XAP044

Last updated
XAP044
XAP044 structure.png
Identifiers
  • 7-hydroxy-3-(4-iodophenoxy)-4H-chromen-4-one
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
Chemical and physical data
Formula C15H9IO4
Molar mass 380.137 g·mol−1
3D model (JSmol)
  • C1=CC(=CC=C1OC2=COC3=C(C2=O)C=CC(=C3)O)I
  • InChI=1S/C15H9IO4/c16-9-1-4-11(5-2-9)20-14-8-19-13-7-10(17)3-6-12(13)15(14)18/h1-8,17H
  • Key:XXZKJJYWINSUMJ-UHFFFAOYSA-N

XAP044 is a drug which acts as a potent and selective antagonist of the metabotropic glutamate receptor 7 (mGluR7). It inhibits long-term potentiation in the amygdala and inhibits responses associated with stress and anxiety in animal models, [1] as well as being used to study the role of mGluR7 in various other processes. [2] [3] [4]

References

  1. ↑ Gee CE, Peterlik D, Neuhäuser C, Bouhelal R, Kaupmann K, Laue G, et al. (April 2014). "Blocking metabotropic glutamate receptor subtype 7 (mGlu7) via the Venus flytrap domain (VFTD) inhibits amygdala plasticity, stress, and anxiety-related behavior". The Journal of Biological Chemistry. 289 (16): 10975–10987. doi: 10.1074/jbc.M113.542654 . PMC   4036238 . PMID   24596089.
  2. ↑ Hajasova Z, Canestrelli C, Acher F, Noble F, Marie N (March 2018). "Role of mGlu7 receptor in morphine rewarding effects is uncovered by a novel orthosteric agonist". Neuropharmacology. 131: 424–430. doi:10.1016/j.neuropharm.2018.01.002. PMID   29307544. S2CID   3391450.
  3. ↑ Gryksa K, Mittmann L, Bauer A, Peterlik D, Flor PJ, Uschold-Schmidt N, Bosch OJ (January 2020). "Metabotropic glutamate receptor subtype 7 controls maternal care, maternal motivation and maternal aggression in mice". Genes, Brain and Behavior. 19 (1) e12627. doi: 10.1111/gbb.12627 . PMID   31793148. S2CID   208609219.
  4. ↑ Estrela KA, Senninger L, Arndt J, Kabas M, Schmid F, Dillmann L, et al. (June 2022). "Blocking Metabotropic Glutamate Receptor Subtype 7 via the Venus Flytrap Domain Promotes a Chronic Stress-Resilient Phenotype in Mice". Cells. 11 (11): 1817. doi: 10.3390/cells11111817 . PMC   9180111 . PMID   35681512.
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