From Wikipedia, the free encyclopedia
Chemical compound
XAP044
7-hydroxy-3-(4-iodophenoxy)-4H-chromen-4-one
CAS Number
PubChem
CID
IUPHAR/BPS
ChemSpider
Formula C 15 H 9 I O 4
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
^ 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 .
Group I
mGluR1 Tooltip Metabotropic glutamate receptor 1
mGluR5 Tooltip Metabotropic glutamate receptor 5
Group II
mGluR2 Tooltip Metabotropic glutamate receptor 2
mGluR3 Tooltip Metabotropic glutamate receptor 3
Group III
mGluR4 Tooltip Metabotropic glutamate receptor 4
mGluR6 Tooltip Metabotropic glutamate receptor 6
mGluR7 Tooltip Metabotropic glutamate receptor 7
mGluR8 Tooltip Metabotropic glutamate receptor 8