|CompTox Dashboard (EPA)|
|Chemical and physical data|
|Molar mass||449.26 g·mol−1|
|3D model (JSmol)|
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. GSK brought this compound for into 4 clinical trials, two of them related to pain management and the other two related to bio-distributions. The trials were either withdrawn or completed without posting result.
- ^ 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.
- ^ Han, S.; Thatte, J.; Jones, R. M. (2009). Chapter 11: Recent Advances in the Discovery of CB2 Selective Agonists. Annual Reports in Medicinal Chemistry. Vol. 44. pp. 227–246. doi:10.1016/S0065-7743(09)04411-X. ISBN 9780123747662.
- ^ "Dose Response and Efficacy of GW842166 in Pain - Full Text View - ClinicalTrials.gov". clinicaltrials.gov. 12 February 2015. Retrieved 2020-02-18.
- ^ "Dental Pain 3rd Molar Tooth Extraction GW842166 - Full Text View - ClinicalTrials.gov". clinicaltrials.gov. 15 May 2009. Retrieved 2020-02-18.
- ^ "Relative Bioavailability Study on a Single Dose of GW842166X in Healthy Male and Female Subjects. - Full Text View - ClinicalTrials.gov". clinicaltrials.gov. 12 February 2015. Retrieved 2020-02-18.
- ^ "An Imaging Study to Investigate the Distribution of GW842166X in the Brain. - Full Text View - ClinicalTrials.gov". clinicaltrials.gov. 3 August 2017. Retrieved 2020-02-18.