Marchi Mario, Grilli Massimo, Pittaluga Anna M
Department of Pharmacy, Pharmacology and Toxicology Section, University of Genoa , Genoa, Italy ; Center of Excellence for Biomedical Research, University of Genoa , Genoa, Italy.
Department of Pharmacy, Pharmacology and Toxicology Section, University of Genoa , Genoa, Italy.
Front Pharmacol. 2015 Apr 29;6:89. doi: 10.3389/fphar.2015.00089. eCollection 2015.
This review focuses on a specific interaction occurring between the nicotinic cholinergic receptors (nAChRs) and the glutamatergic receptors (GluRs) at the nerve endings level. We have employed synaptosomes in superfusion and supplemented and integrated our findings with data obtained using techniques from molecular biology and immuno-cytochemistry, and the assessment of receptor trafficking. In particular, we characterize the following: (1) the direct and unequivocal localization of native α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid (AMPA) and N-methyl-D-aspartate (NMDA) glutamatergic receptors on specific nerve terminals, (2) their pharmacological characterization and functional co-localization with nAChRs on the same nerve endings, and (3) the existence of synergistic or antagonistic interactions among them. Indeed, in the rat nucleus accumbens (NAc), the function of some AMPA and NMDA receptors present on the dopaminergic and glutamatergic nerve terminals can be regulated negatively or positively in response to a brief activation of nAChRs. This effect occurs rapidly and involves the trafficking of AMPA and NMDA receptors. The event takes place also at very low concentrations of nicotine and involves the activation of several nAChRs subtypes. This dynamic control by cholinergic nicotinic system of glutamatergic NMDA and AMPA receptors might therefore represent an important neuronal presynaptic adaptation associated with nicotine administration. The understanding of the role of these nicotine-induced functional changes might open new and interesting perspectives both in terms of explaining the mechanisms that underlie some of the effects of nicotine addiction and in the development of new drugs for smoking cessation.
本综述聚焦于烟碱型胆碱能受体(nAChRs)与谷氨酸能受体(GluRs)在神经末梢水平发生的特定相互作用。我们采用了在灌流条件下的突触体,并将分子生物学、免疫细胞化学技术以及受体转运评估所获得的数据补充并整合到我们的研究结果中。具体而言,我们对以下方面进行了表征:(1)天然α-氨基-3-羟基-5-甲基-4-异恶唑丙酸(AMPA)和N-甲基-D-天冬氨酸(NMDA)谷氨酸能受体在特定神经末梢上的直接且明确的定位;(2)它们的药理学特性以及与同一神经末梢上的nAChRs的功能共定位;(3)它们之间协同或拮抗相互作用的存在。实际上,在大鼠伏隔核(NAc)中,多巴胺能和谷氨酸能神经末梢上存在的一些AMPA和NMDA受体的功能可因nAChRs的短暂激活而受到正向或负向调节。这种效应迅速发生,涉及AMPA和NMDA受体的转运。该事件在极低浓度的尼古丁作用下也会发生,并且涉及多种nAChRs亚型的激活。因此,胆碱能烟碱系统对谷氨酸能NMDA和AMPA受体的这种动态控制可能代表了与尼古丁给药相关的一种重要的神经元突触前适应性变化。对这些尼古丁诱导的功能变化所起作用的理解,可能在解释尼古丁成瘾的某些效应背后的机制以及开发戒烟新药方面都开辟新的且有趣的视角。