GSK1016790A (GSK101, GSK-101)是瞬时受体电位香草酸4 (TRPV4)通道选择性激活剂。TRPV4是一种Ca²⁺可渗透的非选择性阳离子通道，参与多种生理功能，如全身渗透压调节、血管功能、皮肤屏障功能、气道和肺功能以及疼痛。GSK1016790A诱导Ca²⁺流入外源表达人或小鼠TRPV4蛋白的HEK细胞中，IC₅₀为2.1和18 nM。

参考文献

1.Kevin S Thorneloe, et al. N-((1S)-1-{[4-((2S)-2-{[(2,4-dichlorophenyl)sulfonyl]amino}-3-hydroxypropanoyl)-1-piperazinyl]carbonyl}-3-methylbutyl)-1-benzothiophene-2-carboxamide (GSK1016790A), a novel and potent transient receptor potential vanilloid 4 channel agonist induces urinary bladder contraction and hyperactivity: Part I. J Pharmacol Exp Ther. 2008 Aug;326(2):432-42.

2.J Fichna, et al. Transient receptor potential vanilloid 4 inhibits mouse colonic motility by activating NO-dependent enteric neurotransmission. J Mol Med (Berl). 2015 Dec;93(12):1297-309.

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