Department of Physiology and Pharmacology, University Sapienza, Rome, Italy. mail:
J Neurosci. 2010 Feb 24;30(8):2835-43. doi: 10.1523/JNEUROSCI.4834-09.2010.
We applied the group-I metabotropic glutamate (mGlu) receptor agonist, 3,5-dihydroxyphenylglycine (DHPG), to neonatal or adult rat hippocampal slices at concentrations (10 microM) that induced a short-term depression (STD) of excitatory synaptic transmission at the Schaffer collateral/CA1 synapses. DHPG-induced STD was entirely mediated by the activation of mGlu5 receptors because it was abrogated by the mGlu5 receptor antagonist, MPEP [2-methyl-6-(phenylethynyl)pyridine], but not by the mGlu1 receptor antagonist, CPCCOEt [7-(hydroxyimino)cyclopropa[b]chromen-1a-carboxylate ethyl ester]. Knowing that ephrin-Bs functionally interact with group-I mGlu receptors (Calò et al., 2005), we examined whether pharmacological activation of ephrin-Bs could affect DHPG-induced STD. We activated ephrin-Bs using their cognate receptor, EphB1, under the form of a preclustered EphB1/Fc chimera. Addition of clustered EphB1/Fc alone to the slices induced a small but nondecremental depression of excitatory synaptic transmission, which differed from the depression induced by 10 microM DHPG. Surprisingly, EphB1/Fc-induced synaptic depression was abolished by MPEP (but not by CPCCOEt) suggesting that it required the endogenous activation of mGlu5 receptors. In addition, coapplication of DHPG and EphB1/Fc, resulted in a large and nondecremental long-term depression. The effect of clustered EphB1/Fc was specific because it was not mimicked by unclustered EphB1/Fc or clustered EphA1/Fc. These findings raise the intriguing possibility that changes in synaptic efficacy mediated by mGlu5 receptors are under the control of the ephrin/Eph receptor system, and that the neuronal actions of ephrins can be targeted by drugs that attenuate mGlu5 receptor signaling.
我们将组 I 代谢型谷氨酸 (mGlu) 受体激动剂 3,5-二羟苯甘氨酸 (DHPG) 应用于新生或成年大鼠海马切片中,浓度为 10μM,可诱导 Schaffer 侧支/CA1 突触的兴奋性突触传递产生短期抑制 (STD)。DHPG 诱导的 STD 完全由 mGlu5 受体的激活介导,因为它被 mGlu5 受体拮抗剂 MPEP [2-甲基-6-(苯乙炔基)吡啶] 消除,但不受 mGlu1 受体拮抗剂 CPCCOEt [7-(羟基亚氨基)环丙基[b]chromen-1a-羧酸乙酯]的影响。已知 Ephrins-Bs 与组 I mGlu 受体(Calò 等人,2005) 功能相互作用,我们检查了 Ephrins-Bs 的药理学激活是否会影响 DHPG 诱导的 STD。我们使用 EphB1 的同源受体 EphB1/Fc 三聚体来激活 Ephrins-Bs。单独添加三聚 EphB1/Fc 到切片中会引起兴奋性突触传递的小但非递减性抑制,这与 10μM DHPG 诱导的抑制不同。令人惊讶的是,EphB1/Fc 诱导的突触抑制被 MPEP(但不是 CPCCOEt)消除,表明它需要内源性 mGlu5 受体的激活。此外,DHPG 和 EphB1/Fc 的共同应用导致了大的非递减性长时程抑制。三聚 EphB1/Fc 的作用是特异性的,因为未聚集的 EphB1/Fc 或聚集的 EphA1/Fc 不能模拟它。这些发现提出了一个有趣的可能性,即由 mGlu5 受体介导的突触效能变化受 Ephrins/Eph 受体系统的控制,并且 Ephrins 的神经元作用可以通过削弱 mGlu5 受体信号的药物来靶向。