School of Physiology, Pharmacology and Neuroscience, University of Bristol, University Walk, Bristol, BS8 1TD, United Kingdom; Department of Physiology, Development and Neuroscience, University of Cambridge, Cambridge, United Kingdom.
Neuroscience Division, Eli Lilly & Co. Ltd., Windlesham, GU20 6PH, United Kingdom.
Neuropharmacology. 2018 Sep 15;140:246-259. doi: 10.1016/j.neuropharm.2018.07.013. Epub 2018 Jul 11.
Group II metabotropic glutamate receptors (mGluR2 and mGluR3) are implicated in a number of psychiatric disorders. They also control sleep-wake architecture and may offer novel therapeutic targets. However, the roles of the mGluR2 versus mGluR3 subtypes are not well understood. Here, we have taken advantage of the recently described mutant strain of Han Wistar rats, which do not express mGluR2 receptors, to investigate behavioural, sleep and EEG responses to mGluR2/3 ligands. The mGluR2/3 agonist, LY354740 (10 mg/kg), reversed amphetamine- and phencyclidine-induced locomotion and rearing behaviours in control Wistar but not in mGluR2 lacking Han Wistar rats. In control Wistar but not in Han Wistar rats the mGluR2/3 agonist LY379268 (3 & 10 mg/kg) induced REM sleep suppression with dose-dependent effects on wake and NREM sleep. By contrast, the mGluR2/3 antagonist LY3020371 (3 & 10 mg/kg) had wake-promoting effects in both rat strains, albeit smaller in the mGluR2-lacking Han Wistar rats, indicating both mGluR2 and mGluR3-mediated effects on wakefulness. LY3020371 enhanced wake cortical oscillations in the theta (4-9 Hz) and gamma (30-80 Hz) range in both Wistar and Han Wistar rat strains, whereas LY379268 reduced theta and gamma oscillations in control Wistar rats, with minimal effects in Han Wistar rats. Together these studies illustrate the significant contribution of mGluR2 to the antipsychotic-like, sleep and EEG effects of drugs acting on group II mGluRs. However, we also provide evidence of a role for mGluR3 activity in the control of sleep and wake cortical theta and gamma oscillations.
II 型代谢型谷氨酸受体(mGluR2 和 mGluR3)与许多精神疾病有关。它们还控制睡眠-觉醒结构,并可能提供新的治疗靶点。然而,mGluR2 与 mGluR3 亚型的作用尚不清楚。在这里,我们利用最近描述的 Han Wistar 大鼠突变株,该大鼠不表达 mGluR2 受体,来研究 mGluR2/3 配体对行为、睡眠和 EEG 的反应。mGluR2/3 激动剂 LY354740(10mg/kg)逆转了对照 Wistar 大鼠但不逆转缺乏 mGluR2 的 Han Wistar 大鼠中安非他命和苯环己哌啶诱导的运动和后肢抬高行为。在对照 Wistar 大鼠中,但不在缺乏 mGluR2 的 Han Wistar 大鼠中,mGluR2/3 激动剂 LY379268(3 和 10mg/kg)以剂量依赖的方式诱导 REM 睡眠抑制,对觉醒和 NREM 睡眠产生影响。相比之下,mGluR2/3 拮抗剂 LY3020371(3 和 10mg/kg)在两种大鼠品系中均具有促觉醒作用,尽管在缺乏 mGluR2 的 Han Wistar 大鼠中作用较小,表明 mGluR2 和 mGluR3 均对觉醒产生影响。LY3020371 在 Wistar 和 Han Wistar 大鼠中增强了θ(4-9Hz)和γ(30-80Hz)频段的皮层唤醒振荡,而 LY379268 降低了对照 Wistar 大鼠的θ和γ振荡,对 Han Wistar 大鼠的影响最小。这些研究共同说明了 mGluR2 对作用于 II 型 mGluR 的抗精神病样药物、睡眠和 EEG 作用的重要贡献。然而,我们还提供了 mGluR3 活性在控制睡眠和觉醒皮层θ和γ振荡中的作用的证据。