ML337

Last updated

ML337
ML337 structure.png
Identifiers
  • (R)-(2-fluoro-4-[(4-methoxyphenyl)ethynyl]phenyl)(3-hydroxypiperidin-1-yl)methanone
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
ChEMBL
Chemical and physical data
Formula C21H20FNO3
Molar mass 353.393 g·mol−1
3D model (JSmol)
  • COC1=CC=C(C=C1)C#CC2=CC(=C(C=C2)C(=O)N3CCC[C@H](C3)O)F
  • InChI=1S/C21H20FNO3/c1-26-18-9-6-15(7-10-18)4-5-16-8-11-19(20(22)13-16)21(25)23-12-2-3-17(24)14-23/h6-11,13,17,24H,2-3,12,14H2,1H3/t17-/m1/s1
  • Key:QBCRLDPMQHPGIM-QGZVFWFLSA-N

ML337 is an experimental drug that acts as a negative allosteric modulator selective for the glutamate receptor mGluR3. It has only moderate potency with an IC50 of 450 nM, but is highly selective over the closely related subtype mGluR2 with no effect even at 30,000 nM, and so has been used to study the effects of mGluR3 in isolation, which had previously been difficult to separate from mGluR2 mediated effects. [1] [2] [3]

References

  1. ↑ Wenthur C, Daniels JS, Morrison R, Engers JL, Niswender CM, Conn PJ, et al. (December 2012). "Development of a Second Generation mGlu3 NAM Probe". Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US). PMID   23885366.
  2. ↑ Wenthur CJ, Morrison R, Felts AS, Smith KA, Engers JL, Byers FW, et al. (June 2013). "Discovery of (R)-(2-fluoro-4-((-4-methoxyphenyl)ethynyl)phenyl) (3-hydroxypiperidin-1-yl)methanone (ML337), an mGlu3 selective and CNS penetrant negative allosteric modulator (NAM)". Journal of Medicinal Chemistry. 56 (12): 5208–5212. doi:10.1021/jm400439t. PMC   3769689 . PMID   23718281.
  3. ↑ Olivero G, Bonfiglio T, Vergassola M, Usai C, Riozzi B, Battaglia G, et al. (December 2017). "Immuno-pharmacological characterization of group II metabotropic glutamate receptors controlling glutamate exocytosis in mouse cortex and spinal cord". British Journal of Pharmacology. 174 (24): 4785–4796. doi:10.1111/bph.14061. PMC   5727332 . PMID   28967122.
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