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Characterization of Technetium-99m-L,L-ECD for Brain Perfusion Imaging, Part 1: Pharmacology of Technetium-99m ECD in Nonhuman Primates

Medical Products Department, E.I. Du Pont de Nemours & Co., Inc., No. Billerica
New England Deaconess Hospital, Boston, Massachusetts

Correspondence: For reprints contact: Richard C. Walovitch, PhD, Imaging Agents Research, E.I. Du Pont de Nemours Co., Inc., 331 Treble Cove Rd., No. Billerica, MA 01862.

ABSTRACT

Technetium-99m ethyl cysteinate dimer ([^99mTc]ECD) is a neutral, lipophilic complex which rapidly crosses the blood-brain barrier. Brain retention and tissue metabolism of [^99mTc]ECD is dependent upon the stereochemical configuration of the complex. While both L,L and D,D enantiomers are extracted by the brain, only the L,L but not the D,D form, is metabolized and retained in the monkey brain (4.7% injected dose initially, T > 24 hr). Dynamic single photon emission computed tomography imaging studies in one monkey indicates ^99mTc-L,L-ECD to be distributed in a pattern consistent with regional cerebral blood flow for up to 16 hr postinjection. Dual-labeled ^99mTc-L,L-ECD and [¹⁴C]iodoantipyrine autoradiography studies performed 1 hr after administration show cortical gray to white matter ratios of both isotopes to be equivalent (4–5:1). These data suggest that ^99mTc-L,L-ECD will be useful for the scintigraphic assessment of cerebral perfusion in humans.

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