Pharmacological characterization of the vesamicol analogue (+)-[125I]MIBT in primate brain

Julie K. Staley, Deborah C. Mash, Stanley M. Parsons, Anil B. Khare, Simon M.N. Efange

Research output: Contribution to journalArticle

11 Scopus citations

Abstract

The vesamicol analogue, meta-[125I]iodobenzyltrozamicol [(+)-[125I]MIBT] was evaluated as a probe for the in vitro labeling of the vesicular acetylcholine transporter in primate brain. In the striatum, (+)-[125I]MIBT bound a single high-affinity site with a K(d) value of 4.4 ± 0.7 nM. Competition for (+)-[125I]MIBT binding to the striatum by a group of vesamicol analogues displayed a pharmacological profile similar to the rank order of potency previously observed for the vesicular acetylcholine transporter on Torpedo synaptic vesicles. High-affinity binding of(+)-[125I]MIBT in the occipital cortex was characterized by a K(d) value of 4.6 ± 1.1 nM. However, the rank order of potency for inhibition of(+)-[125I]MIBT binding to the occipital cortex by the same test compounds differed from that observed in the striatum. The results suggest that(+)-[125I]MIBT is a reliable probe of the vesicular acetylcholine transporter in primate striatum, but its binding in primate occipital cortex is more complex.

Original languageEnglish (US)
Pages (from-to)159-169
Number of pages11
JournalEuropean Journal of Pharmacology
Volume338
Issue number2
DOIs
StatePublished - Nov 5 1997

Keywords

  • Acetylcholine
  • Acetylcholine transporter
  • Synaptic vesicle
  • Vesamicol receptor
  • Vesicular

ASJC Scopus subject areas

  • Cellular and Molecular Neuroscience
  • Pharmacology

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