[3H]L-694,247 labels the 5-HT1D beta receptor in pig caudate membranes

Eur J Pharmacol. 1994 Oct 24;264(2):213-6. doi: 10.1016/0014-2999(94)00527-3.

Abstract

This study, carried out in pig caudate membranes, characterises the radioligand binding site labelled with [3H]L-694,247 (2-[5-[3-(4-methylsulphonylamino)benzyl-1,2,4-oxadiazol-5-yl ]-1H-indole-3 - yl]ethylamine). The affinities of 27 standard compounds are consistent with binding to a 5-HT1D recognition site. In addition the results indicate that, under the assay conditions described, [3H]L-694,247 specifically labels the 5-HT1D beta recognition site since ketanserin and ritanserin display a low affinity consistent with their activities at this subtype of the 5-HT1D receptor.

MeSH terms

  • Animals
  • Binding, Competitive
  • Caudate Nucleus / drug effects
  • Caudate Nucleus / metabolism*
  • Frozen Sections
  • Oxadiazoles / metabolism*
  • Oxadiazoles / pharmacology
  • Radioligand Assay
  • Receptors, Serotonin / drug effects
  • Receptors, Serotonin / metabolism*
  • Serotonin Receptor Agonists / metabolism*
  • Serotonin Receptor Agonists / pharmacology
  • Structure-Activity Relationship
  • Swine
  • Tissue Preservation
  • Tryptamines / metabolism*
  • Tryptamines / pharmacology

Substances

  • Oxadiazoles
  • Receptors, Serotonin
  • Serotonin Receptor Agonists
  • Tryptamines
  • L 694247