Physiological and pharmacological properties of 5-HT3 receptors--a patch clamp-study

Neuropeptides. 1991 Jul:19 Suppl:25-30. doi: 10.1016/0143-4179(91)90080-3.

Abstract

Whole cell and patch clamp techniques were used to investigate the properties of 5-HT3 receptors of a murine neuroblastoma cell line (N1E-115) and adult rabbit nodose ganglion neurones. In addition, some preliminary results from guinea-pig nodose ganglion neurones are presented. In such cells, voltage-clamped at -60 mV, 5-HT (10 microM) induced an inward current associated with a conductance increase. The results of ion substitution experiments suggest that the 5-HT activated ion channel is permeable to both Na+ and K+ ions with a permeability ratio (PNa/PK) of 0.94 and 0.92 for rabbit nodose ganglion cells and N1E-115 cells respectively. On outside out membrane patches excised from rabbit nodose ganglion neurones, 5-HT (1 microM) activated clearly discernible single channel currents with a conductance of 16.6 +/- 0.7 pS (n = 4). In contrast, fluctuation analysis of 5-HT induced whole cell currents suggests that the single channel conductance of N1E-115 cells is only 0.3 pS, a value some 50 fold lower. The 5-HT-induced whole cell currents recorded from all three preparations were antagonised by the selective 5-HT3 receptor antagonist ondansetron (GR38032F) and by the less selective agents metoclopramide, cocaine and (+)-tubocurarine. However, these preparations demonstrate a differential sensitivity to some antagonists. In particular, (+)-tubocurarine was a potent antagonist in N1E-115 cells (IC50 = 0.85 nM) but was approximately 200 fold (IC50 = 156 nM) and 1200 fold (IC50 = 10 microM) less potent in rabbit and guinea-pig nodose ganglion neurones respectively. Additionally, a novel effect of ketamine (10 microM) to potentiate the 5-HT-induced current of rabbit nodose ganglion neurones is described.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Action Potentials
  • Animals
  • Cocaine / pharmacology
  • Ganglia
  • Guinea Pigs
  • Imidazoles / pharmacology
  • Ion Channels / drug effects
  • Ketamine / pharmacology*
  • Metoclopramide / pharmacology
  • Neuroblastoma
  • Neurons / metabolism*
  • Ondansetron
  • Potassium / metabolism
  • Rabbits
  • Receptors, Serotonin / metabolism*
  • Serotonin / pharmacology*
  • Serotonin Antagonists
  • Sodium / metabolism
  • Tubocurarine / pharmacology
  • Tumor Cells, Cultured

Substances

  • Imidazoles
  • Ion Channels
  • Receptors, Serotonin
  • Serotonin Antagonists
  • Serotonin
  • Ondansetron
  • Ketamine
  • Sodium
  • Cocaine
  • Metoclopramide
  • Potassium
  • Tubocurarine