In vivo studies with [125I]5-I-A-85380, a nicotinic acetylcholine receptor radioligand

D. Bruce Vaupel, Alexey G. Mukhin, Alane S. Kimes, Andrew G. Horti, Andrei O. Koren, Edythe D. London

Research output: Contribution to journalArticlepeer-review

37 Scopus citations


5-[125I]iodo-3-(2(S)-azetidinylmethoxy)pyridine ([125I]5-I-A- 85380) was evaluated in the mouse as a potential in vivo imaging ligand for central nicotinic acetylcholine receptors (nAChRs). After i.v. administration of [125I]5-I-A-85380, peak brain levels of radioactivity were measured within 1 h and declined slowly over 4 h. [125I]5-I-A-85380 binding was saturable, and both its pharmacology, based upon inhibition studies, and its pattern of accumulation in brain regions having high nAChR densities were consistent with an interaction at α4β2 nAChR agonist binding sites. The thalamus:cerebellum radioactivity ratio, a measure of specific labeling, reached 37. Therefore, radiolabeled 5-I-A-85380 has excellent potential as an imaging radiotracer for nAChRs, particularly with single photon emission computed tomography, when 123I is incorporated into the molecule.

Original languageEnglish (US)
Pages (from-to)2311-2317
Number of pages7
Issue number10
StatePublished - Jul 13 1998
Externally publishedYes


  • 5-I-A-85380
  • Autoradiography
  • In vivo binding
  • Nicotine
  • Nicotinic acetylcholine receptor
  • Radiotracer

ASJC Scopus subject areas

  • Neuroscience(all)


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