| 词条 | Fluorophen |
| 释义 |
| IUPAC_name = (1R,9S,13R)-10-[2-(4-fluorophenyl)ethyl]-1,13-dimethyl-10-azatricyclo[7.3.1.02,7]trideca-2,4,6-trien-4-ol | image = Fluorophen structure.svg | CAS_number = 86495-14-9 | ATC_prefix = None | ATC_suffix = | PubChem = 3036297 | ChemSpiderID = 2300351 | C = 22 | H = 26 | F = 1 | N = 1 | O = 1 | molecular_weight = 339.446 g/mol | smiles = Fc1ccc(cc1)CCN4[C@H]3Cc2c(cc(O)cc2)[C@@]([C@H]3C)(CC4)C | StdInChI = 1S/C22H26FNO/c1-15-21-13-17-5-8-19(25)14-20(17)22(15,2)10-12-24(21)11-9-16-3-6-18(23)7-4-16/h3-8,14-15,21,25H,9-13H2,1-2H3/t15-,21-,22+/m0/s1 | StdInChIKey = PUPFATUGTIQBQA-UZQPLGKSSA-N | bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion = | pregnancy_category = | legal_status = | routes_of_administration = }}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] References1. ^1 {{cite journal |vauthors=Rice KC, Konicki PE, Quirion R, Burke TR, Pert CB | title = 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 = Journal of Medicinal Chemistry | volume = 26 | issue = 11 | pages = 1643–5 |date=November 1983 | pmid = 6313921 | doi = 10.1021/jm00365a017| url = }} {{Opioidergics}}{{Nervous-system-drug-stub}}2. ^1 {{cite book | author = Cody Paul Coyne | title = Comparative Diagnostic Pharmacology: Clinical and Research Applications in Living-System Models | url = https://books.google.com/books?id=Kar-JGFMe-AC&pg=PA692 | accessdate = 22 April 2012 | date = 9 January 2008 | publisher = John Wiley & Sons | isbn = 978-0-470-34429-3 | page = 692}} 4 : Benzomorphans|Opioids|Fluoroarenes|Phenols |
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