Protein Information

Name NMDA receptor 1
Synonyms GRIN 1; NR1; GRIN1; Glutamate [NMDA] receptor subunit zeta 1; Glutamate [NMDA] receptor subunit zeta 1 precursor; N methyl D aspartate receptor subunit NR1; NMDA receptor 1; NMDA 1…

Compound Information

Name strychnine
CAS strychnidin-10-one

Reference List

PubMed Abstract RScore(About this table)
12930797 Kinney GG, Sur C, Burno M, Mallorga PJ, Williams JB, Figueroa DJ, Wittmann M, Lemaire W, Conn PJ: The glycine transporter type 1 inhibitor N-[3-(4'-fluorophenyl)-3-(4'-phenylphenoxy) propyl] sarcosine potentiates NMDA receptor-mediated responses in vivo and produces an antipsychotic profile in rodent behavior. J Neurosci. 2003 Aug 20;23(20):7586-91.

Glycine acts as a necessary coagonist for glutamate at the NMDA receptor (NMDAR) complex by binding to the strychnine-insensitive glycine-B binding site on the NR1 subunit.
81(1,1,1,1) Details
15523521 Lavrov I, Cheng J: Activation of NMDA receptors is required for the initiation and maintenance of walking-like activity in the mudpuppy (Necturus Maculatus). Can J Physiol Pharmacol. 2004 Aug-Sep;82(8-9):637-44.

Furthermore, application of L-701,324 (a selective antagonist of the strychnine-insensitive glycine site of NMDA receptor) (1-10 micromol/L) also resulted in complete block of the walking-like activity.
31(0,1,1,1) 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.

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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.
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15045581 Scappaticci AA, Jacques R, Carroll JE, Hufnagel LA, Kass-Simon G: Immunocytochemical evidence for an NMDA1 receptor subunit in dissociated cells of Hydra vulgaris. Cell Tissue Res. 2004 May;316(2):263-70. Epub 2004 Mar 25.

They support other behavioral and biochemical evidence for a D-serine-sensitive, strychnine-insensitive, glycine receptor in hydra and suggest that the glutamatergic AMPA/kainate-NMDA system is an early evolved, phylogenetically old, behavioral control mechanism.
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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.

Glycine coactivates glutamate N-methyl-D-aspartate (NMDA) receptors by binding to a distinct recognition site on the NR1 subunit.
Stimulation (taurine, beta-alanine) or inhibition (strychnine) of the inhibitory strychnine-sensitive glycine receptors did not produce any neurotoxicity.
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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
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.

These receptors may display the triple subunit combination NR1/NR2A/NR2B.
This effect of glycine was strychnine-insensitive and could be mimicked by D-serine, a stereoselective agonist at the NMDA receptor glycine site.
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
11738262 Tapia JC, Mentis GZ, Navarrete R, Nualart F, Figueroa E, Sanchez A, Aguayo LG: Early expression of glycine and GABA (A) receptors in developing spinal cord neurons. Neuroscience. 2001;108(3):493-506.

Immunocytochemical studies with NR1 and GluR1 antibodies showed a delayed appearance of N-methyl-D-aspartate (NMDA) and alpha-amino-3-hydroxy-5-methyl-4-isoxazolepropionate (AMPA) receptors respectively.
The use of various receptor antagonists (strychnine, bicuculline, DL-2-amino-5-phosphonovalerate [APV], 6-cyano-7-nitroquinoxaline-2,3-dione [CNQX]) revealed that this activity was predominantly glycinergic, and to a smaller extent, GABAergic.
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.


Neurons exposed to 50 mm ethanol for 4 d showed an increase in the colocalization of NMDA receptor type 1 (NR1) clusters with the presynaptic marker protein synapsin.
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
7961649 Kumar KN, Babcock KK, Johnson PS, Chen X, Eggeman KT, Michaelis EK: Purification and pharmacological and immunochemical characterization of synaptic membrane proteins with ligand-binding properties of N-methyl-D-aspartate receptors. J Biol Chem. 1994 Nov 4;269(44):27384-93.

The co-purification of NMDA-sensitive L-glutamate binding, dizocilpine-sensitive thienylcyclohexyl piperidine (TCP)-binding, and strychnine-insensitive glycine-binding proteins was achieved by this affinity chromatographic procedure.
These studies indicate that these two proteins might be components of a complex that has some of the characteristics of NMDA receptors and that neuronal membranes may contain varieties of NMDA-like receptors composed of protein subunits that differ from the NMDAR1 and NMDAR2 receptor proteins.
1(0,0,0,1) Details