1287296-93-8Relevant articles and documents
Epiminocyclohepta[b]indole analogs as 5-HT6 antagonists
Henderson, Alan J.,Guzzo, Peter R.,Ghosh, Animesh,Kaur, Jagjit,Koo, Jia-Man,Nacro, Kassoum,Panduga, Shailaja,Pathak, Rashmi,Shimpukade, Bharat,Tan, Valentina,Xiang, Kai,Wierschke, Jonathan D.,Isherwood, Matthew L.
, p. 1494 - 1498 (2012)
A new series of epiminocyclohepta[b]indoles with potent 5-HT6 antagonist activity were discovered and optimized using in vitro protocols. One compound from this series was progressed to advanced pharmacokinetic (PK) studies followed by 5-HT6 receptor occupancy studies. The compound was found to have excellent oral absorption, a highly favorable PK profile and demonstrated pharmacodynamic interaction with the 5-HT6 receptor as shown by ex vivo autoradiography.
