hu-210 and Chronic-Disease

hu-210 has been researched along with Chronic-Disease* in 1 studies

Other Studies

1 other study(ies) available for hu-210 and Chronic-Disease

Article	Year
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. Journal of medicinal chemistry, 2009, Oct-08, Volume: 52, Issue:19 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

Article

Year

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.

Journal of medicinal chemistry, 2009, Oct-08, Volume: 52, Issue:19

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