Preparation and biodistribution of [125I]IBZP: a potential CNS D-1 dopamine receptor imaging agent.

International Journal of Radiation Applications and Instrumentation. Part B, Nuclear Medicine and Biology
H F KungR E Ackerhalt

Abstract

Carrier free [125I]IBZP, R-(+)-8-[125I] iodo-2,3,4,5-tetrahydro-3-methyl-5-phenyl-1H-3-benzazepine-7-ol), was prepared from the corresponding uniodinated compound by an oxidative iodination reaction with chloramine-T and sodium [125I]iodide. After purification by column chromatography the desired uptake was obtained with a high purity (greater than 95%). The agent showed good localization in brain after i.v. injection in rats, with an uptake of 2.7, 1.2 and 0.8% dose/organ at 2, 15 and 30 min post injection, respectively. The regional distribution in rat brain, as measured by in vivo autoradiography, displayed a high uptake in the caudate putamen, accumbens nucleus and substantia nigra, regions known to have a high concentration D-1 dopamine receptors. The uptake ratio of striatum/cerebellum increased with time; at 30 s and 2 h after injection the ratio was 1.1 and 5.3, respectively. The specific uptake in the D-1 dopamine receptor regions can be blocked by pretreatment with SCH-23390, a selective D-1 dopamine receptor antagonist (SCH-23390). The corresponding iodine-123 (t1/2 = 13 h, gamma energy 159 keV) labeled agent may be suitable for SPECT imaging of CNS D-1 dopamine receptors.

Citations

Jan 1, 1990·European Journal of Nuclear Medicine·B Mazière, M Mazière
Aug 1, 1993·Journal of Neuroscience Methods·C P LawlerR B Mailman
Jan 1, 1990·International Journal of Radiation Applications and Instrumentation. Part A, Applied Radiation and Isotopes·S M MoerleinM J Welch
Jun 1, 1992·International Journal of Radiation Applications and Instrumentation. Part A, Applied Radiation and Isotopes·H F BeerP A Schubiger
Sep 7, 2007·Cancer Biotherapy & Radiopharmaceuticals·Sotiris Missailidis, Alan Perkins
Jan 1, 1991·Critical Reviews in Clinical Laboratory Sciences·H F Kung

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