GRN-529

Chemical compound
GRN-529
Identifiers
  • (4-(Difluoromethoxy)-3-(pyridin-2-ylethynyl)phenyl)(5H-pyrrolo[3,4-b]pyridin-6(7H)-yl)methanone
CAS Number
  • 1253291-12-1 checkY
PubChem CID
  • 59548652
IUPHAR/BPS
  • 6428
ChemSpider
  • 27471591
UNII
  • D77QDV7E9J
Chemical and physical data
FormulaC22H15F2N3O2
Molar mass391.378 g·mol−1
3D model (JSmol)
  • Interactive image
  • O=C(N1CC(C=CC=N2)=C2C1)C3=CC(C#CC4=CC=CC=N4)=C(OC(F)F)C=C3
InChI
  • 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

  • Fenobam
  • MPEP
  • MTEP

References

  1. ^ 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 
  2. ^ 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.
  3. ^ 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.
  • v
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Metabotropic glutamate receptor modulators
Group I
mGluR1Tooltip Metabotropic glutamate receptor 1
mGluR5Tooltip Metabotropic glutamate receptor 5
Group II
mGluR2Tooltip Metabotropic glutamate receptor 2
mGluR3Tooltip Metabotropic glutamate receptor 3
Group III
mGluR4Tooltip Metabotropic glutamate receptor 4
  • Antagonists: CPPG
  • MAP4
  • MPPG
  • MSOP
  • MTPG
  • UBP-1112
mGluR6Tooltip Metabotropic glutamate receptor 6
  • Antagonists: CPPG
  • MAP4
  • MPPG
  • MSOP
  • MTPG
  • UBP-1112
mGluR7Tooltip Metabotropic glutamate receptor 7
  • Antagonists: CPPG
  • MAP4
  • MMPIP
  • MPPG
  • MSOP
  • MTPG
  • UBP-1112
  • XAP044; Negative allosteric modulators: ADX71743
mGluR8Tooltip Metabotropic glutamate receptor 8
  • 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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