[3H](+)MK801 Radioligand Binding Assay at the N‐Methyl‐D‐Aspartate Receptor

作者: Ian J. Reynolds

DOI: 10.1002/0471141755.PH0120S11

关键词:

摘要: The N-methyl-D-aspartate subtype of glutamate receptor is unusual in that it requires two endogenous agonists for activation. Thus, addition to glutamate, the amino acid glycine (or possibly D-serine) an essential co-agonist. This unit presents a radioligand binding protocol detects ligand activity at NMDA receptor-associated site. convenient approach exploits ability modulators alter kinetics ligands bind channel-blocking site receptor. takes advantage one most potent and specific this receptor, case [(3)H](+)MK801. Importantly, assay can detect differentiate antagonists A measurement with [(3)H](+)MK801 provided, along support protocols provide information aid design assays site, data analysis.

参考文章(16)
CJ McBain, ML Mayer, None, N-methyl-D-aspartic acid receptor structure and function Physiological Reviews. ,vol. 74, pp. 723- 760 ,(1994) , 10.1152/PHYSREV.1994.74.3.723
J O McNamara, D W Bonhaus, N-methyl-D-aspartate receptor regulation of uncompetitive antagonist binding in rat brain membranes: kinetic analysis. Molecular Pharmacology. ,vol. 34, pp. 250- 255 ,(1988)
B M Baron, R S Gross, B L Harrison, B W Siegel, P Towers, C Hawes, [3H]MDL 105,519, a high-affinity radioligand for the N-methyl-D-aspartate receptor-associated glycine recognition site. Journal of Pharmacology and Experimental Therapeutics. ,vol. 279, pp. 62- 68 ,(1996)
C.F. Starmer, D.L. Packer, A.O. Grant, Ligand binding to transiently accessible sites: mechanisms for varying apparent binding rates. Journal of Theoretical Biology. ,vol. 124, pp. 335- 341 ,(1987) , 10.1016/S0022-5193(87)80120-0
John A. Kemp, Paul D. Leeson, The glycine site of the NMDA receptor — five years on Trends in Pharmacological Sciences. ,vol. 14, pp. 20- 25 ,(1993) , 10.1016/0165-6147(93)90108-V
Paul D. Leeson, Leslie L. Iversen, The glycine site on the NMDA receptor: structure-activity relationships and therapeutic potential. Journal of Medicinal Chemistry. ,vol. 37, pp. 4053- 4067 ,(1994) , 10.1021/JM00050A001
I. J. Reynolds, S. N. Murphy, R. J. Miller, 3H-labeled MK-801 binding to the excitatory amino acid receptor complex from rat brain is enhanced by glycine Proceedings of the National Academy of Sciences of the United States of America. ,vol. 84, pp. 7744- 7748 ,(1987) , 10.1073/PNAS.84.21.7744
H. Wolosker, S. Blackshaw, S. H. Snyder, Serine racemase: a glial enzyme synthesizing D-serine to regulate glutamate-N-methyl-D-aspartate neurotransmission. Proceedings of the National Academy of Sciences of the United States of America. ,vol. 96, pp. 13409- 13414 ,(1999) , 10.1073/PNAS.96.23.13409