2023年5月9日 · To characterize the molecular details of eCB interaction with CB1, we utilized AMG315, an analog of the eCB anandamide to determine the structure of the AMG315-bound CB1 signaling complex.

最近，丹麦诺和诺德（Novo Nordisk）宣布计划以高达10.75亿美元的价格收购加拿大生物技术公司Inversago Pharma，以获取其基于CB1受体（CB1R）的创新疗法INV-202。 这项收购将进一步强化Novo Nordisk在减重领域的战略布局，该公司已拥有了一款强劲的靶向 GLP-1R 的减重药物Wegovy。 INV-202是一种口服CB1R拮抗剂，可以阻断CB1R的活化，从而减少食欲、降低体重、改善血糖和血脂等。 更加令人振奋的是，多款针对 CNR1 （CB1R/CB1）的药物在 肿瘤治疗 …

2023年5月9日 · Endocannabinoids (eCBs) are endogenous ligands of the cannabinoid receptor 1 (CB1), a G protein-coupled receptor that regulates a number of therapeutically relevant physiological responses. Hence, understanding the structural and functional consequences of eCB-CB1 interactions has important implicat …

2021年11月11日 · Here we developed a genetically encoded eCB sensor called GRAB eCB2.0. GRAB eCB2.0 consists of a circular-permutated EGFP and the human CB1 cannabinoid receptor, providing cell membrane...

内源性大麻素 (eCB) 是大麻素受体 1 (CB1) 的内源性配体，大麻素受体 1 是一种 G 蛋白偶联受体，可调节许多治疗相关的生理反应。 因此，了解 eCB-CB1 相互作用的结构和功能后果对于设计针对该受体的有效药物具有重要意义。 为了表征 eCB 与 CB1 相互作用的分子细节，我们利用 AMG315（eCB anandamide 的类似物）来确定 AMG315 结合的 CB1 信号复合物的结构。 与以前的结构相比，配体结合口袋显示出一些差异。 通过对接、分子动力学模拟和信号传导分析， …

2017年9月1日 · Despite the ever-growing complexity of the data and the constant addition of new players, most of what is known in the brain concerning the functions of the endocannabinoid (eCB) system (ECS)...

CB1 receptors are particularly enriched in the nervous system, but are also present in diverse organs including liver, adipose tissue, skin, etc. In adult CNS neurons, CB1 is most abundant on certain GABAergic interneurons [9].

2022年11月11日 · Endocannabinoids (eCBs) are bioactive lipids synthesized in the postsynaptic compartments to regulate synaptic transmission, plasticity, and neuronal excitability primarily through retrograde activation of presynaptic cannabinoid receptor type 1 (CB1). The eCB system is well situated to regulate neuronal network properties and coordinate ...

There is also ample evidence that altering eCB/CB1 signaling affects seizures and epilepsy in animal models, but the effects of experimental manipulations of this system have been mixed.

Endocannabinoids (eCBs) are bioactive lipids synthesized in the postsynaptic compartments to regulate synaptic transmission, plasticity, and neuronal excitability primarily through retrograde activation of presynaptic cannabinoid receptor type 1 (CB1). The eCB system is well situated to regulate neuronal network properties and coordinate ...