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

@article{Blier1991TandospironeAI,
  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},
  journal={Neuropharmacology},
  year={1991},
  volume={30},
  pages={691-701}
}
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.
TLDR
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.
TLDR
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.
TLDR
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
TLDR
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.
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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.
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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.
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Abstract We have studied the α-adrenoceptor antagonist effects of idazoxan (RX 781094) in extracellular recordings from single locus coeruleus and dorsal raphe neurons of chloral hydrate-anesthetized
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