Potent TRPV1 antagonist against capsaicin (pKb
= 7.7), noxious heat and acid-mediated (pIC50
= 7.0) receptor activation (pKi
= 6.22 at the recombinant hTRPV1 receptor). Exhibits analgesic properties.
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Discovery of small molecule antagonists of TRPV1.
Rami et al.
Conservation of functional and pharmacological properties in the distantly related temperature sensors TRPV1 and TRPM8.
Weil et al.
[3H]A-778317 [1-((R)-5-tert-Butyl-indan-1-yl)-3-isoquinolin-5-ylurea]: a novel, stereoselective, high-affinity antagonist is a useful radioligand for the human transient receptor potential vanilloid-1 (TRPV1) receptor.
Bianchi et al.
The citations listed below are publications that use Tocris products. Selected citations for SB 452533 include:
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