Chemistry:GW-842,166X
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Short description: Chemical compound
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| Formula | C18H17Cl2F3N4O2 |
| Molar mass | 449.26 g·mol−1 |
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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of them related to pain management[3][4] and the other two related to bio-distributions.[5][6] The trials were either withdrawn or completed without posting result.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
- ↑ "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. doi:10.1021/jm061195+. PMID 17477516.
- ↑ Chapter 11: Recent Advances in the Discovery of CB2 Selective Agonists. Annual Reports in Medicinal Chemistry. 44. 2009. pp. 227–246. doi:10.1016/S0065-7743(09)04411-X. ISBN 9780123747662. https://archive.org/details/annualreportsinm0000unse_z9v8/page/227.
- ↑ (in en) Dose Response and Efficacy of GW842166 in Pain - Full Text View - ClinicalTrials.gov. 12 February 2015. https://clinicaltrials.gov/ct2/show/NCT00554762. Retrieved 2020-02-18.
- ↑ (in en) Dental Pain 3rd Molar Tooth Extraction GW842166 - Full Text View - ClinicalTrials.gov. 15 May 2009. https://clinicaltrials.gov/ct2/show/NCT00444769. Retrieved 2020-02-18.
- ↑ (in en) Relative Bioavailability Study on a Single Dose of GW842166X in Healthy Male and Female Subjects. - Full Text View - ClinicalTrials.gov. 12 February 2015. https://clinicaltrials.gov/ct2/show/NCT00536497. Retrieved 2020-02-18.
- ↑ (in en) An Imaging Study to Investigate the Distribution of GW842166X in the Brain. - Full Text View - ClinicalTrials.gov. 3 August 2017. https://clinicaltrials.gov/ct2/show/NCT00511524. Retrieved 2020-02-18.
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