title: The NMDA antagonists, CPP and CGS 19755, lack affinity for central benzodiazepine receptors.
abstract: CPP (3-(2-carboxypiperazin-4-yl-propyl-1-phosphonic acid), a rigid analog of AP7 (2-amino-7-phosphonoheptanoate), previously shown to be a selective antagonist of the NMDA (N-methyl-D-aspartate) receptor (IC50 = 209 nM) has been reported to be exceptionally active (IC50 = 430 pM) at benzodiazepine binding sites. Re-examination of CPP, and the rigid AP5 analog, CGS 19755 (cis-4-phosphonomethyl-2-piperidine carboxylic acid; 0.001-10,000 nM), showed that, as previously reported, neither compound affected the binding of [3H]flunitrazepam. These compounds are thus selective NMDA receptor antagonists.
authors.affiliation: Research Department, Ciba-Geigy Corporation, Summit, NJ 07901.
authors.forename: M
authors.initials: M
authors.lastname: Williams
authors.forename: P S
authors.initials: PS
authors.lastname: Loo
authors.forename: M A
authors.initials: MA
authors.lastname: Sills
mesh_terms: D000818:Animals; D000927:Anticonvulsants / Q000378:metabolism*; D001224:Aspartic Acid / Q000031:analogs & derivatives* / Q000037:antagonists & inhibitors; D001667:Binding, Competitive / Q000187:drug effects; D001921:Brain / Q000187:drug effects / Q000378:metabolism; D005445:Flunitrazepam / Q000378:metabolism; D066298:In Vitro Techniques; D016202:N-Methylaspartate; D010875:Pipecolic Acids; D010879:Piperazines / Q000378:metabolism*; D010880:Piperidines / Q000378:metabolism*; D051381:Rats; D011963:Receptors, GABA-A / Q000187:drug effects / Q000378:metabolism*
chemical_list: D000927:Anticonvulsants; D010875:Pipecolic Acids; D010879:Piperazines; D010880:Piperidines; D011963:Receptors, GABA-A; D001224:Aspartic Acid; C053672:selfotel; D005445:Flunitrazepam; D016202:N-Methylaspartate; C050592:3-(2-carboxypiperazin-4-yl)propyl-1-phosphonic acid