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Cyclic benzamidines as orally efficacious NR2B-selective NMDA receptor antagonists |
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| Authors: | Nguyen Kevin T Claiborne Christopher F McCauley John A Libby Brian E Claremon David A Bednar Rodney A Mosser Scott D Gaul Stanley L Connolly Thomas M Condra Cindra L Bednar Bohumil Stump Gary L Lynch Joseph J Koblan Kenneth S Liverton Nigel J |
| Affiliation: | Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA. kevin_nguyen@merck.com |
| Abstract: | A novel series of cyclic benzamidines was synthesized and shown to exhibit NR2B-subtype selective NMDA antagonist activity. Compound 29 is orally active in a carrageenan-induced rat hyperalgesia model of pain. |
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