GW-842,166X explained

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related to pain management^{[3] [4]} and the other two related to bio-distributions.^{[5] [6]} The trials were either withdrawn or completed without posting result.

Notes and References

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 . 6 . 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 . 2597–2600 . May 2007 . 17477516 . 10.1021/jm061195+ .
2. Book: Han S, Thatte J, Jones RM . Chapter 11: Recent Advances in the Discovery of CB2 Selective Agonists . 10.1016/S0065-7743(09)04411-X . 44 . 227–246 . 2009 . Annual Reports in Medicinal Chemistry . 9780123747662 . registration .
3. Dose Response and Efficacy of GW842166 in Pain - Full Text View - ClinicalTrials.gov. clinicaltrials.gov. 12 February 2015. en. 2020-02-18.
4. Dental Pain 3rd Molar Tooth Extraction GW842166 - Full Text View - ClinicalTrials.gov. clinicaltrials.gov. 15 May 2009. en. 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. 12 February 2015. en. 2020-02-18.
6. An Imaging Study to Investigate the Distribution of GW842166X in the Brain. - Full Text View - ClinicalTrials.gov. clinicaltrials.gov. 3 August 2017. en. 2020-02-18.