Determination of the molecular size of the 5-HT3 receptor binding site by radiation inactivation

Eur J Pharmacol. 1989 Dec 5;172(6):497-500. doi: 10.1016/0922-4106(89)90033-3.

Abstract

The radiation inactivation technique has been used to estimate the molecular size of the 5-HT3 receptor binding site labelled by [3H]zacopride, in comparison with that of the 5-HT1A receptor binding site labelled by [3H]8-OH-DPAT, in rat cortical membranes. The calculated molecular weight of the 5-HT3 site: 35.4 +/- 2.2 kDa (mean +/- S.E.M., n = 4) was significantly less than that of the 5-HT1A site: 62.9 +/- 1.8 kDa (mean +/- S.E.M., n = 4) and of other 5-HT1 and 5-HT2 receptors of the G-protein coupled family. These data further support that the 5-HT3 receptor is not coupled to G-proteins in the rat brain.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • 8-Hydroxy-2-(di-n-propylamino)tetralin
  • Animals
  • Benzamides / pharmacology
  • Bridged Bicyclo Compounds / pharmacology
  • Bridged Bicyclo Compounds, Heterocyclic*
  • Cerebral Cortex / drug effects
  • Cerebral Cortex / metabolism
  • Cerebral Cortex / radiation effects
  • In Vitro Techniques
  • Kinetics
  • Male
  • Molecular Weight
  • Rats
  • Rats, Inbred Strains
  • Receptors, Serotonin / analysis
  • Receptors, Serotonin / metabolism*
  • Receptors, Serotonin / radiation effects
  • Tetrahydronaphthalenes / metabolism

Substances

  • Benzamides
  • Bridged Bicyclo Compounds
  • Bridged Bicyclo Compounds, Heterocyclic
  • Receptors, Serotonin
  • Tetrahydronaphthalenes
  • 8-Hydroxy-2-(di-n-propylamino)tetralin
  • zacopride