Memantine binding to a superficial site on NMDA receptors contributes to partial trapping

Journal of Physiology

Volumn 587, Issue 19, 2009, Pages 4589-4604

  Kotermanski, Shawn E ^a   Wood, Jesse T ^a   Johnson, Jon W ^a  

^a UNIVERSITY OF PITTSBURGH SCHOOL OF MEDICINE   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

KETAMINE; MEMANTINE; N METHYL DEXTRO ASPARTIC ACID RECEPTOR 1; N METHYL DEXTRO ASPARTIC ACID RECEPTOR 2A; RECOMBINANT RECEPTOR; MAGNESIUM ION; N METHYL DEXTRO ASPARTIC ACID RECEPTOR;

ARTICLE; CELL MEMBRANE DEPOLARIZATION; CELL MEMBRANE POTENTIAL; CONTROLLED STUDY; DISSOCIATION; DRUG BINDING SITE; DRUG EFFECT; DRUG RECEPTOR BINDING; HUMAN; HUMAN CELL; MEMBRANE ELECTROPHYSIOLOGY; NUCLEOTIDE SEQUENCE; PRIORITY JOURNAL; RECEPTOR BLOCKING; BINDING AFFINITY; BINDING SITE; CELLULAR PARAMETERS; CONCENTRATION (PARAMETERS); DRUG PROTEIN BINDING; EMBRYO; HYPERPOLARIZATION; IC50; MEMBRANE DEPOLARIZATION; MEMBRANE POTENTIAL; PARTIAL TRAPPING; PROTEIN EXPRESSION; WHOLE CELL PATCH CLAMP;

AMINO ACID SUBSTITUTION; BINDING SITES; BINDING, COMPETITIVE; CELL LINE; EXCITATORY AMINO ACID ANTAGONISTS; HUMANS; KETAMINE; KINETICS; MEMANTINE; MEMBRANE POTENTIALS; MODELS, NEUROLOGICAL; MUTAGENESIS, SITE-DIRECTED; PATCH-CLAMP TECHNIQUES; RECEPTORS, N-METHYL-D-ASPARTATE; RECOMBINANT PROTEINS; TRANSFECTION;

EID: 70350412253     PISSN: 00223751     EISSN: 14697793     Source Type: Journal    
DOI: 10.1113/jphysiol.2009.176297     Document Type: Article

References (27)

1. Benveniste M, Mayer ML. Trapping of glutamate and glycine during open channel block of rat hippocampal neuron NMDA receptors by 9-aminoacridine. J Physiol 1995, 483:367-384.
2. Blanpied TA, Boeckman FA, Aizenman E, Johnson JW. Trapping channel block of NMDA-activated responses by amantadine and memantine. J Neurophysiol 1997, 77:309-323.
3. Bliss TV, Collingridge GL. A synaptic model of memory: long-term potentiation in the hippocampus. Nature 1993, 361:31-39.
4. Bolshakov KV, Gmiro VE, Tikhonov DB, Magazanik LG. Determinants of trapping block of N-methyl-D-aspartate receptor channels. J Neurochem 2003, 87:56-65.
5. Burnashev N, Schoepfer R, Monyer H, Ruppersberg JP, Gunther W, Seeburg PH, Sakmann B. Control by asparagine residues of calcium permeability and magnesium blockade in the NMDA receptor. Science 1992, 257:1415-1419.
6. Chen HS, Lipton SA. Mechanism of memantine block of NMDA-activated channels in rat retinal ganglion cells: uncompetitive antagonism. J Physiol 1997, 499:27-46.
7. Chen HS, Pellegrini JW, Aggarwal SK, Lei SZ, Warach S, Jensen FE, Lipton SA. Open-channel block of N-methyl-D-aspartate (NMDA) responses by memantine: therapeutic advantage against NMDA receptor-mediated neurotoxicity. J Neurosci 1992, 12:4427-4436.
8. Chen HSV, Lipton SA. Pharmacological implications of two distinct mechanisms of interaction of memantine with N-methyl-D-aspartate-gated channels. J Pharmacol Exp Ther 2005, 314:961-971.
9. Dingledine R, Borges K, Bowie D, Traynelis SF. The glutamate receptor ion channels. Pharmacol Rev 1999, 51:7-61.
10. Hardingham GE, Bading H. The Yin and Yang of NMDA receptor signalling. Trends Neurosci 2003, 26:81-89.
11. Johnson JW, Kotermanski SE. Mechanism of action of memantine. Curr Opin Pharmacol 2006, 6:61-67.
12. Kashiwagi K, Masuko T, Nguyen CD, Kuno T, Tanaka I, Igarashi K, Williams K. Channel blockers acting at N-methyl-D-aspartate receptors: differential effects of mutations in the vestibule and ion channel pore. Mol Pharmacol 2002, 61:533-545.
13. Kotermanski SE, Johnson JW. Mg2+ imparts NMDA receptor subtype selectivity to the Alzheimer's drug memantine. J Neurosci 2009, 29:2774-2779.
14. Krystal JH, D'Souza DC, Mathalon D, Perry E, Belger A, Hoffman R. NMDA receptor antagonist effects, cortical glutamatergic function, and schizophrenia: toward a paradigm shift in medication development. Psychopharmacology (Berl) 2003, 169:215-233.
15. Kuner T, Schoepfer R. Multiple structural elements determine subunit specificity of Mg2+ block in NMDA receptor channels. J Neurosci 1996, 16:3549-3558.
16. Mealing GA, Lanthorn TH, Murray CL, Small DL, Morley P. Differences in degree of trapping of low-affinity uncompetitive N-methyl-D-aspartic acid receptor antagonists with similar kinetics of block. J Pharmacol Exp Ther 1999, 288:204-210.
17. Mealing GA, Lanthorn TH, Small DL, Murray RJ, Mattes KC, Comas TM, Morley P. Structural modifications to an N-methyl-D-aspartate receptor antagonist result in large differences in trapping block. J Pharmacol Exp Ther 2001, 297:906-914.
18. Olney JW. Excitotoxicity, apoptosis and neuropsychiatric disorders. Curr Opin Pharmacol 2003, 3:101-109.
19. Parsons CG, Gruner R, Rozental J, Millar J, Lodge D. Patch clamp studies on the kinetics and selectivity of N-methyl-D-aspartate receptor antagonism by memantine (1-amino-3,5-dimethyladamantan). Neuropharmacology 1993, 32:1337-1350.
20. Parsons CG, Panchenko VA, Pinchenko VO, Tsyndrenko AY, Krishtal OA. Comparative patch-clamp studies with freshly dissociated rat hippocampal and striatal neurons on the NMDA receptor antagonistic effects of amantadine and memantine. Eur J Neurosci 1996, 8:446-454.
21. Parsons CG, Quack G, Bresink I, Baran L, Przegalinski E, Kostowski W, Krzascik P, Hartmann S, Danysz W. Comparison of the potency, kinetics and voltage-dependency of a series of uncompetitive NMDA receptor antagonists in vitro with anticonvulsive and motor impairment activity in vivo. Neuropharmacology 1995, 34:1239-1258.
22. Parsons CG, Stoffler A, Danysz W. Memantine: a NMDA receptor antagonist that improves memory by restoration of homeostasis in the glutamatergic system - too little activation is bad, too much is even worse. Neuropharmacology 2007, 53:699-723.
23. Sobolevsky A, Koshelev S. Two blocking sites of amino-adamantane derivatives in open N-methyl-D- aspartate channels. Biophys J 1998, 74:1305-1319.
24. Sobolevsky AI, Beck C, Wollmuth LP. Molecular rearrangements of the extracellular vestibule in NMDAR channels during gating. Neuron 2002, 33:75-85.
25. Sobolevsky AI, Koshelev SG, Khodorov BI. Interaction of memantine and amantadine with agonist-unbound NMDA- receptor channels in acutely isolated rat hippocampal neurons. J Physiol 1998, 512:47-60.
26. Wollmuth LP, Kuner T, Sakmann B. Adjacent asparagines in the NR2-subunit of the NMDA receptor channel control the voltage-dependent block by extracellular Mg2+. J Physiol 1998, 506:13-32.
27. Wollmuth LP, Kuner T, Seeburg PH, Sakmann B. Differential contribution of the NR1- and NR2A-subunits to the selectivity filter of recombinant NMDA receptor channels. J Physiol 1996, 491:779-797.