Effects of serotonin and metergoline on 125[I]-iodocyanopindolol binding parameters to beta-adrenergic receptors in rat brain

George N M Gurguis, Jukka Turkka, Markku Linnoila

Research output: Contribution to journalArticlepeer-review

5 Scopus citations


Most ligands which have been employed to investigate the regulation of β-adrenergic receptors (βAR) under pathophysiological conditions and in reSponse to pharmacological manipulations have also been shown to have affinity for 5-HT(1B) receptors. We examined the effects of serotonin and metergoline (10 μM) on 125I-iodocyanopindolol (ICYP, 5-100 pM) binding to βAR in rat frontal cortex and hippocampus membranes. In both brain region, the presence of either serotonin or metergoline significantly lowered iodocyanopindolol dissociation constant (K(d)) and maximum binding capacity (B(max)). Isoproterenol displacement curves showed that the decrease in receptor density was primarily due to a significant decrease in the receptors in the low-conformational state. Thus, a significant fraction of the apparent ICYP binding to βAR in the low-conformational state was due to binding to 5- HT(1B) receptors. Neither serotonin nor metergoline had an effect on the agonist isoproterenol dissociation constant from βAR in either conformational state.

Original languageEnglish (US)
Pages (from-to)131-140
Number of pages10
JournalEuropean Neuropsychopharmacology
Issue number2
StatePublished - May 1 1998


  • 5-HT(1B) receptors
  • Antidepressants
  • Beta-adrenergic receptors (βAR)
  • Iodocyanopindolol
  • Metergoline
  • Serotonin

ASJC Scopus subject areas

  • Pharmacology
  • Neurology
  • Clinical Neurology
  • Psychiatry and Mental health
  • Biological Psychiatry
  • Pharmacology (medical)


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