I-123 - FP-CIT pharmacokinetics and dosimetry show great potential for the evaluation of dopamine transporter system in clinical routine

Journal Article · Wed May 01 04:00:00 EDT 1996 · Journal of Nuclear Medicine

OSTI ID:447764

Costa, D C; Walker, S; Waddington, W ^[1]

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1. UCL Medical School, London (United Kingdom)

FP-CIT is a N-fluoropropyl analogue of the [2{beta}-carbomethoxy-3{beta}-(4-iodophenyl)tropane] which has been labelled with I-123 and developed as a new marker of the pre-synaptic dopamine transporter system. Its selective uptake in the striatum of non-human primates and human volunteers has been reported with advantageous faster brain kinetics than {beta}-CIT. In this pilot work we studied the whole body imaging kinetics of FP-CIT in one normal volunteer - NV (5, 60, 100, 360 minutes and 24 hours post-injection for 20 minutes each) and a drug-free patient with well established Parkinson`s disease - PD (100 minutes) after intravenous injection of 111 MBq. Both subjects had high resolution brain SPECT at 35 minutes and 3.5 hours post-injection. Percent of whole body uptake (geometric mean of anterior and posterior projections) in different organs, including total brain and basal ganglia shows rapid clearance from blood during the first hour with no significant change from 100 minutes to 24 hours. The basal ganglia uptake is approximately 0.4% of total body from 100 minutes onwards. Striatal uptake (ratio to frontal cortex) is different between subjects, mainly at 3.5 hours and more marked in the putamen: Calculated dosimetry (mSv/MBq) showed E.D.E.-0.034, and total doses to whole body - 0.01, total brain - 0.017, basal ganglia - 0.155, small intestine - 0.06, urinary bladder - 0.05 and liver - 0.03. These data confirm that FP-CIT has acceptable dosimetry with good pharmacokinetics enabling the study of pre-synaptic dopamine transport system in nigrostriatal degeneration with clinical SPECT at 3-4 hrs p.i.

• OSTI ID: 447764
• Report Number(s): CONF-960659--
• Journal Information: Journal of Nuclear Medicine, Journal Name: Journal of Nuclear Medicine Journal Issue: Suppl.5 Vol. 37; ISSN JNMEAQ; ISSN 0161-5505
• Country of Publication: United States
• Language: English

Related Subjects

55 BIOLOGY AND MEDICINE
BASIC STUDIES
56 BIOLOGY AND MEDICINE
APPLIED STUDIES
BRAIN
CLEARANCE
DIAGNOSTIC TECHNIQUES
DOPAMINE
DOSIMETRY
IODINE 123
NERVOUS SYSTEM DISEASES
ORGANIC FLUORINE COMPOUNDS
SINGLE PHOTON EMISSION COMPUTED TOMOGRAPHY
UPTAKE