GRC-6211

GRC-6211
Identifiers
	IUPAC name 1-[(4R)-6-fluorospiro[3,4-dihydrochromene-2,1'-cyclobutane]-4-yl]-3-isoquinolin-5-ylurea;
CAS Number	1166398-35-1;
PubChem CID	138393987;
ChemSpider	81367687;
UNII	4S841S9BO9;
Chemical and physical data
Formula	C22H20FN3O2
Molar mass	377.419 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES C1CC2(C1)C[C@H](C3=C(O2)C=CC(=C3)F)NC(=O)NC4=CC=CC5=C4C=CN=C5;
	InChI InChI=1S/C22H20FN3O2/c23-15-5-6-20-17(11-15)19(12-22(28-20)8-2-9-22)26-21(27)25-18-4-1-3-14-13-24-10-7-16(14)18/h1,3-7,10-11,13,19H,2,8-9,12H2,(H2,25,26,27)/t19-/m1/s1; Key:JADKHWDNSKIILG-LJQANCHMSA-N;

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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[1] 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.

[2] 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.

[3] 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.