Initial evaluation of 123I-5-I-R91150, a selective 5-HT2A ligand for single-photon emission tomography, in healthy human subjects

The mapping of 5-HT2 receptors in the brain using functional imaging techniques has been limited by a relative lack of selective radioligands. Iodine-123 labelled 4-amino-N-[1-[3-(4-fluorophenoxy)propyl]-4-methyl-4-piperidinyl]-5-io do-2-methoxybenzamide (123I-5-I-R91150 or 123I-R93274) is a new lig...

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Bibliographic Details
Published in:European journal of nuclear medicine 1997-02, Vol.24 (2), p.119-124
Main Authors: BUSATTO, G. F, PILOWSKY, L. S, GACINOVIC, S, WADDINGTON, W, LINGFORD-HUGHES, A, KERWIN, R. W, COSTA, D. C, MERTENS, J, TERRIERE, D, ELL, P. J, MULLIGAN, R, TRAVIS, M. J, LEYSEN, J. E, LUI, D
Format: Article
Language:English
Subjects:
Adult
Biological and medical sciences
Brain - diagnostic imaging
Brain - metabolism
Contrast media. Radiopharmaceuticals
Female
Humans
Investigative techniques, diagnostic techniques (general aspects)
Iodine Radioisotopes
Male
Medical sciences
Nervous system
Pharmacology. Drug treatments
Piperidines - pharmacokinetics
Radionuclide investigations
Receptor, Serotonin, 5-HT2A
Receptors, Serotonin - analysis
Tissue Distribution
Tomography, Emission-Computed, Single-Photon
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Summary:The mapping of 5-HT2 receptors in the brain using functional imaging techniques has been limited by a relative lack of selective radioligands. Iodine-123 labelled 4-amino-N-[1-[3-(4-fluorophenoxy)propyl]-4-methyl-4-piperidinyl]-5-io do-2-methoxybenzamide (123I-5-I-R91150 or 123I-R93274) is a new ligand for single-photon emission tomography (SPET), with high affinity and selectivity for 5-HT2A receptors. This study reports on preliminary 123I-5-I-R91150 SPET, whole-body and blood distribution findings in five healthy human volunteers. Maximal brain uptake was approximately 2% of total body counts at 180 min post injection (p.i. ). Dynamic SPET sequences were acquired with the brain-dedicated, single-slice multi-detector system SME-810 over 200 min p.i. Early peak uptake (at 5 min p.i.) was seen in the cerebellum, a region free from 5HT2A receptors. In contrast, radioligand binding in the frontal cortex increased steadily over time, up to a peak at approximately 100-120 min p.i. Frontal cortex-cerebellum activity ratios reached values of 1.4, and remained stable from approximately 100 min p.i. onwards. Multi-slice SPET sequences showed a pattern of regional variation of binding compatible with the autoradiographic data on the distribution of 5-HT2A receptors in humans (cerebral cortex>striatum>cerebellum). These findings suggest that 123I-5-I-R91150 may be used for the imaging of 5-HT2A receptors in the living human brain with SPET.
ISSN:0340-6997