LY-487,379 explained
LY-487,379 is a drug used in scientific research that acts as a selective positive allosteric modulator for the metabotropic glutamate receptor group II subtype mGluR2.[1] It is used to study the structure and function of this receptor subtype,[2] [3] and LY-487,379 along with various other mGluR2/3 agonists and positive modulators are being investigated as possible antipsychotic and anxiolytic drugs.[4] [5] [6] [7] [8]
See also
Notes and References
- Johnson MP, Baez M, Jagdmann GE, Britton TC, Large TH, Callagaro DO, Tizzano JP, Monn JA, Schoepp DD . 6 . Discovery of allosteric potentiators for the metabotropic glutamate 2 receptor: synthesis and subtype selectivity of N-(4-(2-methoxyphenoxy)phenyl)-N-(2,2,2- trifluoroethylsulfonyl)pyrid-3-ylmethylamine . Journal of Medicinal Chemistry . 46 . 15 . 3189–92 . July 2003 . 12852748 . 10.1021/jm034015u .
- Schaffhauser H, Rowe BA, Morales S, Chavez-Noriega LE, Yin R, Jachec C, Rao SP, Bain G, Pinkerton AB, Vernier JM, Bristow LJ, Varney MA, Daggett LP . 6 . Pharmacological characterization and identification of amino acids involved in the positive modulation of metabotropic glutamate receptor subtype 2 . Molecular Pharmacology . 64 . 4 . 798–810 . October 2003 . 14500736 . 10.1124/mol.64.4.798 . 15919973 .
- Poisik O, Raju DV, Verreault M, Rodriguez A, Abeniyi OA, Conn PJ, Smith Y . Metabotropic glutamate receptor 2 modulates excitatory synaptic transmission in the rat globus pallidus . Neuropharmacology . 49 . 57–69 . 2005 . Suppl 1 . 15993439 . 10.1016/j.neuropharm.2005.03.006 . 21881395 .
- Galici R, Echemendia NG, Rodriguez AL, Conn PJ . A selective allosteric potentiator of metabotropic glutamate (mGlu) 2 receptors has effects similar to an orthosteric mGlu2/3 receptor agonist in mouse models predictive of antipsychotic activity . The Journal of Pharmacology and Experimental Therapeutics . 315 . 3 . 1181–1187 . December 2005 . 16123306 . 10.1124/jpet.105.091074 . 9159875 . https://web.archive.org/web/20190221225118/http://pdfs.semanticscholar.org/3000/65580e1d888e0d2383e21447ec7b1f1b6a6a.pdf . dead . 2019-02-21 .
- Marino MJ, Conn PJ . Glutamate-based therapeutic approaches: allosteric modulators of metabotropic glutamate receptors . Current Opinion in Pharmacology . 6 . 1 . 98–102 . February 2006 . 16368268 . 10.1016/j.coph.2005.09.006 .
- Harich S, Gross G, Bespalov A . Stimulation of the metabotropic glutamate 2/3 receptor attenuates social novelty discrimination deficits induced by neonatal phencyclidine treatment . Psychopharmacology . 192 . 4 . 511–9 . July 2007 . 17318501 . 10.1007/s00213-007-0742-y . 7551116 .
- Conn PJ, Jones CK . Promise of mGluR2/3 activators in psychiatry . Neuropsychopharmacology . 34 . 1 . 248–9 . January 2009 . 19079073 . 2907744 . 10.1038/npp.2008.156 .
- Hermes ML, Renaud LP . Postsynaptic and presynaptic group II metabotropic glutamate receptor activation reduces neuronal excitability in rat midline paraventricular thalamic nucleus . The Journal of Pharmacology and Experimental Therapeutics . 336 . 3 . 840–9 . March 2011 . 21139059 . 10.1124/jpet.110.176149 . 25111011 . https://web.archive.org/web/20190222071207/http://pdfs.semanticscholar.org/3338/3c0769e7c9f9bffbedd6fdbfec4124dc0140.pdf . dead . 2019-02-22 .