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

• Published in: Brain research Vol. 382; no. 1; p. 169
• Main Authors: Davies, J, Evans, R H, Herrling, P L, Jones, A W, Olverman, H J, Pook, P, Watkins, J C
• Format: Journal Article
• Language: English
• Published: Netherlands 10.09.1986
• Subjects: 2-Amino-5-phosphonovalerate; Animals; Anticonvulsants; Aspartic Acid - analogs & derivatives; Aspartic Acid - antagonists & inhibitors; Binding Sites; Brain - drug effects; Brain - metabolism; Brain - physiology; Cats; Cell Membrane - metabolism; Interneurons - physiology; Membrane Potentials - drug effects; Mice; Motor Neurons - physiology; N-Methylaspartate; Neurons - drug effects; Neurons - physiology; Piperazines - pharmacology; Rats; Spinal Cord - drug effects; Spinal Cord - physiology; Valine - analogs & derivatives; Valine - metabolism
• ISSN: 0006-8993
• DOI: 10.1016/0006-8993(86)90127-7

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.