Misplaced Pages

AZD9272

Article snapshot taken from Wikipedia with creative commons attribution-sharealike license. Give it a read and then ask your questions in the chat. We can research this topic together.
Medication Pharmaceutical compound
AZD 9272
Identifiers
IUPAC name
  • 3-fluoro-5-benzonitrile
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
ChEMBL
Chemical and physical data
FormulaC14H6F2N4O
Molar mass284.226 g·mol
3D model (JSmol)
SMILES
  • N#Cc1cc(cc(F)c1)c1nc(no1)c1ncc(F)cc1
InChI
  • InChI=1S/C14H6F2N4O/c15-10-1-2-12(18-7-10)13-19-14(21-20-13)9-3-8(6-17)4-11(16)5-9/h1-5,7H
  • Key:RBSPCALDSNXWEP-UHFFFAOYSA-N

AZD 9272 is a drug which acts as a selective antagonist for the metabotropic glutamate receptor subtype mGluR5. It was unsuccessful in human trials as an analgesic, but continues to be widely used in research especially as its radiolabelled forms.

See also


References

  1. Raboisson P, Breitholtz-Emanuelsson A, Dahllöf H, Edwards L, Heaton WL, Isaac M, et al. (November 2012). "Discovery and characterization of AZD9272 and AZD6538-Two novel mGluR5 negative allosteric modulators selected for clinical development". Bioorganic & Medicinal Chemistry Letters. 22 (22): 6974–6979. doi:10.1016/j.bmcl.2012.08.100. PMID 23046966.
  2. Kalliomäki J, Huizar K, Kågedal M, Hägglöf B, Schmelz M (November 2013). "Evaluation of the effects of a metabotropic glutamate receptor 5-antagonist on electrically induced pain and central sensitization in healthy human volunteers". European Journal of Pain. 17 (10): 1465–1471. doi:10.1002/j.1532-2149.2013.00327.x. PMID 23650072. S2CID 26095267.
  3. Swedberg MD, Raboisson P (August 2014). "AZD9272 and AZD2066: selective and highly central nervous system penetrant mGluR5 antagonists characterized by their discriminative effects". The Journal of Pharmacology and Experimental Therapeutics. 350 (2): 212–222. doi:10.1124/jpet.114.215137. PMID 24876235. S2CID 29315210.
  4. Varnäs K, Juréus A, Finnema SJ, Johnström P, Raboisson P, Amini N, et al. (June 2018). "The metabotropic glutamate receptor 5 radioligand [C]AZD9272 identifies unique binding sites in primate brain". Neuropharmacology. 135: 455–463. doi:10.1016/j.neuropharm.2018.03.039. PMID 29608920.
  5. Varnäs K, Cselényi Z, Arakawa R, Nag S, Stepanov V, Moein MM, et al. (January 2020). "The pro-psychotic metabotropic glutamate receptor compounds fenobam and AZD9272 share binding sites with monoamine oxidase-B inhibitors in humans". Neuropharmacology. 162: 107809. doi:10.1016/j.neuropharm.2019.107809. PMID 31589885.
  6. Nag S, Varnäs K, Arakawa R, Jahan M, Schou M, Farde L, Halldin C (April 2020). "Synthesis, Biodistribution, and Radiation Dosimetry of a Novel mGluR5 Radioligand: F-AZD9272". ACS Chemical Neuroscience. 11 (7): 1048–1057. doi:10.1021/acschemneuro.9b00680. PMC 7309225. PMID 32167745.
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
mGluR6Tooltip Metabotropic glutamate receptor 6
mGluR7Tooltip Metabotropic glutamate receptor 7
mGluR8Tooltip Metabotropic glutamate receptor 8
See also: Receptor/signaling modulators • Ionotropic glutamate receptor modulators • Glutamate metabolism/transport modulators


Stub icon

This pharmacology-related article is a stub. You can help Misplaced Pages by expanding it.

Categories: