AZD9272
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Formula | C14H6F2N4O |
Molar mass | 284.226 g·mol−1 |
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AZD 9272 is a drug which acts as a selective antagonist for the metabotropic glutamate receptor subtype mGluR5.[1] It was unsuccessful in human trials as an analgesic,[2] but continues to be widely used in research especially as its radiolabelled forms.[3][4][5][6]
See also
References
- ↑ 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.
- ↑ 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.
- ↑ 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.
- ↑ Varnäs K, Juréus A, Finnema SJ, Johnström P, Raboisson P, Amini N, et al. (June 2018). "The metabotropic glutamate receptor 5 radioligand [11C]AZD9272 identifies unique binding sites in primate brain". Neuropharmacology. 135: 455–463. doi:10.1016/j.neuropharm.2018.03.039. PMID 29608920.
- ↑ 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.
- ↑ 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: 18F-AZD9272". ACS Chemical Neuroscience. 11 (7): 1048–1057. doi:10.1021/acschemneuro.9b00680. PMC 7309225. PMID 32167745.
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