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Iofetamine (123I)

Pair of enantiomers

Pair of enantiomers

85068-76-4 (non-labeled) 95896-48-3 (123I-labeled HCl) | elimination_half-life =

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). 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. In addition, on account of its high lipophilicity, iofetamine rapidly penetrates the blood–brain barrier. Accordingly, though not known to have been reported in the medical literature, iofetamine might have stimulant or entactogen effects. However, it might also be neurotoxic to serotonergic and dopaminergic neurons similarly to other para-halogenated amphetamines.

References

References

  1. (2000). "Index Nominum 2000: International Drug Directory". Taylor & Francis US.
  2. (January 1989). "Iofetamine hydrochloride I 123: a new radiopharmaceutical for cerebral perfusion imaging". DICP: The Annals of Pharmacotherapy.
  3. (1982). "Brain imaging with emission computed tomography and radiolabeled amines". Investigative Radiology.
  4. (October 1980). "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.
  5. (March 1989). "Serotonin uptake in cerebral cortex cultures: imipramine-like inhibition by N-isopropyl-p-iodoamphetamine". Experimental Neurology.
  6. (October 1980). "Development of I-123-labeled amines for brain studies: localization of I-123 iodophenylalkyl amines in rat brain". Journal of Nuclear Medicine.
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substituted-amphetamines serotonin-norepinephrine-dopamine-releasing-agents 4-iodophenyl-compounds radiopharmaceuticals stimulants isopropylamino-compounds
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