Differential discrimination of G-protein coupling of serotonin(1A) receptors from bovine hippocampus by an agonist and an antagonist

K. G. Harikumar, Amitabha Chattopadhyay

Research output: Contribution to journalArticle

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Abstract

We have studied the effect of guanosine-5'-O-(3-thiotriphosphate) (GTP-γ-S), a non-hydrolyzable analogue of GTP, on agonist and antagonist binding to bovine hippocampal 5-hydroxytryptamine (5-HT)(1A) receptor in native membranes. Our results show that the specific binding of the agonist is inhibited with increasing concentrations of GTP-γ-S along with a reduction in binding affinity. In sharp contrast to this, antagonist binding to 5-HT(1A) receptor shows no significant reduction and remains invariant over a large range of GTP-γ-S concentrations. The binding affinity of the antagonist also remains unaltered. This shows that the agonist and the antagonist differentially discriminate G-protein coupling of 5-HT(1A) receptors from bovine hippocampus. Copyright (C) 1999 Federation of European Biochemical Societies.

Original languageEnglish (US)
Pages (from-to)389-392
Number of pages4
JournalFEBS Letters
Volume457
Issue number3
DOIs
StatePublished - Sep 3 1999

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Keywords

  • 4-(2'-Methoxy)-phenyl-1-(2'-(N-2''-pyridinyl)-p-fluorobenzamido)ethyl-piperazine
  • 5-Hydroxytryptamine(1A) receptor
  • 8-Hydroxy-2-(di-N-propylamino)tetralin
  • Bovine hippocampus
  • G-protein coupling
  • Guanosine-5'-O-(3-thiotriphosphate)

ASJC Scopus subject areas

  • Biophysics
  • Structural Biology
  • Biochemistry
  • Molecular Biology
  • Genetics
  • Cell Biology

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