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Epiminocyclohepta[b]indole analogs as 5-HT6 antagonists |
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| Authors: | 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 |
| Affiliation: | AMRI, 26 Corporate Circle, Albany, NY 12212-5098, USA. alan.henderson@amriglobal.com |
| Abstract: | A new series of epiminocyclohepta[b]indoles with potent 5-HT(6) 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-HT(6) receptor occupancy studies. The compound was found to have excellent oral absorption, a highly favorable PK profile and demonstrated pharmacodynamic interaction with the 5-HT(6) receptor as shown by ex vivo autoradiography. |
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