The 5-HT1A receptor agonist MKC-242 increases the exploratory activity of mice in the elevated plus-maze

Eur J Pharmacol. 2003 Jan 1;458(1-2):141-4. doi: 10.1016/s0014-2999(02)02786-3.

Abstract

The effect of (S)-5-[3-[(1,4-benzodioxan-2-ylmethyl)amino]propoxy]-1,3-benzodioxole HCl (MKC-242), a 5-HT(1A) receptor agonist, on mouse behavior was examined in the elevated plus-maze. MKC-242 significantly increased the percentage of open-arm entries and the percentage of open-arm time, indices of anxiety reduction, while it did not increase the enclosed-arm entries and time spent in enclosed arms. The effect of MKC-242 was antagonized by a low dose of the 5-HT(1A) receptor antagonist N-[2-[4-(2-methoxyphenyl)-1-piperazinyl]ethyl]-N-(2-pyridinyl)cyclohexanecarboxamide which alone did not affect the behavior. These findings suggest that MKC-242 increases the exploratory activity of mice in the elevated plus-maze via activation of 5-HT(1A) receptors, probably the presynaptic autoreceptors.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anti-Anxiety Agents / pharmacology
  • Behavior, Animal / drug effects
  • Diazepam / pharmacology
  • Dioxanes / pharmacology*
  • Dioxoles / pharmacology*
  • Dose-Response Relationship, Drug
  • Exploratory Behavior / drug effects*
  • Male
  • Maze Learning / drug effects*
  • Mice
  • Motor Activity / drug effects
  • Piperazines / pharmacology
  • Pyridines / pharmacology
  • Receptors, Serotonin / drug effects
  • Receptors, Serotonin / physiology*
  • Receptors, Serotonin, 5-HT1
  • Serotonin Antagonists / pharmacology
  • Serotonin Receptor Agonists / pharmacology*

Substances

  • Anti-Anxiety Agents
  • Dioxanes
  • Dioxoles
  • Piperazines
  • Pyridines
  • Receptors, Serotonin
  • Receptors, Serotonin, 5-HT1
  • Serotonin Antagonists
  • Serotonin Receptor Agonists
  • N-(2-(4-(2-methoxyphenyl)-1-piperazinyl)ethyl)-N-(2-pyridinyl)cyclohexanecarboxamide
  • osemozotan
  • Diazepam