GW-842,166X
GW842166X structure.png
Identifiers
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC18H17Cl2F3N4O2
Molar mass449.26 g·mol−1
3D model (JSmol)
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GW-842,166X is a drug which acts as a potent and selective cannabinoid CB2 receptor agonist, with a novel chemical structure based on a pyrimidine core. It has potent analgesic, anti-inflammatory and anti-hyperalgesic actions in animal models, but without cannabis-like behavioural effects due to its extremely low affinity for the CB1 receptor.[1][2] GSK brought this compound for into 4 clinical trials, two of them related to pain management[3][4] and the other two related to bio-distributions[5][6]. The trials were either withdrawn or completed without posting result.

References[edit]

  1. ^ Giblin GM, O'Shaughnessy CT, Naylor A, Mitchell WL, Eatherton AJ, Slingsby BP, Rawlings DA, Goldsmith P, Brown AJ, Haslam CP, Clayton NM, Wilson AW, Chessell IP, Wittington AR, Green R (May 2007). "Discovery of 2-[(2,4-dichlorophenyl)amino]-N-[(tetrahydro- 2H-pyran-4-yl)methyl]-4-(trifluoromethyl)- 5-pyrimidinecarboxamide, a selective CB2 receptor agonist for the treatment of inflammatory pain". Journal of Medicinal Chemistry. 50 (11): 2597–600. doi:10.1021/jm061195+. PMID 17477516.
  2. ^ Han, S.; Thatte, J.; Jones, R. M. (2009). "Chapter 11: Recent Advances in the Discovery of CB2 Selective Agonists". Annual Reports in Medicinal Chemistry. Annual Reports in Medicinal Chemistry. 44: 227. doi:10.1016/S0065-7743(09)04411-X. ISBN 9780123747662.
  3. ^ "Dose Response and Efficacy of GW842166 in Pain - Full Text View - ClinicalTrials.gov". clinicaltrials.gov. Retrieved 2020-02-18.
  4. ^ "Dental Pain 3rd Molar Tooth Extraction GW842166 - Full Text View - ClinicalTrials.gov". clinicaltrials.gov. Retrieved 2020-02-18.
  5. ^ "Relative Bioavailability Study on a Single Dose of GW842166X in Healthy Male and Female Subjects. - Full Text View - ClinicalTrials.gov". clinicaltrials.gov. Retrieved 2020-02-18.
  6. ^ "An Imaging Study to Investigate the Distribution of GW842166X in the Brain. - Full Text View - ClinicalTrials.gov". clinicaltrials.gov. Retrieved 2020-02-18.