Chemistry:RQ-00203078

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Short description: Chemical compound
RQ-00203078
RQ-00203078 structure.png
Identifiers
CAS Number
PubChem CID
ChemSpider
ChEMBL
Chemical and physical data
FormulaC21H13ClF6N2O5S
Molar mass554.84 g·mol−1
3D model (JSmol)

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

References

  1. "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. December 2014. doi:10.1016/j.bmcl.2014.10.074. PMID 25455182. 
  2. "Sustained Morphine Administration Induces TRPM8-Dependent Cold Hyperalgesia". The Journal of Pain 18 (2): 212–221. February 2017. doi:10.1016/j.jpain.2016.10.015. PMID 27845197. 
  3. "Pharmacological inhibition of TRPM8-induced gene transcription". Biochemical Pharmacology 170: 113678. December 2019. doi:10.1016/j.bcp.2019.113678. PMID 31654626.