Department of Pharmacology and Toxicology, The State University of New York at Buffalo, Buffalo, NY 14203, USA.
Department of Cellular and Integrative Physiology, University of Texas Health Science Center at San Antonio, San Antonio, TX 78229, USA.
Int J Mol Sci. 2020 Jul 12;21(14):4918. doi: 10.3390/ijms21144918.
Inflammation is a key physiological phenomenon that can be pervasive when dysregulated. Persistent chronic inflammation precedes several pathophysiological conditions forming one of the critical cellular homeostatic checkpoints. With a steady global surge in inflammatory diseases, it is imperative to delineate underlying mechanisms and design suitable drug molecules targeting the cellular partners that mediate and regulate inflammation. Nicotinic acetylcholine receptors have a confirmed role in influencing inflammatory pathways and have been a subject of scientific scrutiny underlying drug development in recent years. Drugs designed to target allosteric sites on the nicotinic acetylcholine receptors present a unique opportunity to unravel the role of the cholinergic system in regulating and restoring inflammatory homeostasis. Such a therapeutic approach holds promise in treating several inflammatory conditions and diseases with inflammation as an underlying pathology. Here, we briefly describe the potential of cholinergic allosterism and some allosteric modulators as a promising therapeutic option for the treatment of neuroinflammation.
炎症是一种普遍存在的生理现象，但如果失调就会成为问题。持续的慢性炎症先于几种病理生理状况发生，是细胞内稳态的关键检查点之一。随着炎症性疾病在全球范围内的稳步增加，阐明潜在机制并设计针对调节和控制炎症的细胞伴侣的合适药物分子至关重要。烟碱型乙酰胆碱受体在影响炎症途径方面起着确定的作用，并且近年来一直是药物开发的科学研究主题。旨在针对烟碱型乙酰胆碱受体变构位点的药物为揭示胆碱能系统在调节和恢复炎症内稳态中的作用提供了独特的机会。这种治疗方法有望治疗几种以炎症为潜在病理的炎症性疾病。在这里，我们简要描述了胆碱能变构作用的潜力和一些变构调节剂作为治疗神经炎症的有希望的治疗选择。
