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Chemical compound
GRN-529
(4-(Difluoromethoxy)-3-(pyridin-2-ylethynyl)phenyl)(5H -pyrrolo[3,4-b]pyridin-6(7H )-yl)methanone
CAS Number
PubChem
CID
IUPHAR/BPS
ChemSpider
UNII
Formula C 22 H 15 F 2 N 3 O 2
Molar mass 391.378 g·mol−1 3D model (
JSmol )
O=C(N1CC(C=CC=N2)=C2C1)C3=CC(C#CC4=CC=CC=N4)=C(OC(F)F)C=C3
InChI=1S/C22H15F2N3O2/c23-22(24)29-20-9-7-16(12-15(20)6-8-18-5-1-2-10-25-18)21(28)27-13-17-4-3-11-26-19(17)14-27/h1-5,7,9-12,22H,13-14H2
Key:JITMSIRHBAVREW-UHFFFAOYSA-N
GRN-529 is a drug that was developed by
Wyeth as a
negative allosteric modulator of the
metabotropic glutamate receptor 5 (mGluR5).
[1]
A study conducted by
Pfizer found that GRN-529 reduced repetitive behaviors without sedation and partially increased sociability in mouse models of autism.
[2]
Another study conducted by Pfizer found a therapeutically relevant effect in
animal models of depression . It is theorized to work by reducing glutamate receptor hyperactivity.
[3]
See also
References
^
US 2010273772 , O'Neil SV, Zegarelli BJ, Springer DM, Li DZ, "Bisaryl Alkynylamides as Negative Allosteric Modulators of Metabotropic Glutamate Receptor 5 (MGLUR5)", published 28 October 2010, assigned to Wyeth
^
Silverman JL, Smith DG, Rizzo SJ, Karras MN, Turner SM, Tolu SS, et al. (April 2012).
"Negative allosteric modulation of the mGluR5 receptor reduces repetitive behaviors and rescues social deficits in mouse models of autism" . Science Translational Medicine . 4 (131): 131ra51.
doi :
10.1126/scitranslmed.3003501 .
PMC
4904784 .
PMID
22539775 .
^ Hughes ZA, Neal SJ, Smith DL, Sukoff Rizzo SJ, Pulicicchio CM, Lotarski S, et al. (March 2013). "Negative allosteric modulation of metabotropic glutamate receptor 5 results in broad spectrum activity relevant to treatment resistant depression". Neuropharmacology . 66 : 202–14.
doi :
10.1016/j.neuropharm.2012.04.007 .
PMID
22551786 .
S2CID
26417328 .
External links
"GRN-529" . Adis Insight . Springer Nature Switzerland AG.
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