Richter, H. G. and Freichel, C. and Huwyler, J. and Nakagawa, T. and Nettekoven, M. and Plancher, J. M. and Raab, S. and Roche, O. and Schuler, F. and Taylor, S. and Ullmer, C. and Wiegand, R.. (2010) Discovery of potent and selective histamine H3 receptor inverse agonists based on the 3,4-dihydro-2H-pyrazino[1,2-a]indol-1-one scaffold. Bioorganic & medicinal chemistry letters, Vol. 20, H. 19. pp. 5713-5717.
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Official URL: http://edoc.unibas.ch/dok/A5840961
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Abstract
A novel series of potent histamine H(3) receptor inverse agonists based on the 3,4-dihydro-2H-pyrazino[1,2-a]indol-1-one scaffold has been discovered. Several compounds display high selectivity over other histamine receptor subtypes and have favorable physicochemical properties, low potential for CYP450 enzyme inhibition and high metabolic stability in microsomal preparations. (R)-2-Cyclopropylmethyl-8-(1-isopropyl-piperidin-4-yloxy)-3-methyl-3,4-dih ydro-2H-pyrazino[1,2-a]indol-1-one (8t) showed good in vivo efficacy after per os application in an acute rat dipsogenia model of water intake.
| Faculties and Departments: | 05 Faculty of Science > Departement Pharmazeutische Wissenschaften > Pharmazie > Pharmaceutical Technology (Huwyler) |
|---|---|
| UniBasel Contributors: | Huwyler, Jörg |
| Item Type: | Article, refereed |
| Article Subtype: | Research Article |
| Publisher: | Pergamon |
| ISSN: | 0960-894X |
| Note: | Publication type according to Uni Basel Research Database: Journal article |
| Last Modified: | 08 Jun 2012 06:56 |
| Deposited On: | 08 Jun 2012 06:51 |
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