Protein Information

Name NR2A
Synonyms GRIN2A; Glutamate [NMDA] receptor subunit epsilon 1; Glutamate [NMDA] receptor subunit epsilon 1 precursor; N methyl D aspartate receptor subtype 2A; N methyl D aspartate receptor subunit 2A; NMDAR2A; NR2A; hNR2A…

Compound Information

Name strychnine
CAS strychnidin-10-one

Reference List

PubMed Abstract RScore(About this table)
8558453 Standaert DG, Testa CM, Rudolf GD, Hollingsworth ZR: Inhibition of N-methyl-D-aspartate glutamate receptor subunit expression by antisense oligonucleotides reveals their role in striatal motor regulation. J Pharmacol Exp Ther. 1996 Jan;276(1):342-52.

After NMDAR1 antisense ODN injection, striatal binding of 3H-glutamate to NMDA sites was not altered, although strychnine-insensitive 3H-glycine binding sites exhibited a small but significant reduction.
Recent studies have revealed that NMDA receptors are heteromeric assemblies of structurally related subunits from two families: NMDAR1, which is required for channel activity, and NMDAR2A-D, which modulate the properties of the channels.
3(0,0,0,3) Details
9758163 Paudice P, Gemignani A, Raiteri M: Evidence for functional native NMDA receptors activated by glycine or D-serine alone in the absence of glutamatergic coagonist. Eur J Neurosci. 1998 Sep;10(9):2934-44.

This effect of glycine was strychnine-insensitive and could be mimicked by D-serine, a stereoselective agonist at the NMDA receptor glycine site.
The neuropeptide release elicited by D-serine was strongly inhibited by ifenprodil (0.3 microM) and by Zn2+ ions (50 nM), selective ligands at the NR2B and NR2A subunits of NMDA receptors, respectively.
2(0,0,0,2) Details
17646495 Milutinovic PS, Yang L, Cantor RS, Eger EI 2nd, Sonner JM: Anesthetic-like modulation of a gamma-aminobutyric acid type A, strychnine-sensitive glycine, and N-methyl-d-aspartate receptors by coreleased neurotransmitters. Anesth Analg. 2007 Aug;105(2):386-92.

METHODS: We tested this prediction by applying acetylcholine to a NR1/NR2A N-methyl-d-aspartate receptor, glycine to a wild-type alpha (1) beta (2) and anesthetic-resistant alpha (1)(S270I) beta (2) gamma-amino-butyric acid (GABA) type A receptor, and GABA to a homomeric alpha (1) wild type and anesthetic-resistant alpha (1) S267I glycine receptor.
1(0,0,0,1) Details
20092573 Reed BT, Sullivan SJ, Tsai G, Coyle JT, Esguerra M, Miller RF: The glycine transporter GlyT1 controls N-methyl-D-aspartic acid receptor coagonist occupancy in the mouse retina. Eur J Neurosci. 2009 Dec;30(12):2308-17. Epub 2009 Dec 10.

The interpretation of these studies was simplified by blocking post-synaptic inhibition with picrotoxinin and strychnine.
Immunoblots of NMDA receptor subunits (NR1, NR2A and NR2B) in WT and GlyT1 (-/+) animals showed that the NR1 subunits were identical.
1(0,0,0,1) Details
19523966 Mok MH, Fricker AC, Weil A, Kew JN: Electrophysiological characterisation of the actions of kynurenic acid at ligand-gated ion channels. Neuropharmacology. 2009 Sep;57(3):242-9. Epub 2009 Jun 11.

Using whole-cell patch-clamp recordings, we found that kynA was a more potent antagonist at human NR1a/NR2A compared with NR1a/NR2B receptors (IC (50): 158 muM and 681 muM, respectively; in 30 muM glycine).
KynA inhibited AMPA-evoked currents to a similar degree in cultured hippocampal neurons and a human GluR2 (flip/unedited) cell line (IC (50): 433 and 596 muM, respectively) and at higher concentrations, kynA also inhibited the strychnine-sensitive glycine receptor ( approximately 35% inhibition by 3 mM kynA).
1(0,0,0,1) Details