RetroSearch Browse

Home - News ( United States | United Kingdom | Italy | Germany ) - Football scores

Showing content from https://en.wikipedia.org/wiki/RQ-00203078 below:

RQ-00203078 - Wikipedia

From Wikipedia, the free encyclopedia

Chemical compound

Pharmaceutical compound

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]

^ 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.
^ 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.
^ 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.