XAP044 - Misplaced Pages

Chemical compound Pharmaceutical compound

XAP044
Identifiers

IUPAC name 7-hydroxy-3-(4-iodophenoxy)-4H-chromen-4-one
CAS Number	196928-50-4
PubChem CID	5428913
IUPHAR/BPS	8545
ChemSpider	4558326
Chemical and physical data
Formula	C₁₅H₉IO₄
Molar mass	380.137 g·mol
3D model (JSmol)	Interactive image
SMILES C1=CC(=CC=C1OC2=COC3=C(C2=O)C=CC(=C3)O)I
InChI 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, as well as being used to study the role of mGluR₇ in various other processes.

References

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.
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.
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.
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.

mGluR₁Tooltip Metabotropic glutamate receptor 1

mGluR₅Tooltip Metabotropic glutamate receptor 5

mGluR₂Tooltip Metabotropic glutamate receptor 2

mGluR₃Tooltip Metabotropic glutamate receptor 3

mGluR₄Tooltip Metabotropic glutamate receptor 4	Agonists: Glutamate L-AP4 LSP2-9166 PHCCC VU-001,171 VU-0155,041; Positive allosteric modulators: Foliglurax MPEP Antagonists: CPPG MAP4 MPPG MSOP MTPG UBP-1112
mGluR₆Tooltip Metabotropic glutamate receptor 6	Agonists: Glutamate L-AP4 Antagonists: CPPG MAP4 MPPG MSOP MTPG UBP-1112
mGluR₇Tooltip Metabotropic glutamate receptor 7	Agonists: AMN082 Glutamate L-AP4 LSP2-9166 Antagonists: CPPG MAP4 MMPIP MPPG MSOP MTPG UBP-1112 XAP044; Negative allosteric modulators: ADX71743
mGluR₈Tooltip Metabotropic glutamate receptor 8	Agonists: DCPG Glutamate L-AP4; Positive allosteric modulators: AZ12216052 Antagonists: CPPG MAP4 MPPG MSOP MTPG UBP-1112

See also: Receptor/signaling modulators • Ionotropic glutamate receptor modulators • Glutamate metabolism/transport modulators

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