In vitro and ex vivo autoradiographic studies of nicotinic acetylcholine receptors using [18F]fluoronorchloro- epibatidine in rodent and human brain

S. John Gatley, Yu Shin Ding, Dan Brady, Andrew N. Gifford, Stephen L. Dewey, F. Ivy Carroll, Joanna S. Fowler, Nora D. Volkow

Research output: Contribution to journalArticlepeer-review

27 Scopus citations

Abstract

A fluorine-18-labeled analog of the potent nicotinic agonist epibatidine is a candidate radioligand for positron emission tomographic (PET) studies of nicotinic acetylcholine receptors (nAcChR). Following intravenous administration of [18SF]exo-2-(2'-fluoro-5'-pyridinyl)-7- azabicyclo[2.2.1]heptane (NFEP), high uptake in thalamus was visualized in sections of mouse and rat brain by autoradiography using a phosphor imaging device. Binding of [18F]NFEP to rat thalamic homogenate was consistent with a single class of binding site with a Kd value of 71 pM. In vitro autoradiography of thaw-mounted sections of human thalamus revealed a heterogeneous pattern of binding; Bmax values for ventrolateral nucleus, insular cortex and dorsomedial nucleus, and internal capsule were 20, 8, and 3 pmol/cc of tissue, respectively. However, similar Kd values close to 50 pM were calculated for all regions. These studies support the suitability of [18F]NFEP as a radioligand for PET studies of nAcChR in the living human brain.

Original languageEnglish
Pages (from-to)449-454
Number of pages6
JournalNuclear Medicine and Biology
Volume25
Issue number5
DOIs
StatePublished - Jul 1998
Externally publishedYes

Keywords

  • Epibatidine
  • Fluorine-18
  • Nicotinic receptor
  • Phosphor imaging
  • Thalamus

Fingerprint

Dive into the research topics of 'In vitro and ex vivo autoradiographic studies of nicotinic acetylcholine receptors using [18F]fluoronorchloro- epibatidine in rodent and human brain'. Together they form a unique fingerprint.

Cite this