Antagonist properties of 1-(2-pyrimidinyl)piperazine at presynaptic alpha 2-adrenoceptors in the rat brain

Eur J Pharmacol. 1990 May 3;180(1):183-6. doi: 10.1016/0014-2999(90)90608-9.

Abstract

The effect of 1-(2-pyrimidinyl)piperazine (PmP), the main metabolite of buspirone, was tested on K(+)-evoked [3H]noradrenaline and [3H]serotonin release from superfused synaptosomes obtained from rat cerebral cortex. PmP had no effects per se, but antagonized the effect of noradrenaline, producing a parallel shift to the right of the noradrenaline inhibition curves. From these data pA2 (apparent affinity) values of 6.8 and 7.3 were calculated for PmP on presynaptic alpha 2-adrenoceptors located on noradrenergic and serotonergic nerve terminals, respectively.

MeSH terms

  • Adrenergic alpha-Antagonists / pharmacology*
  • Animals
  • Brain Chemistry / drug effects*
  • Buspirone / analogs & derivatives*
  • Buspirone / pharmacology
  • In Vitro Techniques
  • Male
  • Nerve Endings / drug effects
  • Norepinephrine / antagonists & inhibitors
  • Norepinephrine / metabolism
  • Norepinephrine / pharmacology
  • Potassium / pharmacology
  • Rats
  • Serotonin / metabolism
  • Serotonin / physiology
  • Synapses / drug effects
  • Synaptosomes / drug effects
  • Synaptosomes / metabolism

Substances

  • Adrenergic alpha-Antagonists
  • Serotonin
  • 1-(2-pyrimidinyl)piperazine
  • Potassium
  • Buspirone
  • Norepinephrine