gw-842166x has been researched along with Pain* in 3 studies
3 other study(ies) available for gw-842166x and Pain
| Article | Year |
|---|---|
Pyridine-3-carboxamides as novel CB(2) agonists for analgesia.
We describe herein the medicinal chemistry approach which led to the discovery of a novel pyridine-3-carboxamide series of CB(2) receptor agonists. The SAR of this new template was evaluated and culminated in the identification of analogue 14a which demonstrated efficacy in an in vivo model of inflammatory pain. Topics: Amides; Analgesia; Analgesics; Animals; Disease Models, Animal; Drug Discovery; Inflammation; Pain; Pyridines; Receptor, Cannabinoid, CB2; Structure-Activity Relationship | 2009 |
Discovery of 1-[4-(3-chlorophenylamino)-1-methyl-1H-pyrrolo[3,2-c]pyridin-7-yl]-1-morpholin-4-ylmethanone (GSK554418A), a brain penetrant 5-azaindole CB2 agonist for the treatment of chronic pain.
We report the synthesis and SAR of a series of novel azaindole CB(2) agonists. 6-Azaindole 18 showed activity in an acute pain model but was inactive in a chronic model. 18 is a Pgp substrate with low brain penetration. The template was redesigned, and the resulting 5-azaindole 36 was a potent CB(2) agonist with high CNS penetration. This compound was efficacious in the acute model and the chronic joint pain model. Topics: Aminopyridines; Animals; Aza Compounds; Brain; Cell Line; CHO Cells; Chronic Disease; Cricetinae; Cricetulus; Drug Discovery; Humans; Indoles; Morpholines; Pain; Rats; Receptor, Cannabinoid, CB2; Structure-Activity Relationship | 2009 |
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.
Selective CB2 receptor agonists are promising potential therapeutic agents for the treatment of inflammatory and neuropathic pain. A focused screen identified a pyrimidine ester as a partial agonist at the CB2 receptor with micromolar potency. Subsequent lead optimization identified 35, GW842166X, as the optimal compound in the series. 35 has an oral ED50 of 0.1 mg/kg in the rat FCA model of inflammatory pain and was selected as a clinical candidate for this indication. Topics: Analgesics; Animals; Biological Availability; Half-Life; Humans; Inflammation; Pain; Pyrans; Pyrimidines; Rats; Receptor, Cannabinoid, CB2; Structure-Activity Relationship | 2007 |