Raiteri Luca
Pharmacology and Toxicology Section, Department of Pharmacy (DIFAR), University of Genoa, 16148 Genoa, Italy.
Inter-University Center for the Promotion of the 3Rs Principles in Teaching & Research (Centro 3R), 16148 Genoa, Italy.
Biomedicines. 2024 Jul 8;12(7):1518. doi: 10.3390/biomedicines12071518.
Glycine plays a pivotal role in the Central Nervous System (CNS), being a major inhibitory neurotransmitter as well as a co-agonist of Glutamate at excitatory NMDA receptors. Interactions involving Glycine and other neurotransmitters are the subject of different studies. Functional interactions among neurotransmitters include the modulation of release through release-regulating receptors but also through transporter-mediated mechanisms. Many transporter-mediated interactions involve the amino acid transmitters Glycine, Glutamate, and GABA. Different studies published during the last two decades investigated a number of transporter-mediated interactions in depth involving amino acid transmitters at the nerve terminal level in different CNS areas, providing details of mechanisms involved and suggesting pathophysiological significances. Here, this evidence is reviewed also considering additional recent information available in the literature, with a special (but not exclusive) focus on glycinergic neurotransmission and Glycine-Glutamate interactions. Some possible pharmacological implications, although partly speculative, are also discussed. Dysregulations in glycinergic and glutamatergic transmission are involved in relevant CNS pathologies. Pharmacological interventions on glycinergic targets (including receptors and transporters) are under study to develop novel therapies against serious CNS pathological states including pain, schizophrenia, epilepsy, and neurodegenerative diseases. Although with limitations, it is hoped to possibly contribute to a better understanding of the complex interactions between glycine-mediated neurotransmission and other major amino acid transmitters, also in view of the current interest in potential drugs acting on "glycinergic" targets.
甘氨酸在中枢神经系统(CNS)中起着关键作用,它既是一种主要的抑制性神经递质,也是兴奋性N-甲基-D-天冬氨酸(NMDA)受体上谷氨酸的协同激动剂。涉及甘氨酸与其他神经递质的相互作用是不同研究的主题。神经递质之间的功能相互作用包括通过释放调节受体调节释放,也包括通过转运体介导的机制进行调节。许多转运体介导的相互作用涉及氨基酸递质甘氨酸、谷氨酸和γ-氨基丁酸(GABA)。在过去二十年中发表的不同研究深入调查了在不同中枢神经系统区域神经末梢水平上涉及氨基酸递质的多种转运体介导的相互作用,提供了相关机制的细节并提出了病理生理学意义。在此,我们将回顾这些证据,同时考虑文献中最近获得的其他信息,特别(但非排他性)关注甘氨酸能神经传递和甘氨酸 - 谷氨酸相互作用。还讨论了一些可能的药理学意义,尽管部分具有推测性。甘氨酸能和谷氨酸能传递的失调与相关的中枢神经系统疾病有关。针对甘氨酸能靶点(包括受体和转运体)的药理学干预正在研究中,以开发针对包括疼痛、精神分裂症、癫痫和神经退行性疾病在内的严重中枢神经系统病理状态的新疗法。尽管存在局限性,但希望能有助于更好地理解甘氨酸介导的神经传递与其他主要氨基酸递质之间的复杂相互作用,这也是鉴于目前对作用于“甘氨酸能”靶点的潜在药物的兴趣。