Chemistry:AZD9272
From HandWiki
Short description: Medication
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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
- ↑ "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. November 2012. doi:10.1016/j.bmcl.2012.08.100. PMID 23046966.
- ↑ "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. November 2013. doi:10.1002/j.1532-2149.2013.00327.x. PMID 23650072.
- ↑ "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. August 2014. doi:10.1124/jpet.114.215137. PMID 24876235.
- ↑ "The metabotropic glutamate receptor 5 radioligand [11C]AZD9272 identifies unique binding sites in primate brain". Neuropharmacology 135: 455–463. June 2018. doi:10.1016/j.neuropharm.2018.03.039. PMID 29608920.
- ↑ "The pro-psychotic metabotropic glutamate receptor compounds fenobam and AZD9272 share binding sites with monoamine oxidase-B inhibitors in humans". Neuropharmacology 162: 107809. January 2020. doi:10.1016/j.neuropharm.2019.107809. PMID 31589885.
- ↑ "Synthesis, Biodistribution, and Radiation Dosimetry of a Novel mGluR5 Radioligand: 18F-AZD9272". ACS Chemical Neuroscience 11 (7): 1048–1057. April 2020. doi:10.1021/acschemneuro.9b00680. PMID 32167745.
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