In vitro autoradiography of serotonin 5-HT2A/2C receptor-activated G protein: Guanosine-5 `-(gamma-{[}S-35]thio)triphosphate binding in rat brain

  • Adlersberg M
  • Arango V
  • Hsiung S
 et al. 
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Agonist activation of G protein-coupled receptors induces an increase in
the binding of guanosine 5'-(gamma-{[}S-35]thio)triphosphate
({[}S-35]GTP gamma S); this increase in binding has been used as a tool
to investigate receptor interaction with the heterotrimer guanine
nucleotide-binding regulatory protein (G protein), The present study
uses agonist-stimulated {[}S-35]GTP gamma S binding to characterize
serotonin 5-HMT2A/2C receptors in rat brain membrane fractions and
demonstrate the anatomical localization of the receptors by in vitro
autoradiography on slide-mounted sections. The stimulatory effect of the
agonist {[}1-(2,5-dimethoxy-4-iodophenyl)]-2 aminopropane (DOI) is
compared to that of serotonin (5-HT). Autoradiography revealed a similar
localization of DOI- and 5-HT-stimulated binding of {[}S-35]GTP gamma S
in distinct areas of prefrontal and parietal cortex, consistent with
previously reported 5-HT2A receptor distribution. Specific binding was
demonstrated in the frontal and parietal cortex, medial prefrontal, and
cingular and orbital-insular areas as well as in the hippocampal
formation, septal areas, the nucleus accumbens, and the choroid plexus.
MDL 100105, a specific 5-HT2A antagonist, and ketanserin, an antagonist
of 5-HT2A/2C receptors, blocked DOI stimulation in all labeled areas,
whereas 5-HT stimulation was only partially blocked (70-80%). A small
but significant inhibition was observed with the specific antagonist of
5-HT2C/2B SB 206553, This autoradiographic technique provides a useful
tool for measuring in situ changes in specific receptor-Gq protein
coupling in anatomically discrete brain regions, under physiological and
pathological conditions. (C) 2000 Wiley-Liss, Inc.

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  • M Adlersberg

  • V Arango

  • S C Hsiung

  • J J Mann

  • M D Underwood

  • K P Liu

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