Equilibrium analysis of [3H]TCP binding: effects of glycine, magnesium and N-methyl-D-aspartate agonists.

作者: Kenneth M. Johnson , Aida I. Sacaan , Lawrence D. Snell

DOI: 10.1016/0014-2999(88)90845-X

关键词: AgonistGlutamate receptorNMDA receptorStereochemistryChemistryMagnesium ionPhencyclidineGlycineMagnesiumReceptor

摘要: Abstract It has been reported that glutamate can increase the binding of [ 3 H]TCP to phencyclidine (PCP) receptors by an action on which are selective for N-methyl-D-aspartate (NMDA). Recently this laboratory glycine and magnesium amplify effect NMDA agonists in well-washed, lysed cortical membranes. Here we report maximally effective concentrations (10 μM), (300 MgCl 2 μM) affinity PCP receptor approximately 4-fold absence any change density receptors. However, combination with glutamate, had further increasing B max about 75%. Finally, a synaptosomal P preparation, not washed minimize concentration endogenous effectors value similar well-washed but K D 8-fold lower. These data indicate primary agonists, glycine, low ions is convert from low-affinity high-affinity state. discussed relation functional regulation ionophore.

参考文章(25)
Lawrence D. Snell, Robert S. Morter, Kenneth M. Johnson, Glycine potentiates N-methyl-d-aspartate-induced [3H]TCP binding to rat cortical membranes Neuroscience Letters. ,vol. 83, pp. 313- 317 ,(1987) , 10.1016/0304-3940(87)90106-6
Grant A. McPherson, Analysis of radioligand binding experiments: A collection of computer programs for the IBM PC Journal of Pharmacological Methods. ,vol. 14, pp. 213- 228 ,(1985) , 10.1016/0160-5402(85)90034-8
Daniel C. Javitt, Alan Jotkowitz, Ratna Sircar, Stephen R. Zukin, Non-competitive regulation of phencyclidine/σ-receptors by the N-methyl-d-aspartate receptor antagonist d-(−)-2-amino-5-phosphonovaleric acid Neuroscience Letters. ,vol. 78, pp. 193- 198 ,(1987) , 10.1016/0304-3940(87)90632-X
Neil L. Harrison, Michael A. Simmonds, Quantitative studies on some antagonists of N-methyl D-aspartate in slices of rat cerebral cortex. British Journal of Pharmacology. ,vol. 84, pp. 381- 391 ,(1985) , 10.1111/J.1476-5381.1985.TB12922.X
Jacques Vignon, Robert Chicheportiche, Michèle Chicheportiche, Jean-Marc Kamenka, Patrick Geneste, Michel Lazdunski, [3H]TCP: a new tool with high affinity for the PCP receptor in rat brain. Brain Research. ,vol. 280, pp. 194- 197 ,(1983) , 10.1016/0006-8993(83)91193-9
Lawrence D. Snell, Su-Jin Yi, Kenneth M. Johnson, Comparison of the effects of MK-801 and phencyclidine on catecholamine uptake and NMDA-induced norepinephrine release. European Journal of Pharmacology. ,vol. 145, pp. 223- 226 ,(1988) , 10.1016/0014-2999(88)90235-X
E. H. Wong, J. A. Kemp, T. Priestley, A. R. Knight, G. N. Woodruff, L. L. Iversen, The anticonvulsant MK-801 is a potent N-methyl-D-aspartate antagonist. Proceedings of the National Academy of Sciences of the United States of America. ,vol. 83, pp. 7104- 7108 ,(1986) , 10.1073/PNAS.83.18.7104
L. Nowak, P. Bregestovski, P. Ascher, A. Herbet, A. Prochiantz, Magnesium gates glutamate-activated channels in mouse central neurones Nature. ,vol. 307, pp. 462- 465 ,(1984) , 10.1038/307462A0