Pair of enantiomers
Iofetamine (iodine-123, 123 I), brand names Perfusamine , SPECTamine ), or N -isopropyl-(123 I)-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 .[1] [2]
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.[citation needed ] However, based on structure-activity relationships , it may also be highly neurotoxic to serotonergic and dopaminergic neurons similarly to most other para -halogenated amphetamines.[citation needed ]
See also
References
^ a b Index Nominum 2000: International Drug Directory . Taylor & Francis US. 2000. p. 562. ISBN 978-3-88763-075-1 . Retrieved 25 April 2012 .
^ a b Druckenbrod RW, Williams CC, Gelfand MJ (January 1989). "Iofetamine hydrochloride I 123: a new radiopharmaceutical for cerebral perfusion imaging". DICP: The Annals of Pharmacotherapy . 23 (1): 19–24. doi :10.1177/106002808902300103 . PMID 2655294 . S2CID 1649855 .
^ Holman BL, Hill TC, Magistretti PL (1982). "Brain imaging with emission computed tomography and radiolabeled amines". Investigative Radiology . 17 (3): 206–15. doi :10.1097/00004424-198201730-00002 . PMID 6811496 .
^ Winchell HS, Horst WD, Braun L, Oldendorf WH , Hattner R, Parker H (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 . 21 (10): 947–52. PMID 6775056 .
^ de Jong BM, Feenstra MG, Ruijter JM, van Royen EA (March 1989). "Serotonin uptake in cerebral cortex cultures: imipramine-like inhibition by N-isopropyl-p-iodoamphetamine". Experimental Neurology . 103 (3): 297–9. doi :10.1016/0014-4886(89)90055-1 . PMID 2920796 . S2CID 23266659 .
^ Winchell HS, Baldwin RM, Lin TH (October 1980). "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. PMID 7420195 .
DRAs Tooltip Dopamine releasing agents
NRAs Tooltip Norepinephrine releasing agents
SRAs Tooltip Serotonin releasing agents
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