关键词: Agonist G protein-coupled receptor antagonist cannabinoid receptor type 2 fibrosis inflammation

Mesh : Patents as Topic Humans Receptor, Cannabinoid, CB2 / metabolism agonists antagonists & inhibitors Animals Drug Development Ligands Cannabinoid Receptor Agonists / pharmacology Cannabinoid Receptor Antagonists / pharmacology

来  源:   DOI:10.1080/13543776.2024.2368745

Abstract:
UNASSIGNED: Cannabinoid receptor type 2 (CB2R), predominantly expressed in immune tissues, is believed to play a crucial role within the body\'s protective mechanisms. Its modulation holds immense therapeutic promise for addressing a wide spectrum of dysbiotic conditions, including cardiovascular, gastrointestinal, liver, kidney, neurodegenerative, psychiatric, bone, skin, and autoimmune diseases, as well as lung disorders, cancer, and pain management.
UNASSIGNED: This review is an account of patents from 2016 up to 2023 which describes novel CB2R ligands, therapeutic applications, synthesis, as well as formulations of CB2R modulators.
UNASSIGNED: The patents cover a vast, structurally diverse chemical space. The focus of CB2R ligand development has shifted from unselective dual-cannabinoid receptor type 1 (CB1R) and 2 agonists toward agonists with high selectivity over CB1R, particularly for indications associated with inflammation and tissue injury. Currently, there are at least eight CB2R agonists and one antagonist in active clinical development. A better understanding of the endocannabinoid system (ECS) and in particular of CB2R pharmacology is required to unlock the receptor\'s full therapeutic potential.
摘要:
大麻素受体2型(CB2R),主要在免疫组织中表达,被认为在人体的保护机制中起着至关重要的作用。它的调制具有巨大的治疗前景,可以解决广泛的双生条件,包括心血管,胃肠,肝脏,肾,神经退行性疾病,精神病学,骨头,皮肤,和自身免疫性疾病,以及肺部疾病,癌症,和疼痛管理。
这篇评论是对2016年至2023年的专利的描述,其中描述了新型CB2R配体,治疗应用,合成以及CB2R调节剂的配方。
专利涵盖了巨大的,结构多样的化学空间。CB2R配体开发的重点已经从无选择性的双大麻素受体1型(CB1R)和2激动剂转向对CB1R具有高选择性的激动剂,特别是与炎症和组织损伤相关的适应症。目前,至少有8种CB2R激动剂和1种拮抗剂处于积极的临床开发中.需要更好地了解内源性大麻素系统(ECS),特别是CB2R药理学,以释放受体的全部治疗潜力。
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