5049. Iofetamine 123I

Nomenclature

CAS number: 75917-92-9
4-(Iodo-123I)-α-methyl-N-(1-methylethyl)benzeneethanamine; (±)-p-iodo-123I-N-isopropyl-α-methylphenethylamine; [123I](±)-N-isopropyl-p-iodoamphetamine.
C12H18123IN.

Description and references

Lipid soluble radioactive brain imaging agent. Prepn: R. M. Baldwin et al., EP 11858 (1980 to Hoffmann-La Roche); eidem, US 4360511 (1982 to Medi-Physics). Detailed synthesis: L. Carlsen, K. Andresen, Eur. J. Nucl. Med. 7, 280 (1982). Modified synthesis for improved yields: A. Najafi, J. Labelled Compd. Radiopharm. 24, 1167 (1987). Preparative HPLC purification: J. Mertens et al., Nucl. Med. Commun. 5, 705 (1984). Brain uptake and localization: H. S. Winchell et al., J. Nucl. Med. 21, 940 (1980); H. S. Winchell et al., ibid. 947. Distribution kinetics in animals: P. Som et al., Int. J. Nucl. Med. Biol. 12, 185 (1985); in humans: B. L. Holman et al., J. Nucl. Med. 25, 25 (1984). Diagnostic use for cerebral function in Alzheimer's disease: K. A. Johnson et al., Arch. Neurol. 45, 392 (1988). Reviews of radiopharmaceutical production and diagnostic use with single photon emission computed tomography (SPECT) imaging: M. B. Cohen et al., Appl. Radiat. Isot. 37, 749-763 (1986); of diagnostic applications in stroke: C. H. Park et al., RadioGraphics 8, 305-326 (1988); of metabolism and kinetics: R. M. Baldwin, J.-L. Wu, J. Nucl. Med. 29, 122-124 (1988).

Chemical structure

Properties

bp0.05 91-92°. Also reported as bp0.6 98-99° (Najafi).

Derivative

Hydrochloride.

Nomenclature

CAS number: 85068-76-4
IMP; 123I labeled IMP; 123I-M123; Perfusamine (Medi-Physics); Spectamine (Medi-Physics).
C12H18123IN.HCl.

Properties

Crystals from ether, mp 156-158°.

Therapeutic Category

Diagnostic aid (radioactive imaging agent).

Keywords

Diagnostic Aid (Radioactive Imaging Agent)