An assessment of the effects of serotonin 6 (5-HT6) receptor antagonists in rodent models of learning

J Pharmacol Exp Ther. 2003 Nov;307(2):682-91. doi: 10.1124/jpet.103.056002. Epub 2003 Sep 15.

Abstract

Antagonists of serotonin 6 (5-HT6) receptors have been reported to enhance cognition in animal models of learning, although this finding has not been universal. We have assessed the therapeutic potential of the specific 5-HT6 receptor antagonists 4-amino-N-(2,6-bis-methylamino-pyrimidin-4-yl)-benzenesulfonamide (Ro 04-6790) and 5-chloro-N-(4-methoxy-3-piperazin-1-yl-phenyl)-3-methyl-2-benzothiophenesulfonamide (SB-271046) in rodent models of cognitive function. Although mice express the 5-HT6 receptor and the function of this receptor has been investigated in mice, all reports of activity with 5-HT6 receptor antagonists have used rat models. In the present study, receptor binding revealed that the pharmacological properties of the mouse receptor are different from the rat and human receptor: Ro 04-6790 does not bind to the mouse 5-HT6 receptor, so all in vivo testing included in the present report was conducted in rats. We replicated previous reports that 5-HT6 receptor antagonists produce a stretching syndrome previously shown to be mediated through cholinergic mechanisms, but Ro 04-6790 and SB-271046 failed to attenuate scopolamine-induced deficits in a test of contextual fear conditioning. We also failed to replicate the significant effects reported previously in both an autoshaping task and in a version of the Morris water maze. The results of our experiments are not consistent with previous reports that suggested that 5-HT6 antagonists might have therapeutic potential for cognitive disorders.

MeSH terms

  • Animals
  • Binding Sites
  • Humans
  • Learning / drug effects*
  • Mastication / drug effects
  • Mice
  • Models, Animal
  • Pyrimidines / pharmacology
  • Rats
  • Rats, Long-Evans
  • Rats, Sprague-Dawley
  • Rats, Wistar
  • Receptors, Serotonin / drug effects
  • Receptors, Serotonin / metabolism*
  • Serotonin Antagonists / pharmacology*
  • Sulfonamides / pharmacology*
  • Thiophenes / pharmacology*
  • Yawning / drug effects

Substances

  • Pyrimidines
  • Receptors, Serotonin
  • Ro 4-6790
  • Serotonin Antagonists
  • Sulfonamides
  • Thiophenes
  • serotonin 6 receptor
  • SB 271046