Iofetamine (123I) Explained

Iofetamine (iodine-123, ¹²³I), brand names Perfusamine, SPECTamine), or N-isopropyl-(¹²³I)-p-iodoamphetamine (IMP), is a lipid-soluble amine and radiopharmaceutical drug used in cerebral blood perfusion imaging with single-photon emission computed tomography (SPECT).^{[1] [2] [3]} Labeled with the radioactive isotope iodine-123, it is approved for use in the United States as a diagnostic aid in determining the localization of and in the evaluation of non-lacunar stroke and complex partial seizures, as well as in the early diagnosis of Alzheimer's disease.

An analogue of amphetamine, iofetamine has shown to inhibit the reuptake of serotonin and norepinephrine as well as induce the release of these neurotransmitters and of dopamine with similar potencies to other amphetamines like d-amphetamine and p-chloroamphetamine.^{[4] [5]} In addition, on account of its high lipophilicity, iofetamine rapidly penetrates the blood-brain-barrier.^[6] Accordingly, though not known to have been reported in the medical literature, iofetamine likely possesses psychostimulant and possibly entactogenic effects. However, based on structure-activity relationships, it may also be highly neurotoxic to serotonergic and dopaminergic neurons similarly to most other para-halogenated amphetamines.

See also

• p-Iodoamphetamine
• N-Isopropylamphetamine

Notes and References

1. Book: Index Nominum 2000: International Drug Directory . 25 April 2012 . 2000 . Taylor & Francis US . 978-3-88763-075-1 . 562.
2. Druckenbrod RW, Williams CC, Gelfand MJ . Iofetamine hydrochloride I 123: a new radiopharmaceutical for cerebral perfusion imaging . DICP: The Annals of Pharmacotherapy . 23 . 1 . 19–24 . January 1989 . 2655294 . 10.1177/106002808902300103. 1649855 .
3. Holman BL, Hill TC, Magistretti PL . Brain imaging with emission computed tomography and radiolabeled amines . Investigative Radiology . 17 . 3 . 206–15 . 1982 . 6811496 . 10.1097/00004424-198201730-00002.
4. Winchell HS, Horst WD, Braun L, Oldendorf WH, Hattner R, Parker H . N-isopropyl-[123I] p-iodoamphetamine: single-pass brain uptake and washout; binding to brain synaptosomes; and localization in dog and monkey brain ]. Journal of Nuclear Medicine . 21 . 10 . 947–52 . October 1980 . 6775056 .
5. de Jong BM, Feenstra MG, Ruijter JM, van Royen EA . Serotonin uptake in cerebral cortex cultures: imipramine-like inhibition by N-isopropyl-p-iodoamphetamine . Experimental Neurology . 103 . 3 . 297–9 . March 1989 . 2920796 . 10.1016/0014-4886(89)90055-1. 23266659 .
6. Winchell HS, Baldwin RM, Lin TH . Development of I-123-labeled amines for brain studies: localization of I-123 iodophenylalkyl amines in rat brain . Journal of Nuclear Medicine . 21 . 10 . 940–6 . October 1980 . 7420195 .