XAP044

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−1
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,^[1] as well as being used to study the role of mGluR₇ in various other processes.^[2]^[3]^[4]

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.

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[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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