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Orally Efficacious NR2B-Selective NMDA Receptor Antagonists

Authors :
Rodney A. Bednar
Roger M. Freidinger
John A. McCauley
Keith A. Wafford
David A. Claremon
Christopher F. Claiborne
Brian E. Libby
Stuart R. Michelson
Alison J. Macaulay
Nigel J. Liverton
Thomas M. Connolly
Bohumil Bednar
Kenneth S. Koblan
Stanley L. Gaul
Scott D. Mosser
Joseph J. Lynch
Cindra L. Condra
Gary L. Stump
Helen J. Diggle
Janusz Jozef Kulagowski
Kenneth D. Anderson
Neil Roy Curtis
Source :
Bioorganic & Medicinal Chemistry Letters. 13:697-700
Publication Year :
2003
Publisher :
Elsevier BV, 2003.

Abstract

A novel series of benzamidines was synthesized and shown to exhibit NR2B-subtype selective NMDA antagonist activity. Compound 31 is orally active in a carrageenan-induced rat hyperalgesia model of pain and shows no motor coordination side effects.

Details

ISSN :
0960894X
Volume :
13
Database :
OpenAIRE
Journal :
Bioorganic & Medicinal Chemistry Letters
Accession number :
edsair.doi.dedup.....dd299167537625261e03641a62d5a8a0
Full Text :
https://doi.org/10.1016/s0960-894x(02)01061-2