Ro 15-1788 both antagonizes and potentiates adenosine-evoked depression of cerebral cortical neurons.
Ro 15-1788 both antagonizes and potentiates adenosine-evoked depression of cerebral cortical neurons.
复制标题
Ro 15-1788 可以拮抗并增强腺苷引起的大脑皮层神经元抑制。
DOI：
10.1016/0014-2999(87)90706-0
复制
发表时间：
1987
影响因子：
5
通讯作者：
Stair,RE
中科院分区：
文献类型：
--
作者：
Phillis,JW;Stair,RE
研究了具有激动剂性质的苯二氮卓类拮抗剂ro15 -1788对腺苷和腺苷5′- n -乙基羧胺（NECA）诱发的大鼠大脑皮质神经元活性抑制的作用。离子电泳应用的ro15 -1788与腺苷具有拮抗和电位相互作用。在施用Ro 15-1788期间，腺苷诱发的放电抑制幅度明显降低，在Ro 15-1788施用结束后，其持久的潜在效应变得明显。由NECA（腺苷的抗摄取类似物）引起的细胞放电抑制被Ro 15-1788拮抗，没有随后的增强作用。大量应用ro15 -1788对神经元放电具有抑制作用，这种作用可被腺苷受体阻滞剂咖啡因（20 mg/kg）拮抗。这些结果表明，ro15 -1788可能是腺苷受体的拮抗剂和腺苷反应的增强剂。腺苷抑制的延长可能是由于Ro 15-1788持续抑制腺苷摄取的结果。这些对腺苷反应的不同影响可能解释了Ro 15-1788的一些复杂行为。
The effects of Ro 15-1788, a benzodiazepine antagonist with some agonist properties, were studied on adenosine and adenosine 5′-N-ethyl-carboxamide (NECA)-evoked depressions of rat cerebral cortical neuronal activity. Iontophoretically applied Ro 15-1788 had both antagonistic and potentiative interactions with adenosine. Reductions in the magnitude of adenosine-evoked depressions of firing were evident during the period of Ro 15-1788 application, with a long-lasting potentiative effect becoming apparent upon termination of the Ro 15-1788 application. Depressions of cell firing evoked by NECA, an uptake-resistant analog of adenosine, were antagonized by Ro 15-1788, with no subsequent potentiation. Larger applications of Ro 15-1788 had a depressant action on neuronal firing, which was antagonized by caffeine (20 mg/kg), an adenosine receptor blocker. These results indicate that Ro 15-1788 may be an antagonist at the adenosine receptor as well as a potentiator of the adenosine response. The prolongation of the adenosine depression is likely to be the result of a persistent inhibition of adenosine uptake by Ro 15-1788. These diverse effects on the adenosine response may account for some of the complex behavioral actions of Ro 15-1788.