1. Signaling Pathways
  2. GPCR/G Protein
  3. GPR6

GPR6 (G蛋白偶联受体6)

G Protein-Coupled Receptor 6

GPR6 是一种孤儿 G 蛋白偶联受体,由于其识别大麻素配体的子集,因此与大麻素家族有关。GPR6 在人类纹状体和下丘脑中高度表达。GPR6 被认为是治疗几种神经退行性疾病的潜在靶点。实验证据表明,GPR6 的消耗会导致纹状体组织中的多巴胺增加和 cAMP 减少,同时伴有运动改善。在帕金森病小鼠模型中敲除 GPR6 会导致这种疾病特有的不自主运动减少。事实上,有几项专利声称使用吡嗪衍生物作为 GPR6 反向激动剂来治疗帕金森病症状和其他运动障碍综合征。GPR6 还与亨廷顿氏病和阿尔茨海默氏病等其他神经系统疾病有关。此外,在 GPR6 敲除小鼠模型中,工具学习已被证明受到损害。

GPR6 is an orphan G protein-coupled receptor that has been associated with the cannabinoid family because of its recognition of a sub-set of cannabinoid ligands. GPR6 is highly expressed in human striatum and hypothalamus. GPR6 has been suggested as a possible target for the treatment of several neurodegenerative diseases. Experimental evidence shows that depletion of GPR6 causes both dopamine increase and cAMP decrease in the striatal tissues which are accompanied by improved movement. Knockout of GPR6 in a Parkinson’s disease mice model results in a decrease of the involuntary movements that characterize this disease. In fact, several patents claim the use of pyrazine derivatives as GPR6 inverse agonists for treating Parkinson’s disease symptoms and other dyskinesia syndromes. GPR6 is also involved in other neurological disorders such as Huntington’s and Alzheimer’s Disease. Moreover, instrumental learning has been shown to be impaired in GPR6 knockout mice models.

GPR6 相关产品 (2):

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-134661A
    CVN424 99.70%
    CVN424 是一种具有口服活性和选择性的 GPR6 反向激动剂,Ki 为 9.4 nM,EC50 为 38 nM。CVN424 可以透过血脑屏障,具有用于帕金森病研究的潜力。
    CVN424
  • HY-134661
    (S)-CVN424 99.16%
    (S)-CVN424 是有效的 G 蛋白偶联受体 6 (GPR6) 调节剂。(S)-CVN424 具有用于潜在的多种神经和精神疾病,包括帕金森氏病的潜力。
    (S)-CVN424