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

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

Research output: Contribution to journalArticle

Abstract

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
JournalNeuroReport
Volume9
Issue number10
StatePublished - Jul 13 1998
Externally publishedYes

Fingerprint

Nicotinic Receptors
Radioactivity
A 85380
Brain
Single-Photon Emission-Computed Tomography
Thalamus
Cerebellum
Binding Sites
Pharmacology
Ligands
5-iodo-3-(2-azetidinylmethoxy)pyridine

Keywords

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

ASJC Scopus subject areas

  • Neuroscience(all)

Cite this

Vaupel, D. B., Mukhin, A. G., Kimes, A. S., Horti, A., Koren, A. O., & London, E. D. (1998). In vivo studies with [125I]5-I-A-85380, a nicotinic acetylcholine receptor radioligand. NeuroReport, 9(10), 2311-2317.

In vivo studies with [125I]5-I-A-85380, a nicotinic acetylcholine receptor radioligand. / Vaupel, D. Bruce; Mukhin, Alexey G.; Kimes, Alane S.; Horti, Andrew; Koren, Andrei O.; London, Edythe D.

In: NeuroReport, Vol. 9, No. 10, 13.07.1998, p. 2311-2317.

Research output: Contribution to journalArticle

Vaupel, DB, Mukhin, AG, Kimes, AS, Horti, A, Koren, AO & London, ED 1998, 'In vivo studies with [125I]5-I-A-85380, a nicotinic acetylcholine receptor radioligand', NeuroReport, vol. 9, no. 10, pp. 2311-2317.
Vaupel DB, Mukhin AG, Kimes AS, Horti A, Koren AO, London ED. In vivo studies with [125I]5-I-A-85380, a nicotinic acetylcholine receptor radioligand. NeuroReport. 1998 Jul 13;9(10):2311-2317.
Vaupel, D. Bruce ; Mukhin, Alexey G. ; Kimes, Alane S. ; Horti, Andrew ; Koren, Andrei O. ; London, Edythe D. / In vivo studies with [125I]5-I-A-85380, a nicotinic acetylcholine receptor radioligand. In: NeuroReport. 1998 ; Vol. 9, No. 10. pp. 2311-2317.
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