In vivo evaluation of [123I]-8-[4-[2-(5-Iodothienyl)]-4-oxobutyl]-3-methyl-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one as a potential dopamine D2 receptor radioligand for SPECT

Add time:07/21/2019    Source:sciencedirect.com

[123I]-8-[4-[2-(5-Iodothienyl)]-4-oxobutyl]-3-methyl-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one (1) (Ki D2 = 1.9 nM, Ki 5-HT2D2 = 16.7, log P7.5 = 3.14) has been synthesized as a selective ligand for dopamine D2 receptors. The in vivo distribution of the corresponding radioligand, 123I-1, was studied in male Australian albino Wistar rats. Moderate brain uptake of radio-activity was exhibited (0.39 ± 0.04% ID, 5 min), and the striatum-to-cerebellum ratio reached a maximum of 2.6 at 20 min post-injection. The thyroid uptake increased from 0.21 ± 0.06% ID at 5 min to 9.17 ± 5.94% ID at 2 h post-injection. In spite of its promising in vitro characteristics, the relatively fast clearance of radioactivity from the rat brain, moderate striatum to cerebellum ratios and apparent in vivo deiodination indicate that 123I-1 may not be suitable for in vivo studies of D2 receptors.

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