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PMID: 2876749 Published · ppublish English Journal Article Research Support, Non-U.S. Gov't

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.

Brain research ·Vol. 382 ·No. 1 ·1986-09-10 ·Pages 169-73

Davies J, Evans RH, Herrling PL, Jones AW, Olverman HJ, Pook P, Watkins JC

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
2-Amino-5-phosphonovalerate Animals Anticonvulsants Aspartic Acid/analogs & derivatives,antagonists & inhibitors Binding Sites Brain/drug effects,metabolism,physiology Cats Cell Membrane/metabolism Interneurons/physiology Membrane Potentials/drug effects Mice Motor Neurons/physiology N-Methylaspartate Neurons/drug effects,physiology Piperazines/pharmacology Rats Spinal Cord/drug effects,physiology Valine/analogs & derivatives,metabolism
Chemicals
Anticonvulsants Piperazines Aspartic Acid N-Methylaspartate 2-Amino-5-phosphonovalerate 3-(2-carboxypiperazin-4-yl)propyl-1-phosphonic acid Valine
Authors & Affiliations
7 authors, click to expand affiliations / ORCID
Davies J
Evans R H
Herrling P L
Jones A W
Olverman H J
Pook P
Watkins J C
Article Info
Journal
Brain research
Abbr.
Brain Res
ISSN
0006-8993
Published
1986-09-10
Pages
169-73
Language
English
Region
Netherlands
NLM ID
0045503
Subset
IM
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