PDF(Pubmed)
Abstract：
The large family of transient receptor potential (TRP) channels are integral membrane proteins that function as environmental sensors and act as ion channels after activation by mechanical (touch), physical (heat, pain), and chemical stimuli (pungent compounds such as capsaicin). Most TRP channels are localized in the plasma membrane of cells but some of them are localized in membranes of organelles and function as intracellular Ca2+-ion channels. TRP channels are involved in neurological disorders but their precise role(s) and relevance in these disorders are not clear. Endothelial cells of the blood-brain barrier (BBB) express TRP channels such as TRP vanilloid 1-4 and are involved in thermal detection by regulating BBB permeability. In neurological disorders, TRP channels in the BBB are responsible for edema formation in the brain. Therefore, drug design to modulate locally activity of TRP channels in the BBB is a hot topic. Today, the application of TRP channel antagonists against neurological disorders is still limited.
摘要：
瞬时受体电位（TRP）通道的大家族是完整的膜蛋白，充当环境传感器，并通过机械（触摸）激活后充当离子通道，物理(热，疼痛),和化学刺激（刺激性化合物，如辣椒素）。大多数TRP通道位于细胞质膜中，但其中一些位于细胞器膜中，并充当细胞内Ca2离子通道。TRP通道涉及神经障碍,但它们在这些障碍中的确切作用和相关性尚不清楚。血脑屏障（BBB）的内皮细胞表达TRP通道，例如TRP香草酸1-4，并通过调节BBB通透性参与热检测。在神经系统疾病中，BBB中的TRP通道负责脑水肿形成。因此,药物设计以调节BBB中TRP通道的局部活性是一个热门话题。今天,TRP通道拮抗剂对神经系统疾病的应用仍然有限。
