GRC-6211
Chemical compound
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Formula | C22H20FN3O2 |
Molar mass | 377.419 g·mol−1 |
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GRC-6211 is a drug developed by Glenmark Pharmaceuticals which acts as a potent and selective antagonist for the TRPV1 receptor. It has analgesic and antiinflammatory effects and reached Phase IIb human trials, but was ultimately discontinued from development as a medicine, though it continues to have applications in scientific research.[1][2][3]
References
- ^ Charrua A, Cruz CD, Narayanan S, Gharat L, Gullapalli S, Cruz F, Avelino A (January 2009). "GRC-6211, a new oral specific TRPV1 antagonist, decreases bladder overactivity and noxious bladder input in cystitis animal models". The Journal of Urology. 181 (1): 379–86. doi:10.1016/j.juro.2008.08.121. PMID 19010489.
- ^ Kym PR, Kort ME, Hutchins CW (August 2009). "Analgesic potential of TRPV1 antagonists". Biochemical Pharmacology. 78 (3): 211–6. doi:10.1016/j.bcp.2009.02.014. PMID 19481638.
- ^ Santos-Silva A, Charrua A, Cruz CD, Gharat L, Avelino A, Cruz F (January 2012). "Rat detrusor overactivity induced by chronic spinalization can be abolished by a transient receptor potential vanilloid 1 (TRPV1) antagonist". Autonomic Neuroscience. 166 (1–2): 35–8. doi:10.1016/j.autneu.2011.09.005. PMID 22037502. S2CID 7146812.
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TRP channel modulators
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See also: Receptor/signaling modulators • Ion channel modulators
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