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
作者： J. Davies , R.H. Evans , P.L. Herrling , A.W. Jones , H.J. Olverman
DOI: 10.1016/0006-8993(86)90127-7
关键词: Anticonvulsant 、 Excitatory postsynaptic potential 、 Antagonist 、 NMDA receptor 、 Amino acid 、 2-Amino-5-phosphonovalerate 、 Chemistry 、 Biochemistry 、 Receptor 、 Pharmacology 、 Binding site 、 Developmental biology 、 General Neuroscience 、 Molecular biology 、 Clinical neurology
摘要: 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 (CPP) is more than all previously reported NMDA antagonists in depressing mammalian spinal neuronal responses (cat and immature rat), its affinity for [3H]D-AP5 (a radiolabelled antagonist) binding sites on rat brain membranes, as an anticonvulsant mice.
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sci-hub.se 参考文章(18)
J. Davies, R. H. Evans, A. W. Jones, K. N. Mewett, D. A. S. Smith, J. C. Watkins, Recent Advances in the Pharmacology of Excitatory Amino Acids in the Mammalian Central Nervous System Excitotoxins. pp. 43- 54 ,(1983) , 10.1007/978-1-349-06963-7_4
M.N. Perkins, T.W. Stone, J.F. Collins, K. Curry, Phosphonate analogues of carboxylic acids as aminoacid antagonists on rat cortical neurones. Neuroscience Letters. ,vol. 23, pp. 333- 336 ,(1981) , 10.1016/0304-3940(81)90021-5
M.N. Ferkins, J.F. Collins, T.W. Stone, Isomers of 2-amino-7-phosphonoheptanoic acid as antagonists of neuronal excitants. Neuroscience Letters. ,vol. 32, pp. 65- 68 ,(1982) , 10.1016/0304-3940(82)90230-0
Eric W. Harris, Alan H. Ganong, Daniel T. Monaghan, Jeffrey C. Watkins, Carl W. Cotman, Action of 3-((±)-2-car☐ypiperazin-4-yl)-propyl-1-phosphonic aci (CPP): a new and highly potent antagonist of N-methyl-d-aspartate receptors in the hippocampus Brain Research. ,vol. 382, pp. 174- 177 ,(1986) , 10.1016/0006-8993(86)90128-9
R.H. EVANS, A.A. FRANCIS, A.W. JONES, D.A.S. SMITH, J.C. WATKINS, THE EFFECTS OF A SERIES OF ω‐PHOSPHONIC α‐CARBOXYLIC AMINO ACIDS ON ELECTRICALLY EVOKED AND EXCITANT AMINO ACID‐INDUCED RESPONSES IN ISOLATED SPINAL CORD PREPARATIONS British Journal of Pharmacology. ,vol. 75, pp. 65- 75 ,(1982) , 10.1111/J.1476-5381.1982.TB08758.X
J. Davies, A.A. Francis, A.W. Jones, J.C. Watkins, 2-Amino-5-phosphonovalerate (2APV), a potent and selective antagonist of amino acid-induced and synaptic excitation Neuroscience Letters. ,vol. 21, pp. 77- 81 ,(1981) , 10.1016/0304-3940(81)90061-6
Lechoslaw Turski, Michael Schwarz, Waldemar A. Turski, Thomas Klockgether, Karl-Heinz Sontag, James F. Collins, Muscle relaxant action of excitatory amino acid antagonists Neuroscience Letters. ,vol. 53, pp. 321- 326 ,(1985) , 10.1016/0304-3940(85)90558-0
H. McLennan, Receptors for the excitatory amino acids in the mammalian central nervous system Progress in Neurobiology. ,vol. 20, pp. 251- 271 ,(1983) , 10.1016/0301-0082(83)90004-7
J. Davies, J.C. Watkins, Role of excitatory amino acid receptors in mono- and polysynaptic excitation in the cat spinal cord Experimental Brain Research. ,vol. 49, pp. 280- 290 ,(1983) , 10.1007/BF00238587
J. Davies, J.C. Watkins, Actions of D and L forms of 2-amino-5-phosphonovalerate and 2-amino-4-phosphonobutyrate in the cat spinal cord Brain Research. ,vol. 235, pp. 378- 386 ,(1982) , 10.1016/0006-8993(82)91017-4