针对器官纤维化中的大麻素2型受体的药物的治疗潜力
Lujain Bader Eddin1, M F Nagoor Meeran1, Sandeep B Subramanya2
1Department of Pharmacology and Therapeutics, College of Medicine and Health Sciences, United Arab Emirates University, Al Ain, UAE.
Pharmacology research & perspectives
|October 19, 2024
概括
准2型大麻素受体 (CB2) 显示出治疗纤维化的前景. CB2激动剂可以抑制纤维化反应和炎症,提供治疗潜力,没有中枢神经系统的副作用.
科学领域:
- 药理学和毒理学 药理学和毒理学
- 细胞和分子生物学 细胞和分子生物学
- 病理生理学 病理生理学
背景情况:
- 内分泌系统,包括大麻素受体2型 (CB2),是各种疾病的潜在治疗点.
- CB2受体是参与细胞内信号通路的G蛋白合受体.
- 纤维化是一种涉及组织重塑的病理状况,越来越多地被认为受到CB2受体活性的影响.
研究的目的:
- 审查CB2激动剂在器官纤维化病理生理学中的作用.
- 综合自然和合成CB2激动剂治疗纤维化的实验证据.
- 突出调节心脏,肝脏和脏系统中的CB2受体的治疗潜力.
主要方法:
- 独立实验研究的综合综合.
- 对CB2激动剂的临床前数据的分析.
- 在器官纤维化模型中对CB2受体调节的研究的审查.
主要成果:
- CB2激动剂有效调节炎症和纤维生成.
- 激活CB2受体抑制了与转化生长因子β1.1相关的基因表达.
- CB2激动剂在各种组织中减轻慢性炎症和纤维化方面表现出有效性.
结论:
- 调节CB2受体为器官纤维化提供了一个有前途的治疗策略.
- CB2激动剂可能会提供益处,减少中枢神经系统的不良影响.
- 进一步开发CB2化合物对于纤维性疾病的药物发现是有必要的.
相关概念视频
Drugs for Treatment of Crohn's Disease in IBD Using Biologic Agents: Anti-TNF
117
Tumor Necrosis Factor (TNF), a proinflammatory cytokine, contributes significantly to the inflammation seen in Crohn's disease. It exists as soluble TNF and membrane-bound TNF, with actions mediated through TNF receptors (TNFR). TNFR activation leads to the release of proinflammatory cytokines, T-cell activation, collagen production, and leukocyte migration, all contributing to inflammation in Crohn's disease. Anti-TNF monoclonal antibodies, namely infliximab (Remicade), adalimumab...
117
Chemotherapy-Induced Nausea and Vomiting: Cannabinoids
202
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,...
202
Treatment for Pulmonary Arterial Hypertension: Prostacyclin Receptor Agonists
154
Prostacyclin receptor agonists are a class of therapeutic agents integral to managing pulmonary arterial hypertension (PAH). These drugs operate by mimicking the action of prostaglandin I2, or PGI2, a naturally occurring compound in the body.
These agonists bind to the IPR receptor situated on the plasma membrane of the pulmonary artery smooth muscle cells. This binding triggers a cascade of reactions known as the GS-AC-cAMP-PKA pathway. This pathway results in the relaxation of smooth muscle...
These agonists bind to the IPR receptor situated on the plasma membrane of the pulmonary artery smooth muscle cells. This binding triggers a cascade of reactions known as the GS-AC-cAMP-PKA pathway. This pathway results in the relaxation of smooth muscle...
154
Heart Failure Drugs: Inhibitors of Renin-Angiotensin System
394
The activation of the sympathetic nervous system and the renin-angiotensin-aldosterone system (RAAS) contributes to cardiac remodeling, and inhibiting the RAAS is a pharmacological target in heart failure management. As a result, neurohumoral modulation is a crucial treatment principle for managing heart failure. This approach involves using medications like ACE inhibitors (ACEIs), angiotensin receptor blockers (ARBs), β-blockers, mineralocorticoid receptor antagonists (MRAs), and neutral...
394
CNS Stimulants: Cocaine, Amphetamines and Cannabinoids
165
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...
165
Treatment for Pulmonary Arterial Hypertension: Endothelin Receptor Antagonists
136
Endothelins (ETs) are potent vasoactive peptides critical in the human body's various physiological and pathological processes. One of the most promising therapeutic strategies for treating pulmonary arterial hypertension (PAH) involves counteracting the effects of these endothelins using a class of drugs known as endothelin receptor antagonists.
ETs are synthesized through a complex sequence of enzymatic steps, primarily involving an enzyme referred to as endothelin-converting enzyme...
ETs are synthesized through a complex sequence of enzymatic steps, primarily involving an enzyme referred to as endothelin-converting enzyme...
136


