title: CPP, a new potent and selective NMDA antagonist. Depression of central neuron responses, affinity for [3H]D-AP5 binding sites on brain membranes and anticonvulsant activity.
abstract: Properties of a new potent antagonist acting selectively at N-methyl-D-aspartate (NMDA) type excitatory amino acid receptors are described. This compound, 3-((+/-)-2-carboxypiperazin-4-yl)propyl-1-phosphonic acid (CPP) is more potent than all previously reported NMDA antagonists in depressing mammalian spinal neuronal responses (cat and immature rat), in its affinity for [3H]D-AP5 (a radiolabelled NMDA antagonist) binding sites on rat brain membranes, and as an anticonvulsant in mice.
mesh_terms: D015763:2-Amino-5-phosphonovalerate; D000818:Animals; D000927:Anticonvulsants; D001224:Aspartic Acid / Q000031:analogs & derivatives* / Q000037:antagonists & inhibitors; D001665:Binding Sites; D001921:Brain / Q000187:drug effects / Q000378:metabolism / Q000502:physiology*; D002415:Cats; D002462:Cell Membrane / Q000378:metabolism; D007395:Interneurons / Q000502:physiology; D008564:Membrane Potentials / Q000187:drug effects; D051379:Mice; D009046:Motor Neurons / Q000502:physiology; D016202:N-Methylaspartate; D009474:Neurons / Q000187:drug effects / Q000502:physiology*; D010879:Piperazines / Q000494:pharmacology*; D051381:Rats; D013116:Spinal Cord / Q000187:drug effects / Q000502:physiology*; D014633:Valine / Q000031:analogs & derivatives* / Q000378:metabolism
chemical_list: D000927:Anticonvulsants; D010879:Piperazines; D001224:Aspartic Acid; D016202:N-Methylaspartate; D015763:2-Amino-5-phosphonovalerate; C050592:3-(2-carboxypiperazin-4-yl)propyl-1-phosphonic acid; D014633:Valine