Characterization of 5-hydroxytryptamine1A properties of flesinoxan: In Vivo electrophysiology and hypothermia study

@article{Hadrava1995CharacterizationO5,
  title={Characterization of 5-hydroxytryptamine1A properties of flesinoxan: In Vivo electrophysiology and hypothermia study},
  author={Vratislav Hadrava and Pierre U. Blier and Trevor Dennis and Catherine Ortemann and Claude de Montigny},
  journal={Neuropharmacology},
  year={1995},
  volume={34},
  pages={1311-1326}
}
Flesinoxan is a high affinity and selective 5-hydroxytryptamine1A (5-HT1A) ligand which, unlike the 5-HT1A agonists of the azapirone class, does not generate 1-(2-pyrimidinyl)piperazine, an alpha 2-adrenoreceptor antagonist. In view of potential antidepressant effects of flesinoxan, this study was undertaken to characterize its 5-HT1A properties in the rat brain using in vivo electrophysiology and hypothermia paradigms. The suppressant effect of microiontophoretic applications of flesinoxan on… Expand
Acute Effects of Brexpiprazole on Serotonin, Dopamine, and Norepinephrine Systems: An In Vivo Electrophysiologic Characterization
TLDR
In conclusion, the in vivo action of brexpiprazole on monoamine targets relevant in the treatment of depression and schizophrenia is assessed and α1- and α2-adrenergic receptors are evaluated. Expand
Potentiation by (-)Pindolol of the Activation of Postsynaptic 5-HT1A Receptors Induced by Venlafaxine
TLDR
Results indicate that (-)pindolol potentiated the activation of postsynaptic 5-HT1A receptors resulting from5-HT reuptake inhibition probably by blocking the somatodendritic 5- HT1A autoreceptor, but not its post Synaptic congener. Expand
Effect of a 5-HT1A receptor agonist, flesinoxan, on the extracellular noradrenaline level in the hippocampus and on the locomotor activity of rats
We have studied effects of 5-hydroxytryptamine 1A (5-HT(1A)) receptor-selective compounds on the extracellular noradrenaline (NA) level in the hippocampus of rats using microdialysis and on theirExpand
Effect of sustained administration of the 5-HT1A receptor agonist flesinoxan on rat 5-HT neurotransmission
TLDR
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
The peptidic antidepressant spadin interacts with prefrontal 5-HT4 and mGluR2 receptors in the control of serotonergic function
TLDR
The results indicate that spadin, as a natural compound, constitutes a very good candidate to explore the “glutamatergic path” of fast-acting AD research, and provide the first evidence of 5-HT depolarization block, showing that the combination of5-HT activators for strategies of AD augmentation should be performed with extreme caution. Expand
EMD 68843, a serotonin reuptake inhibitor with selective presynaptic 5-HT1A receptor agonistic properties.
TLDR
The 5-HT1A receptor agonist 8-hydroxy-(di-n-propylamino)tetralin and EMD 68843 are suggested to be a 5- HT1Aceptor agonist selective for presynaptic 5-ht1A receptors. Expand
Effects of a benzodioxan derivative MKC-242 on the firing activity of the dorsal hippocampus CA1 pyramidal neurons in awake and urethane- anaesthetized rats: in vivo electrophysiological evidence for a 5-HT 1A agonistic property.
TLDR
The present results provided the first in vivo electrophysiological evidence that MKC-242, when systemically administered, exerts a 5-HT1A agonistic action at the postsynaptic level. Expand
Modulation of Serotonergic Function in Rat Brain by VN2222, a Serotonin Reuptake Inhibitor and 5-HT1A Receptor Agonist
TLDR
Results show that VN2222 is a mixed 5-HT reuptake inhibitor/5-HT1A agonist that markedly desensitizes 5- HT1A autoreceptors and suggest that it may be a clinically effective dual action antidepressant drug. Expand
F 11440, a potent, selective, high efficacy 5-HT1A receptor agonist with marked anxiolytic and antidepressant potential.
TLDR
F 11440, shown here to be a potent, selective, high efficacy 5-HT1A receptor agonist, appears to have the potential to exert marked anxiolytic and antidepressant activity in humans. Expand
In vivo electrophysiological assessment of the agonistic properties of flibanserin at pre‐ and postsynaptic 5‐HT1A receptors in the rat brain
TLDR
The present in vivo electrophysiological study investigated the agonistic properties of this novel compound in pre‐ and postsynaptic areas of the anesthetized rat brain using local microiontophoretic application and systemic administration and found that flibanserin presented a marked selectivity for post Synaptic 5‐HT1A receptors when applied locally, but not when administered intravenously. Expand
...
1
2
3
4
5
...

References

SHOWING 1-10 OF 37 REFERENCES
Effects of the 5-hydroxytryptamine receptor antagonist, BMY 7378, on 5-hydroxytryptamine neurotransmission: electrophysiological studies in the rat central nervous system.
TLDR
It is concluded that BMY 7378 is an effective antagonist of 5-HT1A receptors in vivo and that the mechanism of its enhancing effect on5-HT transmission at low doses, although still undetermined, is not due to a competitive interaction at the terminal 5- HT autoreceptor. Expand
Behavioral and biochemical effects of the 5-HT1A receptor agonists flesinoxan and 8-OH-DPAT in the rat.
TLDR
The 5-HT1A receptor agonists flesinoxan and 8-hydroxy-2-(di-n-propylamino)tetralin produced a dose-dependent facilitation of male rat ejaculatory behavior and characteristic, dose- dependent effects on spontaneous motor activity, which decreased total locomotor activity and rearing activity but increased forward locomotion and peripheral locomotion. Expand
Induction of hypothermia as a model of 5-hydroxytryptamine1A receptor-mediated activity in the rat: a pharmacological characterization of the actions of novel agonists and antagonists.
TLDR
Hypothermia is a highly specific and sensitive response to activation of postsynaptic 5-HT1A receptors, an interpretation supported by the observation that destruction of central 5- HT neurons with 5,7-dihydroxytryptamine failed to reduce 8-OH-DPAT-induced hypothermia (DIH). Expand
Preferential action of 5-methoxytryptamine and 5-methoxydimethyltryptamine on presynaptic serotonin receptors: A comparative iontophoretic study with LSD and serotonin
Abstract The effects of iontophoretic application of 5-methoxytryptamine (5-MeOT) and 5-methoxy-dimethyltryptamine (5-MeODMT) were studied on serotonin (5-HT)-containing neurones of the mid-brainExpand
Receptor reserve for 5-hydroxytryptamine1A-mediated inhibition of serotonin synthesis: possible relationship to anxiolytic properties of 5-hydroxytryptamine1A agonists.
TLDR
The results suggest that 5- HT1A receptor-mediated regulation of 5-HT synthesis appears to be mediated by somatodendritic autoreceptors on5-HT neurons in the midbrain raphé nuclei, and suggest that these autoreceptor possess a large receptor reserve for agonists. Expand
Comparison of 5-hydroxytryptamine1A-mediated hyperpolarization in CA1 and CA3 hippocampal pyramidal cells.
TLDR
It is concluded that the hyperpolarization elicited by 5-HT in areas CA1 and CA3 is mediated by the 5- HT1A receptor, which may be attributed to differences in receptor-effector number, receptor- effector coupling and/or the structure of the recognition site. Expand
Tandospirone and its metabolite, 1-(2-pyrimidinyl)-piperazine—I. Effects of acute and long-term administration of tandospirone on serotonin neurotransmission
TLDR
It is concluded that desensitization of somatodendritic 5-HT autoreceptors permits5-HT neurones to regain their physiological rate of firing during long-term treatment with tandospirone and, consequently, to release a normal amount of 5- HT into the synaptic cleft. Expand
Central pre- and postsynaptic 5-HT1A receptors in rats treated chronically with a novel antidepressant, cericlamine.
TLDR
The idea that postsynaptic and somatodendritic 5-HT1A receptors are differently regulated in the rat brain is supported, because only the latter receptors desensitized after a long-term blockade of serotonin reuptake by cericlamine is suggested. Expand
Analysis of tandospirone (SM-3997) interactions with neurotransmitter receptor binding sites
TLDR
The primary pharmacological effect of tandospirone appears to be partial agonism at the 5-HT1A receptor, an activity similar to other pyrimidinyl-piperazines which are being developed as novel anxiolytic agents. Expand
Differential Effect of Gepirone on Presynaptic and Postsynaptic Serotonin Receptors: Single‐Cell Recording Studies
TLDR
It is proposed that gepirone, being a partial agonist at postsynaptic 5‐HT1A receptors, fails to desensitize them; whereas, because of its full agonistic activity at the somatodendritic 5‐ HT1A receptor, it desensitizes this autoreceptor with longterm administration. Expand
...
1
2
3
4
...