LY-487,379

LY-487,379
Clinical data
ATC code	none;
Identifiers
	IUPAC name N-(4-(2-methoxyphenoxy)phenyl)- N-(2,2,2-trifluoroethylsulfonyl)pyrid- 3-ylmethylamine;
CAS Number	353231-17-1 ;
PubChem CID	9825084;
IUPHAR/BPS	1402;
ChemSpider	8000831 ;
UNII	7WF5ZLL4D9;
ChEMBL	ChEMBL108939 ;
CompTox Dashboard (EPA)	DTXSID10431366 ;
Chemical and physical data
Formula	C21H19F3N2O4S
Molar mass	452.45 g·mol−1
3D model (JSmol)	Interactive image;
	SMILES c3ncccc3CN(S(=O)(=O)CC(F)(F)F)c2ccc(cc2)Oc1ccccc1OC;
	InChI InChI=1S/C21H19F3N2O4S/c1-29-19-6-2-3-7-20(19)30-18-10-8-17(9-11-18)26(14-16-5-4-12-25-13-16)31(27,28)15-21(22,23)24/h2-13H,14-15H2,1H3 ; Key:ALMACYDZFBMGOR-UHFFFAOYSA-N ;
	(what is this?) (verify)

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 mGluR_2/3 agonists and positive modulators are being investigated as possible antipsychotic and anxiolytic drugs.^[4]^[5]^[6]^[7]^[8]

References

^ Johnson MP, Baez M, Jagdmann GE, Britton TC, Large TH, Callagaro DO, et al. (July 2003). "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. doi:10.1021/jm034015u. PMID 12852748.
^ Schaffhauser H, Rowe BA, Morales S, Chavez-Noriega LE, Yin R, Jachec C, et al. (October 2003). "Pharmacological characterization and identification of amino acids involved in the positive modulation of metabotropic glutamate receptor subtype 2". Molecular Pharmacology. 64 (4): 798–810. doi:10.1124/mol.64.4.798. PMID 14500736. S2CID 15919973.
^ Poisik O, Raju DV, Verreault M, Rodriguez A, Abeniyi OA, Conn PJ, Smith Y (2005). "Metabotropic glutamate receptor 2 modulates excitatory synaptic transmission in the rat globus pallidus". Neuropharmacology. 49 (Suppl 1): 57–69. doi:10.1016/j.neuropharm.2005.03.006. PMID 15993439. S2CID 21881395.
^ Galici R, Echemendia NG, Rodriguez AL, Conn PJ (December 2005). "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" (PDF). The Journal of Pharmacology and Experimental Therapeutics. 315 (3): 1181–1187. doi:10.1124/jpet.105.091074. PMID 16123306. S2CID 9159875. Archived from the original (PDF) on 2019-02-21.
^ Marino MJ, Conn PJ (February 2006). "Glutamate-based therapeutic approaches: allosteric modulators of metabotropic glutamate receptors". Current Opinion in Pharmacology. 6 (1): 98–102. doi:10.1016/j.coph.2005.09.006. PMID 16368268.
^ Harich S, Gross G, Bespalov A (July 2007). "Stimulation of the metabotropic glutamate 2/3 receptor attenuates social novelty discrimination deficits induced by neonatal phencyclidine treatment". Psychopharmacology. 192 (4): 511–9. doi:10.1007/s00213-007-0742-y. PMID 17318501. S2CID 7551116.
^ Conn PJ, Jones CK (January 2009). "Promise of mGluR2/3 activators in psychiatry". Neuropsychopharmacology. 34 (1): 248–9. doi:10.1038/npp.2008.156. PMC 2907744. PMID 19079073.
^ Hermes ML, Renaud LP (March 2011). "Postsynaptic and presynaptic group II metabotropic glutamate receptor activation reduces neuronal excitability in rat midline paraventricular thalamic nucleus" (PDF). The Journal of Pharmacology and Experimental Therapeutics. 336 (3): 840–9. doi:10.1124/jpet.110.176149. PMID 21139059. S2CID 25111011. Archived from the original (PDF) on 2019-02-22.

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[1] Johnson MP, Baez M, Jagdmann GE, Britton TC, Large TH, Callagaro DO, et al. (July 2003). "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. doi:10.1021/jm034015u. PMID 12852748.

[2] Schaffhauser H, Rowe BA, Morales S, Chavez-Noriega LE, Yin R, Jachec C, et al. (October 2003). "Pharmacological characterization and identification of amino acids involved in the positive modulation of metabotropic glutamate receptor subtype 2". Molecular Pharmacology. 64 (4): 798–810. doi:10.1124/mol.64.4.798. PMID 14500736. S2CID 15919973.

[3] Poisik O, Raju DV, Verreault M, Rodriguez A, Abeniyi OA, Conn PJ, Smith Y (2005). "Metabotropic glutamate receptor 2 modulates excitatory synaptic transmission in the rat globus pallidus". Neuropharmacology. 49 (Suppl 1): 57–69. doi:10.1016/j.neuropharm.2005.03.006. PMID 15993439. S2CID 21881395.

[4] Galici R, Echemendia NG, Rodriguez AL, Conn PJ (December 2005). "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" (PDF). The Journal of Pharmacology and Experimental Therapeutics. 315 (3): 1181–1187. doi:10.1124/jpet.105.091074. PMID 16123306. S2CID 9159875. Archived from the original (PDF) on 2019-02-21.

[5] Marino MJ, Conn PJ (February 2006). "Glutamate-based therapeutic approaches: allosteric modulators of metabotropic glutamate receptors". Current Opinion in Pharmacology. 6 (1): 98–102. doi:10.1016/j.coph.2005.09.006. PMID 16368268.

[6] Harich S, Gross G, Bespalov A (July 2007). "Stimulation of the metabotropic glutamate 2/3 receptor attenuates social novelty discrimination deficits induced by neonatal phencyclidine treatment". Psychopharmacology. 192 (4): 511–9. doi:10.1007/s00213-007-0742-y. PMID 17318501. S2CID 7551116.

[7] Conn PJ, Jones CK (January 2009). "Promise of mGluR2/3 activators in psychiatry". Neuropsychopharmacology. 34 (1): 248–9. doi:10.1038/npp.2008.156. PMC 2907744. PMID 19079073.

[8] Hermes ML, Renaud LP (March 2011). "Postsynaptic and presynaptic group II metabotropic glutamate receptor activation reduces neuronal excitability in rat midline paraventricular thalamic nucleus" (PDF). The Journal of Pharmacology and Experimental Therapeutics. 336 (3): 840–9. doi:10.1124/jpet.110.176149. PMID 21139059. S2CID 25111011. Archived from the original (PDF) on 2019-02-22.

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See also

References