Lovinger David M
Laboratory for Integrative Neuroscience, Division of Intramural Clinical and Biological Research, National Institute on Alcohol Abuse and Alcoholism, Bethesda, MD, USA.
Handb Exp Pharmacol. 2018;248:29-54. doi: 10.1007/164_2017_76.
Ethanol produces intoxication through actions on numerous molecular and cellular targets. Adaptations involving these and other targets contribute to chronic drug actions that underlie continued and problematic drinking. Among the mechanisms involved in these ethanol actions are alterations in presynaptic mechanisms of synaptic transmission, including presynaptic protein function and excitation-secretion coupling. At synapses in the central nervous system (CNS), excitation-secretion coupling involves ion channel activation followed by vesicle fusion and neurotransmitter release. These mechanisms are altered by presynaptic neurotransmitter receptors and prominently by G protein-coupled receptors (GPCRs). Studies over the last 20-25 years have revealed that acute ethanol exposure alters neurotransmitter secretion, with especially robust effects on synapses that use the neurotransmitter gamma-aminobutyric acid (GABA). Intracellular signaling pathways involving second messengers such as cyclic AMP and calcium are implicated in these acute ethanol actions. Ethanol-induced release of neuropeptides and small molecule neurotransmitters that act on presynaptic GPCRs also contribute to presynaptic potentiation at synapses in the amygdala and hippocampus and inhibition of GABA release in the striatum. Prolonged exposure to ethanol alters neurotransmitter release at many CNS GABAergic and glutamatergic synapses, and changes in GPCR function are implicated in many of these neuroadaptations. These presynaptic neuroadaptations appear to involve compensation for acute drug effects at some synapses, but "allostatic" effects that result in long-term resetting of synaptic efficacy occur at others. Current investigations are determining how presynaptic neuroadaptations contribute to behavioral changes at different stages of alcohol drinking, with increasing focus on circuit adaptations underlying these behaviors. This chapter will discuss the acute and chronic presynaptic effects of ethanol in the CNS, as well as some of the consequences of these effects in amygdala and corticostriatal circuits that are related to excessive seeking/drinking and ethanol abuse.
乙醇通过作用于众多分子和细胞靶点而产生中毒效应。涉及这些及其他靶点的适应性变化导致了慢性药物作用,而这种作用是持续饮酒及饮酒问题的基础。在这些乙醇作用机制中,包括突触前蛋白功能和兴奋 - 分泌偶联在内的突触传递前机制发生了改变。在中枢神经系统(CNS)的突触处,兴奋 - 分泌偶联涉及离子通道激活,随后是囊泡融合和神经递质释放。这些机制会被突触前神经递质受体改变,尤其是G蛋白偶联受体(GPCRs)。过去20 - 25年的研究表明,急性乙醇暴露会改变神经递质分泌,对使用神经递质γ-氨基丁酸(GABA)的突触影响尤为显著。涉及环磷酸腺苷和钙等第二信使的细胞内信号通路与这些急性乙醇作用有关。乙醇诱导的作用于突触前GPCRs的神经肽和小分子神经递质释放,也有助于杏仁核和海马体突触处的突触前增强以及纹状体中GABA释放的抑制。长期暴露于乙醇会改变许多中枢神经系统GABA能和谷氨酸能突触处的神经递质释放,GPCR功能的变化与许多这些神经适应性变化有关。这些突触前神经适应性变化在某些突触似乎是对急性药物效应的代偿,但在其他突触则会导致突触效能的长期重置的“应变稳态”效应。目前的研究正在确定突触前神经适应性变化如何在饮酒的不同阶段导致行为改变,并且越来越关注这些行为背后的神经回路适应性变化。本章将讨论乙醇在中枢神经系统中的急性和慢性突触前效应,以及这些效应在杏仁核和皮质纹状体回路中与过度觅酒/饮酒及乙醇滥用相关的一些后果。