title: Orally efficacious NR2B-selective NMDA receptor antagonists.
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.
authors.affiliation: Department of Medicinal Chemistry, Merck Research Laboratories, West Point, PA 19486, USA.
authors.forename: Christopher F
authors.initials: CF
authors.lastname: Claiborne
authors.forename: John A
authors.initials: JA
authors.lastname: McCauley
authors.forename: Brian E
authors.initials: BE
authors.lastname: Libby
authors.forename: Neil R
authors.initials: NR
authors.lastname: Curtis
authors.forename: Helen J
authors.initials: HJ
authors.lastname: Diggle
authors.forename: Janusz J
authors.initials: JJ
authors.lastname: Kulagowski
authors.forename: Stuart R
authors.initials: SR
authors.lastname: Michelson
authors.forename: Kenneth D
authors.initials: KD
authors.lastname: Anderson
authors.forename: David A
authors.initials: DA
authors.lastname: Claremon
authors.forename: Roger M
authors.initials: RM
authors.lastname: Freidinger
authors.forename: Rodney A
authors.initials: RA
authors.lastname: Bednar
authors.forename: Scott D
authors.initials: SD
authors.lastname: Mosser
authors.forename: Stanley L
authors.initials: SL
authors.lastname: Gaul
authors.forename: Thomas M
authors.initials: TM
authors.lastname: Connolly
authors.forename: Cindra L
authors.initials: CL
authors.lastname: Condra
authors.forename: Bohumil
authors.initials: B
authors.lastname: Bednar
authors.forename: Gary L
authors.initials: GL
authors.lastname: Stump
authors.forename: Joseph J
authors.initials: JJ
authors.lastname: Lynch
authors.forename: Alison
authors.initials: A
authors.lastname: Macaulay
authors.forename: Keith A
authors.initials: KA
authors.lastname: Wafford
authors.forename: Kenneth S
authors.initials: KS
authors.lastname: Koblan
authors.forename: Nigel J
authors.initials: NJ
authors.lastname: Liverton
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001550:Benzamidines / Q000138:chemical synthesis / Q000494:pharmacology*; D002351:Carrageenan; D004353:Drug Evaluation, Preclinical; D006930:Hyperalgesia / Q000188:drug therapy; D010146:Pain / Q000188:drug therapy; D011597:Psychomotor Performance / Q000187:drug effects; D051381:Rats; D016194:Receptors, N-Methyl-D-Aspartate / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
chemical_list: D001550:Benzamidines; C121001:NR2B NMDA receptor; D016194:Receptors, N-Methyl-D-Aspartate; D002351:Carrageenan