Tandospirone and its metabolite, 1-(2-pyrimidinyl)-piperazine—II. Effects of acute administration of 1-PP and long-term adminstration of tandospirone on noradrenergic neurotransmission

  title={Tandospirone and its metabolite, 1-(2-pyrimidinyl)-piperazine—II. Effects of acute administration of 1-PP and long-term adminstration of tandospirone on noradrenergic neurotransmission},
  author={Pierre U. Blier and Olivier Louis Curet and Yves JA Chaput and Claude de Montigny},

Evaluation of the alpha 2-adrenoceptor blocking properties of buspirone and ipsapirone in healthy subjects. Relationship with the plasma concentration of the common metabolite 1-(2-pyrimidinyl)-piperazine.

Clonidine decreased blood pressure, heart rate, oral body temperature, salivary excretion, plasma noradrenaline, 3,4-dihydroxyphenylglycol (DHPG) concentrations, increased plasma growth hormone but did not modify plasma insulin and C-peptide concentrations.

Effects of sustained (+/-)pindolol administration on serotonin neurotransmission in rats.

Prolonged administration of (+/-)pindolol by itself is not sufficient to enhance overall 5-HT neurotransmission; pindoll should therefore not be endowed with intrinsic antidepressant activity.

Tandospirone suppresses impulsive action by possible blockade of the 5-HT1A receptor.

Tandospirone could be a therapeutic candidate for impulsivity-related disorders and may be due to the antagonistic action of the 5-HT1A receptor.

Tandospirone activates neuroendocrine and ERK (MAP kinase) signaling pathways specifically through 5-HT1A receptor mechanisms in vivo

The results are the first evidence that systemic 5-HT1A receptor agonist administration produces a rapid increase in p-ERK levels in vivo, providing further insight into the signaling mechanisms of the 5- HT1A receptors.



Effects of buspirone and its metabolite, 1-(2-pyrimidinyl)piperazine, on brain monoamines and their metabolites in rats.

  • R. FullerK. Perry
  • Biology, Chemistry
    The Journal of pharmacology and experimental therapeutics
  • 1989
Both buspirone and 1- PP increased hypothalamic concentrations of 3-methoxy-4-hydroxyphenylethyleneglycol (MHPG) sulfate, the norepinephrine metabolite, the effect being more pronounced with 1-PP but occurring after doses as low as 0.3 mg/kg s.c. with each compound.

1-(2-Pyrimidinyl)-piperazine as active metabolite of buspirone in man and rat.

Results, together with the fact that PmP is biochemically and pharmacologically active, suggest that the metabolite may contribute significantly to the central effects of the parent drug.

Differential blocking actions of idazoxan against the inhibitory effects of 6‐fluoronoradrenaline and clonidine in the rat vas deferens

The failure of idazoxan to block the inhibitory effects of 6‐FNA, while exerting a potent competitive antagonism of clonidine‐induced inhibitory results, supports the proposal that α2‐adrenoceptors may in fact be subdivided into two subclasses, involving imidazoline and phenylethylamine recognition sites.

Presynaptic alpha-2 adrenoceptors play a major role in the effects of idazoxan on cortical noradrenaline release (as measured by in vivo dialysis) in the rat.

The results suggest that the effects of idazoxan on cortical Noradrenaline release are mediated primarily by alpha-2 adrenoceptors on noradrenergic nerve terminals, rather than by those located postsynaptically, somatodendritically or on the terminals of other neuronal inputs to the cerebral cortex.