6-环戊基腺苷（CPA）和A2激动剂CGS 21680均能抑制皮质神经元放电。低剂量（0.001-0.01mg/kg）时，A1拮抗剂DPCPX可阻断CPA的作用，但不影响CGS 21680的作用。高剂量时，它对两种激动剂均有拮抗作用。A2拮抗剂CGS 15943（0.01-0.1mg/kg）可选择性阻断CGS 21680的作用。在1mg/kg时，它也能拮抗部分神经元对CPA的反应。这些结果表明，腺苷能激动剂对大鼠大脑皮质神经元放电的抑制作用涉及A1和A2受体。
