An investigation of the 5-HT1D receptor binding affinity of 5-hydroxytryptamine, 5-carboxyamidotryptamine and sumatriptan in the central nervous system of seven species

Eur J Pharmacol. 1992 Mar 24;213(2):193-7. doi: 10.1016/0014-2999(92)90681-s.

Abstract

The ability of three 5-HT1 receptor agonists, 5-HT (5-hydroxytryptamine), 5-CT (5-carboxyamidotryptamine) and sumatriptan to inhibit the binding of [3H]5-HT, in the presence of cyanopindolol and mesulergine, from cerebral cortical and/or caudate membranes in seven species (dog, guinea-pig, rabbit, pig, human, hamster and calf) has been investigated. Under the experimental conditions used, 5-CT and sumatriptan consistently yielded displacement curves best fit to a two-site model whereas 5-HT always gave a monophasic displacement curve. The pIC50 values obtained with 5-HT displacement gave a mean of 8.1 +/- 0.1 (mean +/- S.E.M.). In contrast the biphasic displacement curves for 5-CT and sumatriptan yielded high and low affinity pIC50 values of 8.3 +/- 0.1, 5.5 +/- 0.1 and 7.6 +/- 0.1, 5.0 +/- 0.1, respectively. These data indicate that under these experimental conditions the high affinity component labelled by [3H]5-HT is the same receptor subtype, previously denoted the 5-HT1D receptor, in all seven species.

MeSH terms

  • Animals
  • Brain / metabolism*
  • Cattle
  • Caudate Nucleus / metabolism
  • Cerebral Cortex / metabolism
  • Cricetinae
  • Dogs
  • Guinea Pigs
  • Humans
  • Indoles / metabolism*
  • Kinetics
  • Rabbits
  • Radioligand Assay
  • Receptors, Serotonin / metabolism*
  • Serotonin / analogs & derivatives*
  • Serotonin / metabolism*
  • Species Specificity
  • Sulfonamides / metabolism*
  • Sumatriptan
  • Swine

Substances

  • Indoles
  • Receptors, Serotonin
  • Sulfonamides
  • Serotonin
  • Sumatriptan
  • 5-carboxamidotryptamine