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ID: ALA1136591

Journal: Bioorg Med Chem Lett

Title: Novel N1-(benzyl)cinnamamidine derived NR2B subtype-selective NMDA receptor antagonists.

Authors: Curtis NR, Diggle HJ, Kulagowski JJ, London C, Grimwood S, Hutson PH, Murray F, Richards P, Macaulay A, Wafford KA.

Abstract: Novel (E)-N(1)-(benzyl)cinnamamidines were prepared and evaluated as NR2B subtype NMDA receptor ligands. Excellent affinity was achieved by appropriate substitution of either phenyl ring. The 2-methoxybenzyl compound 1h had approximately 1,000-fold lower IC(50) in NR2B than NR2A-containing cells. Replacement of the styryl unit by 2-naphthyl was well tolerated.

CiteXplore: 12639560

DOI: 10.1016/s0960-894x(02)01060-0