RQ-00203078

RQ-00203078 is a drug which acts as a potent and selective blocker of the TRPM8 ion channel, which is the main receptor responsible for the sensation of cold. It was developed as a potential analgesic, and blocks the development of hyperalgesia following exposure to cold temperatures or chronic morphine administration.^[1][2][3]

RQ-00203078

Identifiers
IUPAC name 4-([3-chloro-5-(trifluoromethyl)pyridin-2-yl]-{[4-(trifluoromethoxy)phenyl]methyl}sulfamoyl)benzoic acid
CAS Number	1254205-52-1
PubChem CID	49783953
ChemSpider	34979854
ChEMBL	ChEMBL3353597
Chemical and physical data
Formula	C21H13ClF6N2O5S
Molar mass	554.84 g·mol−1
3D model (JSmol)	Interactive image
SMILES C1=CC(=CC=C1CN(C2=C(C=C(C=N2)C(F)(F)F)Cl)S(=O)(=O)C3=CC=C(C=C3)C(=O)O)OC(F)(F)F
InChI InChI=1S/C21H13ClF6N2O5S/c22-17-9-14(20(23,24)25)10-29-18(17)30(11-12-1-5-15(6-2-12)35-21(26,27)28)36(33,34)16-7-3-13(4-8-16)19(31)32/h1-10H,11H2,(H,31,32) Key:IJGQFZYYEHCCIZ-UHFFFAOYSA-N

See also

• AMG-333
• PF-05105679

References

1. Ohmi M, Shishido Y, Inoue T, Ando K, Fujiuchi A, Yamada A, et al. (December 2014). "Identification of a novel 2-pyridyl-benzensulfonamide derivative, RQ-00203078, as a selective and orally active TRPM8 antagonist". Bioorganic & Medicinal Chemistry Letters. 24 (23): 5364–8. doi:10.1016/j.bmcl.2014.10.074. PMID 25455182.
2. Gong K, Jasmin L (February 2017). "Sustained Morphine Administration Induces TRPM8-Dependent Cold Hyperalgesia". The Journal of Pain. 18 (2): 212–221. doi:10.1016/j.jpain.2016.10.015. PMC 5291755. PMID 27845197.
3. Thiel G, Backes TM, Welck J, Steinhausen S, Fischer AL, Langfermann DS, et al. (December 2019). "Pharmacological inhibition of TRPM8-induced gene transcription". Biochemical Pharmacology. 170: 113678. doi:10.1016/j.bcp.2019.113678. PMID 31654626. S2CID 204918567.