RQ-00203078
Chemical compound
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Formula | C21H13ClF6N2O5S |
Molar mass | 554.84 g·mol−1 |
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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]
See also
- AMG-333
- PF-05105679
References
- ^ 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.
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TRP channel modulators
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See also: Receptor/signaling modulators • Ion channel modulators
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