Piperidyl amides as novel, potent and orally active mGlu5 receptor antagonists with anxiolytic-like activity
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Spanka, Carsten, Glatthar, Ralf, Desrayaud, Sandrine, Fendt, Markus, Orain, David, Troxler, Thomas J. and Vranesic, Ivan-Toma (2010) Piperidyl amides as novel, potent and orally active mGlu5 receptor antagonists with anxiolytic-like activity. Bioorganic & Medicinal Chemistry Letters, 20 (1). pp. 184-188. ISSN 0960-894X
Abstract
High throughput screening led to the identification of nicotinamide derivative 2 as a structurally novel mGluR5 antagonist. Optimization of the modular scaffold led to the discovery of 16m, a compound with high affinity for mGluR5 and excellent selectivity over other glutamate receptors. Compound 16m exhibits a favorable PK profile in rats, robust anxiolytic-like effects in three different animal models of fear and anxiety, as well as a good PK/PD correlation.
| Item Type: | Article |
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| Additional Information: | Author can archive post-print (ie final draft post-refereeing); Publisher's version/PDF cannot be used |
| Keywords: | Metabotropic glutamate receptor; mGluR5 antagonist; Piperidylamides |
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| Date Deposited: | 13 Oct 2015 13:17 |
| Last Modified: | 13 Oct 2015 13:17 |
| URI: | https://oak.novartis.com/id/eprint/1141 |