SB-705498
SB-705498 is a drug which acts as a potent and selective blocker of the TRPV1 ion channel.[1][2] It has been evaluated in clinical trials for the treatment of rhinitis and chronic cough.[3][4][5]
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Formula | C17H16BrF3N4O |
Molar mass | 429.241 g·mol−1 |
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References
- Rami HK, Thompson M, Stemp G, Fell S, Jerman JC, Stevens AJ, et al. (June 2006). "Discovery of SB-705498: a potent, selective and orally bioavailable TRPV1 antagonist suitable for clinical development". Bioorganic & Medicinal Chemistry Letters. 16 (12): 3287–91. doi:10.1016/j.bmcl.2006.03.030. PMID 16580202.
- Gunthorpe MJ, Hannan SL, Smart D, Jerman JC, Arpino S, Smith GD, et al. (June 2007). "Characterization of SB-705498, a potent and selective vanilloid receptor-1 (VR1/TRPV1) antagonist that inhibits the capsaicin-, acid-, and heat-mediated activation of the receptor". The Journal of Pharmacology and Experimental Therapeutics. 321 (3): 1183–92. doi:10.1124/jpet.106.116657. PMID 17392405. S2CID 6957155.
- Wong GY, Gavva NR (April 2009). "Therapeutic potential of vanilloid receptor TRPV1 agonists and antagonists as analgesics: Recent advances and setbacks". Brain Research Reviews. 60 (1): 267–77. doi:10.1016/j.brainresrev.2008.12.006. PMID 19150372. S2CID 9951052.
- Bareille P, Murdoch RD, Denyer J, Bentley J, Smart K, Yarnall K, et al. (July 2013). "The effects of a TRPV1 antagonist, SB-705498, in the treatment of seasonal allergic rhinitis". International Journal of Clinical Pharmacology and Therapeutics. 51 (7): 576–84. doi:10.5414/CP201890. PMID 23735181.
- Holland C, van Drunen C, Denyer J, Smart K, Segboer C, Terreehorst I, et al. (May 2014). "Inhibition of capsaicin-driven nasal hyper-reactivity by SB-705498, a TRPV1 antagonist". British Journal of Clinical Pharmacology. 77 (5): 777–88. doi:10.1111/bcp.12219. PMC 4004398. PMID 23909699.
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