小分子对大麻素2受体 (CB2R) 的进展
Qinying Zhang1, Ying Zhao1, Jianan Wu1
1Hangzhou Medical College, Hangzhou, Zhejiang, China.
Bioorganic chemistry
|January 13, 2024
概括
研究人员正在开发新的CB2受体配体,用于治疗炎症和疼痛等疾病. 这些配体通过将中枢神经系统的副作用降到最低,为CB1受体药物提供了更安全的替代品.
科学领域:
- 药理学和药物化学 药理学和药物化学
- 神经科学是一个神经科学.
- 免疫学 免疫学 免疫学
背景情况:
- 大麻素受体 (CBR),包括CB1R和CB2R,是针对各种疾病的G蛋白结合受体 (GPCR).
- CB1R的中枢神经系统 (CNS) 分布导致精神病副作用和成.
- CB2R的外周免疫系统分布提供了更安全的治疗特征,对中枢神经系统的影响较少.
研究的目的:
- 审查最近在CB2受体 (CB2R) 配体开发方面的进展.
- 为未来关于CB2R配体发现的研究提供参考.
- 突出选择性CB2R激动剂的治疗潜力.
主要方法:
- 关于CB2R配体的最新研究的文献综述.
- 配体的分类为内源性,天然化合物和新型小分子.
- 对已开发的CB2R配体的结合亲和力和选择性的分析.
主要成果:
- 在开发高结合亲和力和选择性CB2R配体方面取得了重大进展.
- 已经确定了各种各样的CB2R配体,包括天然产品和合成分子.
- 这些连接体显示出治疗炎症,神经病痛和免疫系统疾病等疾病的前景.
结论:
- 与CB1R配体相比,CB2R配体是一个有前途的治疗策略,与CB1R配体相比,具有有利的安全性.
- 对于各种临床应用而言,对CB2R配体发展的持续研究是有必要的.
- 审查的配体是未来针对CB2R的药物发现工作的宝贵资源.
更多相关视频
14:25Synthesis of a Deuterated Standard for the Quantification of 2-Arachidonoylglycerol in Caenorhabditis elegans
Published on: September 21, 2019
7.3K
07:41A Kinetic Fluorescence-based Ca2+ Mobilization Assay to Identify G Protein-coupled Receptor Agonists, Antagonists, and Allosteric Modulators
Published on: February 20, 2018
8.9K
相关概念视频
Chemotherapy-Induced Nausea and Vomiting: Cannabinoids
279
Tetrahydrocannabinol (THC) is a phytocannabinoid that primarily interacts with the CB1 receptor, a type of G protein-coupled receptor (GPCR) predominantly in and around the chemoreceptor trigger zone (CTZ) and emetic center. THC also blocks the serotonin receptor activity in the dorsal vagal complex (DVC) by inhibiting serotonin release. THC exerts its anti-emetic effects through these interactions, which are beneficial for patients undergoing chemotherapy.
Two synthetic agonists of THC,...
Two synthetic agonists of THC,...
279
CNS Stimulants: Cocaine, Amphetamines and Cannabinoids
197
CNS stimulants, such as cocaine, amphetamines, and cannabinoids, have varying structures and mechanisms of action that lead to different therapeutic effects and side effects. Cocaine, with its molecular formula C17H21NO4, is a tropane alkaloid and a tertiary amino compound. It has two chemical forms: the hydrochloride salt and the "freebase." The former is in powder form, while the latter involves removing the hydrochloride salt to create a form that can be smoked. Cocaine exerts its...
197
Carrier-Mediated Transport
436
Carrier-mediated transport is a pivotal process in drug absorption, particularly for lipid-insoluble drugs, and encompasses facilitated diffusion and active transport. Facilitated diffusion allows drugs to move along their concentration gradient without energy expenditure, while active transport utilizes ATP to drive drug movement against this gradient.
Active transport involves two types of membrane-spanning transporters: uptake and efflux. Uptake transporters are expressed in the small...
Active transport involves two types of membrane-spanning transporters: uptake and efflux. Uptake transporters are expressed in the small...
436
The Two-State Receptor Model
1.9K
The two-state receptor model explains a drug's interaction with receptors, such as G protein-coupled receptors and ligand-gated ion channels, to induce or inhibit a biological response. When no natural ligands are present, a receptor exists in an equilibrium of inactive (Ri) and active (Ra) conformations. The inactive form does not produce a response, while the active form generates a basal effect known as constitutive activity.
The binding affinity of a drug determines its interaction with...
The binding affinity of a drug determines its interaction with...
1.9K
Opioid Receptors: Overview
847
Opioid receptors, including the mu (μ, MOR), delta (δ, DOR), and kappa (κ, KOR) types, belong to the rhodopsin family of G protein-coupled receptors. These receptors are located throughout the central and peripheral nervous systems and in non-neuronal tissues such as macrophages and astrocytes. Opioid receptor ligands can be categorized into agonists or antagonists. Highly selective agonists include [d-Ala2, MePhe4, Gly(ol)5]-enkephalin or DAMGO for MOR, [D-Pen2,...
847
Ligand-Gated Ion Channel Receptor: Gating Mechanism
2.2K
Ligand-gated ion channels are transmembrane proteins that play a vital role in intercellular communication and functions of the nervous system. They allow the influx of ions across the membrane once the neurotransmitter binds, allowing the subsequent transmission of electrical excitation across the neurons. Other ligand-gated ion channels, like the γ-aminobutyric acid (GABA) receptor, permit anions like chloride into the cells on the binding of the GABA molecule. Their entry into the cell...
2.2K
