This halogenated hydrocarbon was first synthesized by C. W. Suckling of Imperial Chemical Industries in 1951 and was first used clinically by M. Johnstone in Manchester in 1956.
3-Methylfentanyl was also reported by Russian media as the identity of the anaesthetic "gas" Kolokol-1 (it may have been an aerosol, of a free base dissolved in halothane) used in the Moscow theater hostage crisis in 2002, in which many hostages died from accidental overdoses of the narcotic.