3-FPM acts as anorepinephrine–dopamine releasing agent with EC50 values of 30 nM and 43 nM, respectively.[3][4] It shows only negligible efficacy as a releaser of serotonin, with an EC50 value of 2558 nM.[3]
3-FPM also inhibits uptake mediated by dopamine transporters and norepinephrine transporters in HEK293 cells with potencies comparable to cocaine (IC50 values <2.5 μM), but with less potent effects at serotonin transporters (IC50 values >80 μM).[4]
At sufficient doses, 3-FPM is capable of reversing monoamine transporters, particularly transporters of the catecholamines dopamine and norepinephrine, and, to a much lesser degree, serotonin transporters, thereby releasing these neurotransmitters from the cytosol into the extracellular space, where they are active.[4]
Evaluation of itsmetabolic pathway revealedN-oxidation, aryl hydroxylation and subsequentO-methylation, alkyl hydroxylation, oxidation, and degradation of the ethyl-bridge yielding theO/N-bis-dealkylated metabolite, combinations thereof and further glucuronidation or sulfations.[5]
In the United States, 3-fluorophenmetrazine is not explicitly illegal at the federal level, but may be considered under thefederal analogue act if intended for consumption as a structural analog of the Schedule II drugPhenmetrazine, but only if intended for human consumption.
On November 16, 2016, it became an illegal substance in the state of Virginia.[6] As of 2019, it is also a schedule I substance in Virginia. Thepositional isomers of 3-fluorophenmetrazine such as 2-fluorophenmetrazine and 4-fluorophenmetrazine are also illegal under Virginia law,[7] but not federal law.[8]
Sweden's public health agency suggested to classify 3-Fluorophenmetrazine as illegal narcotic on June 1, 2015.[9] It was finally classified on October 15, 2015.[10]
3-Fluorophenmetrazine is illegal in Switzerland as of December 2015.[11]
^Bäckberg M, Westerbergh J, Beck O, Helander A (November 2016). "Adverse events related to the new psychoactive substance 3-fluorophenmetrazine - results from the Swedish STRIDA project".Clinical Toxicology.54 (9):819–825.doi:10.1080/15563650.2016.1211288.PMID27491700.S2CID26118285.
^abUS 20130203752, Blough BE, Rothman R, Landavazo A, Page KM, Decker AM, "Phenylmorpholines and analogues thereof", issued 8 August 2013
^Mardal M, Miserez B, Bade R, Portolés T, Bischoff M, Hernández F, Meyer MR (September 2016). "3-Fluorophenmetrazine, a fluorinated analogue of phenmetrazine: Studies on in vivo metabolism in rat and human, in vitro metabolism in human CYP isoenzymes and microbial biotransformation in Pseudomonas Putida and wastewater using GC and LC coupled to (HR)-MS techniques".Journal of Pharmaceutical and Biomedical Analysis.128:485–495.doi:10.1016/j.jpba.2016.06.011.PMID27372653.
