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Synthesis of an I-123 analog of A-85380 and preliminary SPECT imaging of nicotinic receptors in baboon.

A radiosynthetic method to prepare the nicotinic acetylcholine receptor radioligand (S)-5-[123I]iodo-3-(2-azetidinylmethoxy)pyridine, 5-IA, has been developed. The two-step sequence produced [123I]-5-IA in high radiochemical yield (52%), high radiochemical purity (98%), and high specific radioactivities (> 8,500 mCi/mumol). Preliminary single photon emission computed tomography studies with [123I]-5-IA in baboon demonstrated the appropriate regional localization for a high-affinity nicotinic radioprobe (thalamus > frontal cortex > cerebellum). Pretreatment with cytisine blocked [123I]-5-IA uptake in all brain regions (78-59% reduction), demonstrating the specificity of the radiotracer.[1]

References

  1. Synthesis of an I-123 analog of A-85380 and preliminary SPECT imaging of nicotinic receptors in baboon. Musachio, J.L., Villemagne, V.L., Scheffel, U.A., Dannals, R.F., Dogan, A.S., Yokoi, F., Wong, D.F. Nucl. Med. Biol. (1999) [Pubmed]
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