In vivo electrophysiological assessment of the agonistic properties of flibanserin at pre‐ and postsynaptic 5‐HT1A receptors in the rat brain

  title={In vivo electrophysiological assessment of the agonistic properties of flibanserin at pre‐ and postsynaptic 5‐HT1A receptors in the rat brain},
  author={Lynne E. Rueter and Claude de Montigny and Pierre U. Blier},
Flibanserin (BIMT 17) has been described as a 5‐HT1A agonist with preferential affinity for postsynaptic 5‐HT1A receptors and as a 5‐HT2A antagonist. Indeed, using the forskolin‐stimulated cAMP accumulation technique, flibanserin but not the 5‐HT1A agonists buspirone and 8‐OH‐DPAT had agonistic activity at postsynaptic 5‐HT1A receptors in the cerebral cortex. The present in vivo electrophysiological study investigated the agonistic properties of this novel compound in pre‐ and postsynaptic… 

Electrophysiological examination of the effects of sustained flibanserin administration on serotonin receptors in rat brain

The results suggest that flibanserin could be a therapeutically useful compound putatively endowed with a more rapid onset of antidepressant action.

Ex vivo binding of flibanserin to serotonin 5-HT1A and 5-HT2A receptors.

It is concluded that 5-HT2 antagonism brought about by low doses of flibanserin may reflect functional mechanisms more than receptor-mediated effects.

Flibanserin, a potential antidepressant drug, lowers 5‐HT and raises dopamine and noradrenaline in the rat prefrontal cortex dialysate: role of 5‐HT1A receptors

The results show that the stimulation of 5‐ HT1A receptors plays a major role in the effect of flibanserin on brain extracellular 5‐HT, DA and NA.

Region-dependent effects of flibanserin and buspirone on adenylyl cyclase activity in the human brain.

Findings suggest a region-related action of flibanserin and buspirone on forskolin-stimulated AC activity in human brain.

Behavioral Effects of Flibanserin (BIMT 17)

Pharmacology of flibanserin.

Flibanserin displays antidepressant-like activity in most animal models sensitive to antidepressants and does not display consistent effects in animal models of anxiety and seems to exert potential antipsychotic effects.


  • Biology
  • 2004
Data obtained from in vitro whole-cell patch clamp reording in the rat BNST slice show that exogenous application f 5-hydroxytryptamine (5-HT) evoked a heterogeneous reponse in BN STAL neurons, and fusion of 5-CT into the BnST significantly reduced the acousic startle response, without affecting the general motor activity.

5-hydroxytryptamine1A-like receptor activation in the bed nucleus of the stria terminalis: electrophysiological and behavioral studies.

It is proposed that in response to stressful stimuli, enhanced levels of 5-HT in the BNST AL plays a critical homeostatic role in feedback inhibition of the anxiogenic response to these stimuli.



Electrophysiological evidence for a functional interaction between 5‐HT1A and 5‐HT2A receptors in the rat medial prefrontal cortex: An lontophoretic study

Results confirm and extend the hypothesis that there is an interaction between 5‐HT1A and5‐HT2A receptors in the mPFc at the neuronal level.

Differential Effect of Gepirone on Presynaptic and Postsynaptic Serotonin Receptors: Single‐Cell Recording Studies

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.

Effect of acute and repeated versus sustained administration of the 5-HT1A receptor agonist ipsapirone: electrophysiological studies in the rat hippocampus and dorsal raphe

Long-term administration of ipsapirone most likely increases 5-HT neurotransmission by enhancing the tonic activation of postsynaptic 5- HT1A receptors, and should not alter their therapeutic effectiveness in anxiety and affective disorders.

Effects of the 5-hydroxytryptamine receptor antagonist, BMY 7378, on 5-hydroxytryptamine neurotransmission: electrophysiological studies in the rat central nervous system.

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.

Differential properties of pre- and postsynaptic 5-hydroxytryptamine1A receptors in the dorsal raphe and hippocampus: I. Effect of spiperone.

The i.v. administration of the 5-hydroxytryptamine (5-HT)1A antagonist spiperone did not alter the responsiveness to microiontophoretic applications of 5-HT and 8-OH-DPAT of pyramidal neurons in the CA3 region of the hippocampus, therefore indicating that spiper one does not act as a classical antagonist at these postsynaptic 5- HT1A receptors.

Electrophysiological characterization of 5-hydroxytryptamine2 receptors in the rat medial prefrontal cortex.

Overall the results indicate that DOI predominantly inhibits mPFc cells in a direct manner and this effect is mediated by 5-HT2 receptors.