大麻烯对大麻素受体的选择性激活
Noa Raz1, Aharon M Eyal1, Nardine Fahoum-Khalefa1
1Bazelet Medical Cannabis Group, Or Akiva, Israel.
Biochemical pharmacology
|October 31, 2025
概括
大麻烯激活大麻素受体 (CB1R和CB2R),作为部分激动剂. 这项研究阐明了它们的分子机制和潜在的治疗应用.
科学领域:
- 药理学 药理学是指药理学的学科.
- 分子生物学分子生物学
- 大麻研究 大麻研究
背景情况:
- 烯是植物化合物,在大麻中丰富,具有药理作用的新兴证据.
- 烯的分子机制,特别是大麻制剂中的烯,尚不清楚.
- 之前的研究表明,某些烯激活大麻素受体1型 (CB1R).
研究的目的:
- 为了研究单个大麻烯和混合物激活大麻素受体2型 (CB2R) 的作用.
- 为了补充之前关于大麻烯CB1R激活的发现.
- 阐明了烯对大麻素受体作用的分子机制.
主要方法:
- 使用了一种Xenopus卵细胞功能异质表达系统.
- 通过受体诱导的GIRK电流测量受体激活.
- 对CB1R和CB2R激活进行了十六个单独的大麻烯和烯混合物的测试.
主要成果:
- 多种烯在CB1R和CB2R表现出剂量依赖的反应,THC的最大激活率为10-60%.
- 烯表现出与THC相似或较低的EC50值,表明具有相似或更高的强度但效率较低.
- 几种烯在CB2R中达到与THC (≥0.1μM) 相当或低于THC的度时达到"临床效应水平".
结论:
- 大麻烯作为CB1R和CB2R的部分激动剂起作用.
- 烯表现出不同的激活水平和对CB1R和CB2R的差异性影响,表明受体选择性.
- 这些发现为选择烯用于针对大麻素受体的治疗应用提供了基础.
相关概念视频
01:21Chemotherapy-Induced Nausea and Vomiting: Cannabinoids
658
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,...
658
01:24CNS Stimulants: Cocaine, Amphetamines and Cannabinoids
758
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...
758
01:09GPCRs Regulate Adenylyl Cylase Activity
7.3K
Some GPCRs transmit signals through adenylyl cyclase (AC), a transmembrane enzyme. AC helps synthesize second messenger cyclic adenosine monophosphate (cAMP). AC catalyzes cyclization reaction and converts ATP to cAMP by releasing a pyrophosphate. The pyrophosphate is further hydrolyzed to phosphate by the enzyme pyrophosphatase, which drives cAMP synthesis to completion. However, cAMP is rapidly degraded to 5′ AMP by the enzymes phosphodiesterase (PDE), preventing overstimulation of...
7.3K
01:12GPCR Desensitization
7.9K
G protein-coupled receptor (GPCR) signaling plays a crucial role in cell functioning. GPCR desensitization is an equally essential process. It allows cells to respond to changing environments and regain sensitivity to new stimuli while preventing unnecessary stimulation when no longer needed. Prolonged exposure to stimuli leads to GPCR desensitization. It involves blocking the receptors from binding and activating additional G proteins. This inhibits activation of downstream effectors, thereby...
7.9K
01:07MAPK Signaling Cascades
7.9K
Mitogen-activated protein kinase, or MAPK pathway, activates three sequential kinases to regulate cellular responses such as proliferation, differentiation, survival, and apoptosis. The canonical MAPK pathway starts with a mitogen or growth factor binding to an RTK. The activated RTKs stimulate Ras, which recruits Raf or MAP3 Kinase (MAPKKK), the first kinase of the MAPK signaling cascade. Raf further phosphorylates and activates MEK or MAP2 Kinases (MAPKK), which in turn phosphorylates MAP...
7.9K
01:22Opioid Receptors: Overview
4.0K
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,...
4.0K