GRIN2B

N-methyl-D-aspartate (NMDA) receptors are a class of ionotropic glutamate receptors. The NMDA receptor channel has been shown to be involved in long-term potentiation, an activity-dependent increase in the efficiency of synaptic transmission thought to underlie certain kinds of memory and learning. NMDA receptor channels are heterotetramers composed of two molecules of the key receptor subunit NMDAR1 (GRIN1) and two drawn from one or more of the four NMDAR2 subunits: NMDAR2A (GRIN2A), NMDAR2B (GRIN2B), NMDAR2C (GRIN2C), and NMDAR2D (GRIN2D). The NR2 subunit acts as the agonist binding site for glutamate, one of the predominant excitatory neurotransmitter receptors in the mammalian brain.{{cite web | title = Entrez Gene: GRIN2B glutamate receptor, ionotropic, N-methyl D-aspartate 2B| url = https://www.ncbi.nlm.nih.gov/sites/entrez?Db=gene&Cmd=ShowDetailView&TermToSearch=2904}}

NR2B has been associated with age- and visual-experience-dependent plasticity in the neocortex of rats, where an increased NR2B/NR2A ratio correlates directly with the stronger excitatory LTP in young animals. This is thought to contribute to experience-dependent refinement of developing cortical circuits.{{cite journal | vauthors = Yoshimura Y, Ohmura T, Komatsu Y | title = Two forms of synaptic plasticity with distinct dependence on age, experience, and NMDA receptor subtype in rat visual cortex | journal = The Journal of Neuroscience | volume = 23 | issue = 16 | pages = 6557–66 | date = July 2003 | pmid = 12878697 | doi = 10.1523/JNEUROSCI.23-16-06557.2003 | pmc = 6740618 | doi-access = free }}

Engineered to overexpress GRIN2B in their brains, mice and rats exhibit improved mental function. The "Doogie" mouse performed twice as well on one learning test.{{cite journal | vauthors = Tang YP, Shimizu E, Dube GR, Rampon C, Kerchner GA, Zhuo M, Liu G, Tsien JZ | title = Genetic enhancement of learning and memory in mice | journal = Nature | volume = 401 | issue = 6748 | pages = 63–9 | date = September 1999 | pmid = 10485705 | doi = 10.1038/43432 | bibcode = 1999Natur.401...63T | s2cid = 481884 }}{{cite journal | vauthors = Wang D, Cui Z, Zeng Q, Kuang H, Wang LP, Tsien JZ, Cao X | title = Genetic enhancement of memory and long-term potentiation but not CA1 long-term depression in NR2B transgenic rats | journal = PLOS ONE | volume = 4 | issue = 10 |page = e7486 | date = October 2009 | pmid = 19838302 | doi = 10.1371/journal.pone.0007486 | pmc=2759522| bibcode = 2009PLoSO...4.7486W | doi-access = free }}

• Besonprodil
• CERC-301, a selective NR2B receptor antagonist
• Eliprodil
• Ethanol - apparent induction of dephosphorylation of the NR2B Tyr1472 residue by STEP, leading to reduced receptor function
• Ifenprodil
• Rislenemdaz
• EVT-101, a selective NR2B receptor antagonist. This compound was tested as a potentially fast-acting antidepressant.{{cite journal | url = http://clinicaltrials.gov/ct2/show/NCT00526968 | title = The Effects of a Novel NMDA NR2B-Subtype Selective Antagonist, EVT 101, on Brain Function | date = 2008-02-14 | journal = Nct00526968 | publisher = ClinicalTrials.gov | access-date = 2010-08-19 }} In 2011 it was voluntarily withdrawn from a Phase II clinical study in treatment-resistant depression due to an unsatisfactory toxicity profile.{{cite web | url = http://www.evotec.com/archive/en/Press-releases/2011/Phase-II-study-with-NR2B-sub-type-selective-NMDA-antagonist-in-treatment-resistant-depression-voluntarily-terminated/2157/1 | title = Phase II study with NR2B sub-type selective NMDA antagonist in treatment-resistant depression voluntarily terminated | date = 2011-05-18 | publisher = evotec.com | access-date = 2015-08-24 }}{{Dead link|date=May 2024 |bot=InternetArchiveBot |fix-attempted=yes }}
• Felbamate, an anticonvulsant that is also a positive allosteric modulator for the GABA_A receptor
• Ro-25-6981 (also known as MI-4), a selective NR2B receptor antagonist
• Traxoprodil, a selective NR2B receptor antagonist
• Toluene - noncompetitive antagonist

GRIN2B has been shown to interact with:

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• Actinin, alpha 2,{{cite journal | vauthors = Wyszynski M, Lin J, Rao A, Nigh E, Beggs AH, Craig AM, Sheng M | title = Competitive binding of alpha-actinin and calmodulin to the NMDA receptor | journal = Nature | volume = 385 | issue = 6615 | pages = 439–42 | date = January 1997 | pmid = 9009191 | doi = 10.1038/385439a0 | bibcode = 1997Natur.385..439W | s2cid = 4266742 }}
• DLG2,
• DLG3,
• DLG4,{{cite journal | vauthors = Inanobe A, Fujita A, Ito M, Tomoike H, Inageda K, Kurachi Y | title = Inward rectifier K+ channel Kir2.3 is localized at the postsynaptic membrane of excitatory synapses | journal = American Journal of Physiology. Cell Physiology | volume = 282 | issue = 6 | pages = C1396–403 | date = June 2002 | pmid = 11997254 | doi = 10.1152/ajpcell.00615.2001 }}{{cite journal | vauthors = Irie M, Hata Y, Takeuchi M, Ichtchenko K, Toyoda A, Hirao K, Takai Y, Rosahl TW, Südhof TC | title = Binding of neuroligins to PSD-95 | journal = Science | volume = 277 | issue = 5331 | pages = 1511–5 | date = September 1997 | pmid = 9278515 | doi = 10.1126/science.277.5331.1511 }}{{cite journal | vauthors = Sans N, Prybylowski K, Petralia RS, Chang K, Wang YX, Racca C, Vicini S, Wenthold RJ | title = NMDA receptor trafficking through an interaction between PDZ proteins and the exocyst complex | journal = Nature Cell Biology | volume = 5 | issue = 6 | pages = 520–30 | date = June 2003 | pmid = 12738960 | doi = 10.1038/ncb990 | s2cid = 13444388 }}{{cite journal | vauthors = Lim IA, Hall DD, Hell JW | title = Selectivity and promiscuity of the first and second PDZ domains of PSD-95 and synapse-associated protein 102 | journal = The Journal of Biological Chemistry | volume = 277 | issue = 24 | pages = 21697–711 | date = June 2002 | pmid = 11937501 | doi = 10.1074/jbc.M112339200 | doi-access = free }}{{cite journal | vauthors = Niethammer M, Valtschanoff JG, Kapoor TM, Allison DW, Weinberg RJ, Craig AM, Sheng M | title = CRIPT, a novel postsynaptic protein that binds to the third PDZ domain of PSD-95/SAP90 | journal = Neuron | volume = 20 | issue = 4 | pages = 693–707 | date = April 1998 | pmid = 9581762 | doi = 10.1016/s0896-6273(00)81009-0 | s2cid = 16068361 | doi-access = free }}{{cite journal | vauthors = Kornau HC, Schenker LT, Kennedy MB, Seeburg PH |author-link3=Mary B. Kennedy| title = Domain interaction between NMDA receptor subunits and the postsynaptic density protein PSD-95 | journal = Science | volume = 269 | issue = 5231 | pages = 1737–40 | date = September 1995 | pmid = 7569905 | doi = 10.1126/science.7569905 |bibcode=1995Sci...269.1737K}}
• EXOC4,
• LIN7B,{{cite journal | vauthors = Jo K, Derin R, Li M, Bredt DS | title = Characterization of MALS/Velis-1, -2, and -3: a family of mammalian LIN-7 homologs enriched at brain synapses in association with the postsynaptic density-95/NMDA receptor postsynaptic complex | journal = The Journal of Neuroscience | volume = 19 | issue = 11 | pages = 4189–99 | date = June 1999 | pmid = 10341223 | doi = 10.1523/JNEUROSCI.19-11-04189.1999| pmc = 6782594 | doi-access = free }} and
• RICS.{{cite journal | vauthors = Nakazawa T, Watabe AM, Tezuka T, Yoshida Y, Yokoyama K, Umemori H, Inoue A, Okabe S, Manabe T, Yamamoto T | title = p250GAP, a novel brain-enriched GTPase-activating protein for Rho family GTPases, is involved in the N-methyl-d-aspartate receptor signaling | journal = Molecular Biology of the Cell | volume = 14 | issue = 7 | pages = 2921–34 | date = July 2003 | pmid = 12857875 | pmc = 165687 | doi = 10.1091/mbc.E02-09-0623 }}

{{Div col end}}

• NMDA receptor
• Glutamate receptor

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{{NLM content}}

{{Ligand-gated ion channels}}

Category:Ionotropic glutamate receptors