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GRC-6211

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Chemical compound

Pharmaceutical compound

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
PubChemCID	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 byGlenmark Pharmaceuticals which acts as a potent and selectiveantagonist for theTRPV1 receptor. It hasanalgesic andantiinflammatory effects and reachedPhase 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

[edit]

^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.

TRP channel modulators

TRPA

Activators

Blockers

TRPC

Activators	Adhyperforin (St John's wort) Diacyl glycerol GSK1702934A Hyperforin (St John's wort) Substance P
Blockers	DCDPC DHEA-S Flufenamic acid GSK417651A GSK2293017A Meclofenamic acid N-(p-Amylcinnamoyl)anthranilic acid Niflumic acid Pregnenolone sulfate Progesterone Pyr3 Tolfenamic acid

TRPM

Activators	ADP-ribose BCTC Calcium (intracellular) CIM-0216 Cold Coolact P Cooling Agent 10 Eucalyptol (eucalyptus) Frescolat MGA Frescolat ML Geraniol Hydroxycitronellal Icilin Linalool Menthol (mint) PMD 38 Pregnenolone sulfate Rutamarin (Ruta graveolens) Steviol glycosides (e.g.,stevioside) (Stevia rebaudiana) Sweettastants (e.g.,glucose,fructose,sucrose; indirectly) Thio-BCTC WS-12
Blockers	AMG-333 Capsazepine Clotrimazole DCDPC Elismetrep Flufenamic acid Meclofenamic acid Mefenamic acid N-(p-Amylcinnamoyl)anthranilic acid Nicotine (tobacco) Niflumic acid Ononetin PF-05105679 RQ-00203078 Ruthenium red Rutamarin (Ruta graveolens) Tolfenamic acid TPPO TRPM4-IN-5