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

Abstract：

: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.

journal_name

Nucl Med Biol

journal_title

Nuclear medicine and biology

authors

Musachio JL,Villemagne VL,Scheffel UA,Dannals RF,Dogan AS,Yokoi F,Wong DF

doi

10.1016/s0969-8051(98)00101-2

keywords:

subject

Has Abstract

pub_date

1999-02-01 00:00:00

pages

201-7

issue

2

eissn

0969-8051

issn

1872-9614

pii

S0969-8051(98)00101-2

journal_volume

26

pub_type

杂志文章

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