title: Pharmacokinetics and dosimetry of iodine-123 labelled PE2I in humans, a radioligand for dopamine transporter imaging.
abstract: The iodine-123 labelled selective ligand N-(3-iodoprop-2E-enyl)-2-beta-carbomethoxy-3beta-(4-methylphenyl) nortropane ([123I]PE2I) was evaluated as a probe for in vivo dopamine transporter imaging in the human brain. Six healthy subjects were imaged with a high-resolution single-photon emission tomography scanner. Striatal radioactivity peaked at 1 h after injection. The background radioactivity was low. The volume of distribution in the striatum was 94+/-24 ml/ml. The results were compared with those of [123I]beta-CIT imaging. There was no significant uptake of [123I]PE2I in serotonin-rich regions such as the midbrain, hypothalamus and anterior gingulus, suggesting that in vivo binding is specific for the dopamine transporter. One main polar metabolite of [123I]PE2I was found in plasma, and the parent plasma concentration decayed rapidly. Radiation exposure to the study subject is 0.022+/-0.004 mSv/MBq (effective dose). The preliminary results suggest that [123I]PE2I is a selective SPET ligand for imaging striatal dopamine transporter density.
authors.affiliation: Department of Clinical Physiology, Kuopio University Hospital, FIN-70210 Kuopio, Finland.
authors.forename: J T
authors.initials: JT
authors.lastname: Kuikka
authors.forename: J L
authors.initials: JL
authors.lastname: Baulieu
authors.forename: J
authors.initials: J
authors.lastname: Hiltunen
authors.forename: C
authors.initials: C
authors.lastname: Halldin
authors.forename: K A
authors.initials: KA
authors.lastname: Bergström
authors.forename: L
authors.initials: L
authors.lastname: Farde
authors.forename: P
authors.initials: P
authors.lastname: Emond
authors.forename: S
authors.initials: S
authors.lastname: Chalon
authors.forename: M
authors.initials: M
authors.lastname: Yu
authors.forename: T
authors.initials: T
authors.lastname: Nikula
authors.forename: T
authors.initials: T
authors.lastname: Laitinen
authors.forename: J
authors.initials: J
authors.lastname: Karhu
authors.forename: E
authors.initials: E
authors.lastname: Tupala
authors.forename: T
authors.initials: T
authors.lastname: Hallikainen
authors.forename: V
authors.initials: V
authors.lastname: Kolehmainen
authors.forename: L
authors.initials: L
authors.lastname: Mauclaire
authors.forename: B
authors.initials: B
authors.lastname: Maziere
authors.forename: J
authors.initials: J
authors.lastname: Tiihonen
authors.forename: D
authors.initials: D
authors.lastname: Guilloteau
mesh_terms: D000328:Adult; D001921:Brain / Q000000981:diagnostic imaging* / Q000378:metabolism; D002352:Carrier Proteins / Q000378:metabolism*; D003042:Cocaine / Q000031:analogs & derivatives / Q000493:pharmacokinetics; D003342:Corpus Striatum / Q000000981:diagnostic imaging / Q000378:metabolism; D004298:Dopamine / Q000378:metabolism*; D050483:Dopamine Plasma Membrane Transport Proteins; D005260:Female; D006801:Humans; D007457:Iodine Radioisotopes; D008297:Male; D008562:Membrane Glycoproteins; D026901:Membrane Transport Proteins; D009419:Nerve Tissue Proteins; D009662:Nortropanes / Q000493:pharmacokinetics; D011829:Radiation Dosage; D015899:Tomography, Emission-Computed, Single-Photon
chemical_list: D002352:Carrier Proteins; D050483:Dopamine Plasma Membrane Transport Proteins; D007457:Iodine Radioisotopes; D008562:Membrane Glycoproteins; D026901:Membrane Transport Proteins; C113010:N-(3-iodoprop-2-enyl)-2-beta-carbomethoxy-3-(4-methylphenyl)nortropane; D009419:Nerve Tissue Proteins; D009662:Nortropanes; C069723:2beta-carbomethoxy-3beta-(4-iodophenyl)tropane; D003042:Cocaine; D004298:Dopamine