Fluradoline (HP 494), a centrally acting analgesic with antidepressant properties: Analgesic pharmacology

✍ Scribed by T. Spaulding; Dr. S. Fielding; M. Ma; D. B. Ellis; W. J. Novick; H. H. Ong

• Publisher: John Wiley and Sons
• Year: 1985
• Tongue: English
• Weight: 571 KB
• Volume: 5
• Category: Article
• ISSN: 0272-4391
• DOI: 10.1002/ddr.430050302

✦ Synopsis

Fluradoline, (HP 494), 2-fluoro-1l-[P-(methylamino)ethylthio]dibenz[b,f]oxepin maleate, was assessed in a variety of antinociceptive testing procedures which are used to predict analgesic efficacy in man. The compound, after oral or systemic administration, effectively attenuated chemical-induced writhing, heat-induced tail flick, pressure-induced clip biting and hypersensitivity, and tail shock-induced lever pressing. When used for comparative purposes, morphine andlor codeine were also active in all tests, while the tricyclic antidepressant, irnipramine, was weakly or not active. The pharmacologic profile differs from that of opiates in that the antinociceptive effect is not reversed by naloxone, and there is no cross tolerance to morphine and no interaction in in vitro binding studies using 3H-naloxone as the ligand. These data show that fluradoline has the potential for clinical effectiveness as an analgesic agent with a unique mechanism of action that differs from those of opiates and irnipramine.