Protein Information

Name NR2B
Synonyms GRIN2B; Glutamate [NMDA] receptor subunit epsilon 2; Glutamate [NMDA] receptor subunit epsilon 2 precursor; N methyl D aspartate receptor subtype 2B; N methyl D aspartate receptor subunit 2B; N methyl D aspartate receptor subunit 3; NMDAR2B; NR2B…

Compound Information

Name strychnine
CAS strychnidin-10-one

Reference List

PubMed Abstract RScore(About this table)
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
15490133 Barth A, Nguyen LB, Barth L, Newell DW: Glycine-induced neurotoxicity in organotypic hippocampal slice cultures. Exp Brain Res. 2005 Mar;161(3):351-7. Epub 2004 Oct 14.

Purely excitatory glycine receptors composed of NR1 and NR3/NR4 NMDA receptor subunits have recently been described, raising the possibility of excitotoxic effects mediated by glycine alone.
Stimulation (taurine, beta-alanine) or inhibition (strychnine) of the inhibitory strychnine-sensitive glycine receptors did not produce any neurotoxicity.
1(0,0,0,1) Details
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.
In situ hybridization demonstrated that injection of the NMDAR1, NMDAR2A or NMDAR2B antisense ODNs produced specific reductions in target mRNA signal intensity in the injected striatum.
1(0,0,0,1) Details
11698028 Parsons CG: NMDA receptors as targets for drug action in neuropathic pain. Eur J Pharmacol. 2001 Oct 19;429(1-3):71-8.

Functional inhibition of NMDA receptors can be achieved through actions at different recognition sites such as the primary transmitter site (competitive), strychnine-insensitive glycine site (glycine (B)), polyamine site (NR2B selective) and phencyclidine site located inside the cationic channel.
32(0,1,1,2) Details
17502428 Smothers CT, Woodward JJ: Pharmacological characterization of glycine-activated currents in HEK 293 cells expressing N-methyl-D-aspartate NR1 and NR3 subunits. J Pharmacol Exp Ther. 2007 Aug;322(2):739-48. Epub 2007 May 14.

2(0,0,0,2) Details
15888962 Leewanich P, Tohda M, Takayama H, Sophasan S, Watanabe H, Matsumoto K: Corymine potentiates NMDA-induced currents in Xenopus oocytes expressing NR1a/NR2B glutamate receptors. J Pharmacol Sci. 2005 May;98(1):58-65. Epub 2005 May 12.

Previous studies demonstrated that corymine, an indole alkaloid isolated from the leaves of Hunter zeylanica, dose-dependently inhibited strychnine-sensitive glycine-induced currents.
2(0,0,0,2) 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
18554813 Cervetto C, Taccola G: GABAA and strychnine-sensitive glycine receptors modulate N-methyl-D-aspartate-evoked acetylcholine release from rat spinal motoneurons: a possible role in neuroprotection. Neuroscience. 2008 Jul 17;154(4):1517-24. Epub 2008 May 3.

NMDA-mediated [(3) H] ACh release was completely prevented by MK-801, 5,7-diclorokynurenic acid and ifenprodil, while it was strongly inhibited by a lower external pH, suggesting that the involved NMDA receptors contain NR1 and NR2B subunits.
1(0,0,0,1) Details
15356198 Carpenter-Hyland EP, Woodward JJ, Chandler LJ: Chronic ethanol induces synaptic but not extrasynaptic targeting of NMDA receptors. J Neurosci. 2004 Sep 8;24(36):7859-68.


Similar effects were observed with NR2B clustering after chronic ethanol exposure.
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