From Wikipedia, the free encyclopedia
Chemical compound
GRC-6211
1-[(4R)-6-fluorospiro[3,4-dihydrochromene-2,1'-cyclobutane]-4-yl]-3-isoquinolin-5-ylurea
CAS Number
PubChem
CID
ChemSpider
UNII
Formula C 22 H 20 F N 3 O 2
Molar mass 377.419 g·mol−1 3D model (
JSmol )
C1CC2(C1)C[C@H](C3=C(O2)C=CC(=C3)F)NC(=O)NC4=CC=CC5=C4C=CN=C5
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 .
TRPA
Activators
4-Hydroxynonenal
4-Oxo-2-nonenal
4,5-EET
12S-HpETE
15-Deoxy-Δ12,14 -prostaglandin J2
α-Sanshool (
ginger ,
Sichuan and
melegueta peppers )
Acrolein
Allicin (
garlic )
Allyl isothiocyanate (
mustard ,
radish ,
horseradish ,
wasabi )
AM404
ASP-7663
Bradykinin
Cannabichromene (
cannabis )
Cannabidiol (
cannabis )
Cannabigerol (
cannabis )
Cinnamaldehyde (
cinnamon )
CR gas (dibenzoxazepine; DBO)
CS gas (2-chlorobenzal malononitrile)
Cuminaldehyde (
cumin )
Curcumin (
turmeric )
Dehydroligustilide (
celery )
Diallyl disulfide
Dicentrine (
Lindera spp.)
Farnesyl thiosalicylic acid
Formalin
Gingerols (
ginger )
Hepoxilin A3
Hepoxilin B3
Hydrogen peroxide
Icilin
Isothiocyanate
JT-010
Ligustilide (
celery ,
Angelica acutiloba )
Linalool (
Sichuan pepper ,
thyme )
Methylglyoxal
Methyl salicylate (
wintergreen )
N-Methylmaleimide
Nicotine (
tobacco )
Oleocanthal (
olive oil )
Paclitaxel (
Pacific yew )
Paracetamol (acetaminophen)
PF-4840154
Phenacyl chloride
Polygodial (
Dorrigo pepper )
Shogaols (
ginger ,
Sichuan and
melegueta peppers )
Tear gases
Tetrahydrocannabinol (
cannabis )
Tetrahydrocannabiorcol
Thiopropanal S-oxide (
onion )
Umbellulone (Umbellularia californica )
WIN 55,212-2
Blockers
TRPC
TRPM
TRPML
TRPP
TRPV
Activators
2-APB
5',6'-EET
9-HODE
9-oxoODE
12S-HETE
12S-HpETE
13-HODE
13-oxoODE
20-HETE
α-Sanshool (
ginger ,
Sichuan and
melegueta peppers )
Allicin (
garlic )
AM404
Anandamide
Bisandrographolide (
Andrographis paniculata )
Camphor (
camphor laurel ,
rosemary ,
camphorweed ,
African blue basil ,
camphor basil )
Cannabidiol (
cannabis )
Cannabidivarin (
cannabis )
Capsaicin (
chili pepper )
Carvacrol (
oregano ,
thyme ,
pepperwort ,
wild bergamot , others)
DHEA
Diacyl glycerol
Dihydrocapsaicin (
chili pepper )
Estradiol
Eugenol (
basil ,
clove )
Evodiamine (
Euodia ruticarpa )
Gingerols (
ginger )
GSK1016790A
Heat
Hepoxilin A3
Hepoxilin B3
Homocapsaicin (
chili pepper )
Homodihydrocapsaicin (
chili pepper )
Incensole (
incense )
Lysophosphatidic acid
Low
pH (acidic conditions)
Menthol (
mint )
N-Arachidonoyl dopamine
N-Oleoyldopamine
N-Oleoylethanolamide
Nonivamide (PAVA) (
PAVA spray )
Nordihydrocapsaicin (
chili pepper )
Paclitaxel (
Pacific yew )
Paracetamol (acetaminophen)
Phenylacetylrinvanil
Phorbol esters (e.g.,
4α-PDD )
Piperine (
black pepper ,
long pepper )
Polygodial (
Dorrigo pepper )
Probenecid
Protons
RhTx
Rutamarin (
Ruta graveolens )
Resiniferatoxin (RTX) (
Euphorbia resinifera /
pooissonii )
Shogaols (
ginger ,
Sichuan and
melegueta peppers )
Tetrahydrocannabivarin (
cannabis )
Thymol (
thyme ,
oregano )
Tinyatoxin (
Euphorbia resinifera /
pooissonii )
Tramadol
Vanillin (
vanilla )
Zucapsaicin
Blockers