153501-26-9Relevant academic research and scientific papers
Synthesis and biological activities of novel aryl indole-2-carboxylic acid analogs as PPARγ partial agonists
Dropinski, James F.,Akiyama, Taro,Einstein, Monica,Habulihaz, Bahanu,Doebber, Tom,Berger, Joel P.,Meinke, Peter T.,Shi, Guo Q.
, p. 5035 - 5038 (2007/10/03)
A series of novel aryl indole-2-carboxylic acids has been identified as potent selective PPARγ modulators. Their chemical synthesis and in vitro activities are discussed. Compound 5 was selected for in vivo testing in the db/db mouse model of type 2 diabetes and resulted in reduction of hyperglycemia at comparable plasma exposure when compared to rosiglitazone.
Synthesis, pharmacology and therapeutic potential of 10-methoxypyrazinoindoles, partial agonists at the 5HT2C receptor
Boes, M.,Jenck, F.,Martin, J. R.,Moreau, J. L.,Mutel, V.,et al.
, p. 253 - 262 (2007/10/03)
A series of new 10-methoxypyrazinoindoles has been prepared and shown to be 5HT2C receptor ligands.The studied compounds 10a-j were found to act as partial agonists at the 5HT2C receptor, binding with high affinity and moderate selectivity versus 5HT1A and 5HT2A receptors, but inducing only a submaximal increase in phosphonoinositol formation.Compound 10j was demonstrated to be active in animal models of obsessive-compulsive disorder, depression and panic anxiety. - Keywords: pyrazinoindole; serotonin; 5HT2C receptor; partial agonist; psychiatric disorder.
