Affordable Access

Publisher Website

Lu 28-179 labels a σ2-site in rat and human brain

Authors
Journal
Neuropharmacology
0028-3908
Publisher
Elsevier
Publication Date
Volume
43
Issue
1
Identifiers
DOI: 10.1016/s0028-3908(02)00071-0
Keywords
  • Sigma-2 Binding Site
  • Autoradiography
  • Anxiety
  • Siramesine

Abstract

Abstract 1′-[4-[1-(4-Fluorophenyl)-1 H-indol-3-yl]-1-butyl]spiro[isobenzofuran-1(3H),4′-piperidine] (Lu 28-179) or Siramesine is a σ-ligand with high specificity for σ 2-sites, has been tritiated to directly label these sites in brain. [ 3H]Lu 28-179 bound in a saturable manner to homogenates prepared from rat brain or human cortices with high affinity ( K d=2.2 and 1.1 nM, respectively) and moderate capacity ( B max=50±12 and 26±3 fmol mg tissue −1, respectively). The rank order of affinity for [ 3H]Lu 28-179 binding to homogenates from human and rat brain was: Lu 28-179>ifenprodil=haloperidol>1,3-di(2-tolyl)-guanidine (DTG)>(−)pentazocine≫(+)pentazocine. Using in vitro receptor autoradiography to rat brain sections [ 3H]Lu 28-179 binding was shown to be most predominant in the cerebral cortex, piriform cortex, hippocampal formation (CA1–CA3 and dentate gyrus), superior colliculus, molecular layer of the cerebellar cortex and locus coeruleus. Overall, these data are consistent with [ 3H]Lu 28-179 labelling a σ 2-like binding site.

There are no comments yet on this publication. Be the first to share your thoughts.

Statistics

Seen <100 times
0 Comments

More articles like this

Is the σ2receptor in rat brain related to the K+ch...

on European Journal of Pharmacolo... Jan 01, 1993

A multipartite interaction betweenSalmonellatransc...

on Journal of Molecular Biology Jan 01, 2001

Effects of neurosteroids on ischemia–reperfusion i...

on European Journal of Pharmacolo... Jan 01, 2004
More articles like this..