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

John L. Musachio, Victor L. Villemagne, Ursula A. Scheffel, Robert F. Dannals, A. Semih Dogan, Fuji Yokoi, Dean F. Wong

Research output: Contribution to journalArticle

62 Scopus citations

Abstract

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

Original languageEnglish
Pages (from-to)201-207
Number of pages7
JournalNuclear Medicine and Biology
Volume26
Issue number2
DOIs
StatePublished - Feb 1999
Externally publishedYes

Keywords

  • Iodine-123
  • Nicotinic acetylcholine receptor
  • SPECT

Fingerprint Dive into the research topics of 'Synthesis of an I-123 analog of A-85380 and preliminary SPECT imaging of nicotinic receptors in baboon'. Together they form a unique fingerprint.

  • Cite this