An open study of oral flesinoxan, a 5‐HT1A receptor agonist, in treatment‐resistant depression

  title={An open study of oral flesinoxan, a 5‐HT1A receptor agonist, in treatment‐resistant depression},
  author={Paul Grof and Russell T. Joffe and S. Kennedy and Emmanuel Persad and J Syrotiuk and Dawn Bradford},
  journal={International Clinical Psychopharmacology},
Flesinoxan, a full 5-HT1A, receptor agonist, was administered (4–8 mg) to treatment-resistant depressed patients in an open study. Safety and tolerance of the substance appeared satisfactory. Headache, dizziness and nausea were the most frequently reported side effects. The observations suggested that flesinoxan is an antidepressant agent and that it may be of particular value in some difficult, treatment-resistant depressions. Based on these observations, a double-blind, placebo-controlled… Expand
Effects of the 5-HT1A receptor agonist flesinoxan in panic disorder
The worsening of symptoms seen with the highest dose of flesinoxan is intriguing and might give a clue to the understanding of the mechanism underlying similar effects seen with antidepressants in panic disorder patients. Expand
The effects of the 5-HT1A agonist flesinoxan, in three paradigms for assessing antidepressant potential in the rat
Both doses of flesinoxan significantly reduced the immobility time in the sham and OB groups when compared to their respective controls, and significantly attenuated the 8-OH-DPAT-induced hypothermic response. Expand
Mirtazapine: pharmacology in relation to adverse effects
  • D. Nutt
  • Medicine
  • Acta psychiatrica Scandinavica. Supplementum
  • 1997
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Dual, Postsynaptic 5-HT2B Antagonist and 5-HT1A Agonist Approach to the Treatment of METH/MDMA Addiction and Related Behavioral Disorders. Part 2. Proof of Concept.
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Flesinoxan challenge suggests that chronic treatment with paroxetine in rats does not desensitize receptors controlling 5-HT synthesis
The results presented here suggest a greater effect of flesinoxan on synthesis reduction in rats chronically treated with paroxetine, and that the stimulation of 5-HT(1A) receptors with an agonist is still capable of reducing 5- HT synthesis. Expand
The anxiolytic effects of flesinoxan, a 5-HT1A receptor agonist, are not related to its neuroendocrine effects.
The data show that the anxiolytic effects of flesinoxan in the shock-probe burying paradigm are not related to increases in plasma corticosterone and glucose levels. Expand
Characterization of 5-hydroxytryptamine1A properties of flesinoxan: In Vivo electrophysiology and hypothermia study
The flesinoxan-induced hypothermia was significantly attenuated by prior administration of the non-selective 5-HT1A antagonist pindolol and the 5- HT1/2 antagonist methysergide, suggesting that it may be an effective anxiolytic/ant antidepressant agent. Expand
Effect of sustained administration of the 5-HT1A receptor agonist flesinoxan on rat 5-HT neurotransmission
As for selective 5- HT re-uptake inhibitors, monoamine oxidase inhibitors and 5-HT1A receptor agonists, flesinoxan produced most of the adaptive changes exerted by these antidepressant drugs on the 4-HT system and the marked potency and the long dissociation constant of fles inoxan for the 5-ht1A receptors may account for the latter discrepancy. Expand
Apomorphine-induced emesis in dogs: differential sensitivity to established and novel dopamine D2/5-HT(1A) antipsychotic compounds.
Dogs are very sensitive to the dopaminergic blocking effects of antipsychotics in this model of central D2 receptor activation, and this model can thus be advantageously used to investigate the pharmacological activity of novel D 2 receptor antagonists/partial agonists in dogs. Expand
Effects of Antiglucocorticoid Treatment on 5-HT1A Function in Depressed Patients and Healthy Subjects
This study failed to show that glucocorticoid modulation of 5-HT1A receptor function is altered in depression, as expected, but non-HPA responses to IPS were not enhanced. Expand