2-Fluoroamphetamine Explained

2-Fluoroamphetamine (2-FA) is a stimulant drug from the amphetamine family which has been sold as a designer drug.[1] 2-Fluoroamphetamine differs from 3- and 4-fluoroamphetamine in the position of the fluorine atom on the aromatic ring, making them positional isomers of one another. 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.[2] [3]

Pharmacology

Anorexiant dose (amount inhibiting food intake by 50% for 2 hours, given 1 hour earlier) = 15 mg/kg (rat; p.o.).[4]

Analgesic dose (50% inhibition of response to tail-clamp) = 20 mg/kg (mouse; i.p.).[4]

Effect on blood pressure: 0.5 mg/kg (rat; i.v.) produces an increase in BP of 29 mm.[4]

Toxicology

LD50 (mouse; i.p.) = 100 mg/kg.[4]

Legal status

United States

The Federal Analogue Act, 21 U.S.C. § 813, is a section of the United States Controlled Substances Act, allowing any chemical "substantially similar" to an illegal drug (in Schedule I or II) to be treated as if it were also in Schedule I or II, but only if it is intended (ref 1) for human consumption. 2-FA may be considered to be an analog of amphetamine, thus falling under the Federal Analog Act.

China

As of October 2015 2-FA is a controlled substance in China.[5]

See also

Notes and References

  1. Rösner P, Quednow B, Girreser U, Junge T . Isomeric fluoro-methoxy-phenylalkylamines: a new series of controlled-substance analogues (designer drugs) . Forensic Science International . 148 . 2-3 . 143–156 . March 2005 . 15639609 . 10.1016/j.forsciint.2004.05.003 .
  2. Smart BE . Fluorine substituent effects on bioactivity . Journal of Fluorine Chemistry . 109 . 3–11 . 2001 . 10.1016/s0022-1139(01)00375-x.
  3. Ismail FM . Important fluorinated drugs in experimental and clinical use . Journal of Fluorine Chemistry . 118 . 1–2. 27–33 . 2002 . 10.1016/s0022-1139(02)00201-4.
  4. Book: Costa E, Garattini S . 1970 . Amphetamines and Related Compounds . 28 . New York . Raven Press .
  5. Web site: 关于印发《非药用类麻醉药品和精神药品列管办法》的通知 . China Food and Drug Administration . 27 September 2015 . zh . 1 October 2015 . https://web.archive.org/web/20151001222554/http://www.sfda.gov.cn/WS01/CL0056/130753.html . 1 October 2015 . dead .