Fluorophen, or fluorofen, is a fluorinated analogue of phenazocine, an opioid drug of the benzomorphan group, which was developed as a radioligand for the purpose of labeling opioid receptors during PET scans (with 18F).[1][2] Unlike most other benzomorphan derivatives, fluorophen acts as a full agonist of the opioid receptors with preferential affinity for the μ-opioid receptor (approximately 6x that of morphine), similar but slightly lower affinity for the δ-opioid receptor (equipotent to [D-Ala2, D-Leu5]enkephalin), and very low affinity for the κ-opioid receptor.[1][2]
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| Formula | C22H26FNO |
| Molar mass | 339.454 g·mol−1 |
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References
edit- ^ a b Rice KC, Konicki PE, Quirion R, Burke TR, Pert CB (November 1983). "Synthesis and pharmacological characterization of (+/-)-5,9 alpha-dimethyl-2-[2-(4-fluorophenyl)ethyl]-2'-hydroxy-6,7-benzomorphan (fluorophen), a ligand suitable for visualization of opiate receptors in vivo". Journal of Medicinal Chemistry. 26 (11): 1643–5. doi:10.1021/jm00365a017. PMID 6313921.
- ^ a b Cody Paul Coyne (9 January 2008). Comparative Diagnostic Pharmacology: Clinical and Research Applications in Living-System Models. John Wiley & Sons. p. 692. ISBN 978-0-470-34429-3. Retrieved 22 April 2012.
