XAP044: Difference between revisions

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Created page with '{{drugbox | drug_name = XAP044 | image = XAP044_structure.png | legal_UK = | legal_DE = | C = 15 | H = 9 | I = 1 | O = 4 | IUPAC_name = 7-hydroxy-3-(4-iodophenoxy)-4H-chromen-4-one | CAS_number = 196928-50-4 | CAS_number_Ref = {{cascite|correct|CAS}} | ChEMBL = | ChemSpiderID = | PubChem = 5428913 | UNII = | smiles = C1=CC(=CC=C1OC2=COC3=C(C2=O)C=CC(=C3)O)I | StdInChI = 1S/C15H9IO4/c16-9-1-4-11(5-2-9)20-14-8-19-13-7-10(17)3-6-12...'
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Revision as of 06:18, 1 July 2022

XAP044
Identifiers
  • 7-hydroxy-3-(4-iodophenoxy)-4H-chromen-4-one
CAS Number
PubChem CID
Chemical and physical data
FormulaC15H9IO4
Molar mass380.137 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, Uschold-Schmidt N, Feuerbach D, Zimmermann K, Ofner S, Cryan JF, van der Putten H, Fendt M, Vranesic I, Glatthar R, Flor PJ. Blocking metabotropic glutamate receptor subtype 7 (mGlu7) via the Venus flytrap domain (VFTD) inhibits amygdala plasticity, stress, and anxiety-related behavior. J Biol Chem. 2014 Apr 18;289(16):10975-10987. doi:10.1074/jbc.M113.542654 PMID 24596089
  2. ^ Hajasova Z, Canestrelli C, Acher F, Noble F, Marie N. Role of mGlu7 receptor in morphine rewarding effects is uncovered by a novel orthosteric agonist. Neuropharmacology. 2018 Mar 15;131:424-430. doi:10.1016/j.neuropharm.2018.01.002 PMID 29307544
  3. ^ Gryksa K, Mittmann L, Bauer A, Peterlik D, Flor PJ, Uschold-Schmidt N, Bosch OJ. Metabotropic glutamate receptor subtype 7 controls maternal care, maternal motivation and maternal aggression in mice. Genes Brain Behav. 2020 Jan;19(1):e12627. doi:10.1111/gbb.12627 PMID 31793148
  4. ^ Estrela KAR, Senninger L, Arndt J, Kabas M, Schmid F, Dillmann L, Auer S, Stepfer T, Flor PJ, Uschold-Schmidt N. Blocking Metabotropic Glutamate Receptor Subtype 7 via the Venus Flytrap Domain Promotes a Chronic Stress-Resilient Phenotype in Mice. Cells. 2022 Jun 2;11(11):1817. doi:10.3390/cells11111817 PMID 35681512