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The replacement of a hydrogen atom with a fluorine atom in certain compounds to facilitate passage through the blood–brain barrier, as is desirable in central nervous system pharmaceutical agents, is a common practice due to the corresponding increase in lipophilicity granted by this substitution.

Halogenated amphetamines, including 4-fluoroamphetamine (4-FA), are psychostimulatory designer drugs which inhibit the uptake of monoamine neurotransmitters.  2-Fluoroamphetamine (2-FA) (hydrochloride) is a structural isomer of 4-FA, having the fluorine at the 2, rather than the 4, position. The physiological and toxicological properties of 2-FA are not known.

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