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

  title={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},
  author={Kevin S. Thorneloe and Anthony C. Sulpizio and Zuojun Lin and David J. Figueroa and Angela K Clouse and Gerald P McCafferty and Tim P Chendrimada and Erin S. R. Lashinger and Earl Gordon and Louise Evans and Blake A Misajet and Douglas J Demarini and Josephine H L Nation and Linda N Casillas and Robert W. Marquis and Bartholomew J Votta and Steven A Sheardown and Xiaoping Xu and David P. Brooks and Nicholas J. Laping and Timothy D. Westfall},
  journal={The Journal of pharmacology and experimental therapeutics},
  volume={326 2},
The transient receptor potential (TRP) vanilloid 4 (TRPV4) member of the TRP superfamily has recently been implicated in numerous physiological processes. In this study, we describe a small molecule TRPV4 channel activator, (N-((1S)-1-{[4-((2S)-2-{[(2,4-dichlorophenyl)sulfonyl]amino}-3-hydroxypropanoyl)-1-piperazinyl]carbonyl}-3-methylbutyl)-1-benzothiophene-2-carboxamide (GSK1016790A), which we have used as a valuable tool in investigating the role of TRPV4 in the urinary bladder. GSK1016790A… CONTINUE READING
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