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NMDA receptor
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===Partial agonists=== [[Image:NMDA.svg|thumb|right|200px|[[N-Methyl-D-aspartic acid|''N''-Methyl-<small>D</small>-aspartic acid]] (NMDA), a synthetic partial agonist of the main site of the NMDAR]] [[N-Methyl-D-aspartic acid|''N''-Methyl-<small>D</small>-aspartic acid]] (NMDA), which the NMDA receptor was named after, is a partial agonist of the active or glutamate recognition site. 3,5-Dibromo-<small>L</small>-phenylalanine, a naturally occurring halogenated derivative of [[Phenylalanine|<small>L</small>-phenylalanine]], is a weak partial NMDA receptor agonist acting on the glycine site.<ref>{{cite journal | vauthors = Yarotskyy V, Glushakov AV, Sumners C, Gravenstein N, Dennis DM, Seubert CN, Martynyuk AE | title = Differential modulation of glutamatergic transmission by 3,5-dibromo-L-phenylalanine | journal = Molecular Pharmacology | volume = 67 | issue = 5 | pages = 1648β1654 | date = May 2005 | pmid = 15687225 | doi = 10.1124/mol.104.005983 | s2cid = 11672391 }}</ref><ref>{{Cite journal |last1=Kagiyama |first1=Tomoko |last2=Glushakov |first2=Alexander V. |last3=Sumners |first3=Colin |last4=Roose |first4=Brandy |last5=Dennis |first5=Donn M. |last6=Phillips |first6=M. Ian |last7=Ozcan |first7=Mehmet S. |last8=Seubert |first8=Christoph N. |last9=Martynyuk |first9=Anatoly E. |date=April 8, 2004 |title=Neuroprotective Action of Halogenated Derivatives of L-Phenylalanine |url=https://www.ahajournals.org/doi/10.1161/01.str.0000125722.10606.07 |journal=Stroke |volume=35 |issue=5 |pages=1192β1196 |doi=10.1161/01.STR.0000125722.10606.07|pmid=15073406 |url-access=subscription }}</ref> 3,5-Dibromo-<small>L</small>-phenylalanine has been proposed a novel therapeutic drug candidate for treatment of neuropsychiatric disorders and diseases such as [[schizophrenia]],<ref>{{cite journal | vauthors = Martynyuk AE, Seubert CN, Yarotskyy V, Glushakov AV, Gravenstein N, Sumners C, Dennis DM | title = Halogenated derivatives of aromatic amino acids exhibit balanced antiglutamatergic actions: potential applications for the treatment of neurological and neuropsychiatric disorders | journal = Recent Patents on CNS Drug Discovery | volume = 1 | issue = 3 | pages = 261β270 | date = November 2006 | pmid = 18221208 | doi = 10.2174/157488906778773706 }}</ref> and neurological disorders such as [[ischemic stroke]] and [[epileptic seizure]]s.<ref>{{cite journal | vauthors = Cao W, Shah HP, Glushakov AV, Mecca AP, Shi P, Sumners C, Seubert CN, Martynyuk AE | display-authors = 6 | title = Efficacy of 3,5-dibromo-L-phenylalanine in rat models of stroke, seizures and sensorimotor gating deficit | journal = British Journal of Pharmacology | volume = 158 | issue = 8 | pages = 2005β2013 | date = December 2009 | pmid = 20050189 | pmc = 2807662 | doi = 10.1111/j.1476-5381.2009.00498.x }}</ref> Other partial agonists of the NMDA receptor acting on novel sites such as [[rapastinel]] (GLYX-13) and [[apimostinel]] (NRX-1074) are now viewed for the development of new drugs with antidepressant and analgesic effects without obvious psychotomimetic activities.<ref>J. Moskal, D. Leander, R. Burch (2010). Unlocking the Therapeutic Potential of the NMDA Receptor. [http://www.dddmag.com/articles/2010/10/unlocking-therapeutic-potential-nmda-receptor ''Drug Discovery & Development News''.] Retrieved 19 December 2013.</ref> ====Examples==== * [[Aminocyclopropanecarboxylic acid]] (ACC) β synthetic glycine site partial agonist * [[Cycloserine]] ([[D-cycloserine|<small>D</small>-cycloserine]]) β naturally occurring glycine site partial agonist found in ''[[Streptomyces|Streptomyces orchidaceus]]'' * [[HA-966]] and [[L-687,414]] β synthetic glycine site weak partial agonists * [[Homoquinolinic acid]] β synthetic glutamate site partial agonist * [[N-Methyl-D-aspartic acid|''N''-Methyl-<small>D</small>-aspartic acid]] (NMDA) β synthetic glutamate site partial agonist Positive allosteric modulators include: * [[AGN-241751|Zelquistinel]] (GATE-251) β synthetic novel site partial agonist * [[Apimostinel]] (GATE-202) β synthetic novel site partial agonist * [[Rapastinel]] (GLYX-13) β synthetic novel site partial agonist<ref>{{cite journal | vauthors = Donello JE, Banerjee P, Li YX, Guo YX, Yoshitake T, Zhang XL, Miry O, Kehr J, Stanton PK, Gross AL, Burgdorf JS, Kroes RA, Moskal JR | display-authors = 6 | title = Positive N-Methyl-D-Aspartate Receptor Modulation by Rapastinel Promotes Rapid and Sustained Antidepressant-Like Effects | journal = The International Journal of Neuropsychopharmacology | volume = 22 | issue = 3 | pages = 247β259 | date = March 2019 | pmid = 30544218 | pmc = 6403082 | doi = 10.1093/ijnp/pyy101 }}</ref>
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