The mechanism by which the selective 5-HT1A receptor antagonist S-(−)UH 301 produces head-twitches in mice

  title={The mechanism by which the selective 5-HT1A receptor antagonist S-(−)UH 301 produces head-twitches in mice},
  author={Nissar A. Darmani and Sharon L. Reeves},
  journal={Pharmacology Biochemistry and Behavior},

The silent and selective 5-HT1A antagonist, WAY 100635, produces via an indirect mechanism, a 5-HT2A receptor-mediated behaviour in mice during the day but not at night

  • N. Darmani
  • Biology
    Journal of Neural Transmission
  • 1998
It appears that WAY 100635 produces the HTR indirectly via disinhibition of endogenous serotonergic inhibitory tone operating on the somatodenritic pulse-modulating 5-HT1A autoreceptors, which subsequently stimulates postsynaptic 5- HT2A receptors to produce the head-twitch behaviour.

Role of 5-HT2A, 5-HT2C, 5-HT1A and TAAR1 Receptors in the Head Twitch Response Induced by 5-Hydroxytryptophan and Psilocybin: Translational Implications

The key role of 5-HT2AR is confirmed in in the induction of HTR by5-HTP and psilocybin, and the effect of a 5- HT1AR agonist to attenuate HTR and a bimodal contribution of 5 -HT2CR as well as a role of TAAR1 in modulating HTR induced by 5-htP are confirmed.

5-HT1AReceptors Modulate the Consolidation of Learning in Normal and Cognitively Impaired Rats

Data confirm a role for presynaptic 5-HT1A receptors during the consolidation of learning and support the hypothesis that serotonergic, cholinergic, and glutamatergic systems interact in cognitively impaired animals.

The 5-HT1A receptor active compounds (R)-8-OH-DPAT and (S)-UH-301 modulate auditory evoked EEG responses in rats

It is suggested that 5-HT1A signaling is involved in sensory inhibition and support the evaluation of 5- HT1A receptor active compounds in conditions with central filtering deficits, such as schizophrenia.

Evidence for functional interactions between 5-HT1A and 5-HT2A receptors in rat thermoregulatory mechanisms.

The present results provide evidence for functional interactions between 5-HT1A and 5- HT2A receptors in temperature regulation in rats, and also suggest an important role for postsynaptic 4-HT2A/C receptors in the mediation of DOI-induced hyperthermia.

Pharmacological characterization of JNJ-28583867, a histamine H(3) receptor antagonist and serotonin reuptake inhibitor.

Multiple receptors contribute to the behavioral effects of indoleamine hallucinogens



Interaction between a selective 5‐HT1A receptor antagonist and an SSRI in vivo: effects on 5‐HT cell firing and extracellular 5‐HT

Pretreatment with the selective 5‐HT1A receptor antagonist, WAY 100635, blocked the inhibitory effect of paroxetine on5‐HT neuronal activity in the DRN and, at the same time, markedly enhanced the effect ofParoxetines on extracellular 5‐ HT in the FCx.

The citalopram/5-HTP-induced head shake syndrome is correlated to 5-HT2 receptor affinity and also influenced by other transmitters.

The results indicate that 1-5-HTP-induced head shakes are most sensitive to 5-HT2 antagonists, but that the syndrome is influenced by other neuronal systems.

Electrophysiological assessment of putative antagonists of 5-hydroxytryptamine receptors: a single-cell study in the rat dorsal raphe nucleus.

Results indicate that, among the five putative 5-HT receptor antagonists tested, only spiperone can antagonize the suppressant effect of 5-hydroxytryptamine1A (5-HT1A) receptor agonists on the firing of dorsal raphe 5- HT neurons.

Receptor reserve for 5-hydroxytryptamine1A-mediated inhibition of serotonin synthesis: possible relationship to anxiolytic properties of 5-hydroxytryptamine1A agonists.

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.

Do functional relationships exist between 5-HT1A and 5-HT2 receptors?

Electrophysiological responses of serotoninergic dorsal raphe neurons to 5‐HT1A and 5‐HT1B agonists

D dorsal raphe 5‐HT neurons appear highly responsive to 5‐ht1A, but not to 5-HT1B compounds; these findings are discussed with regard to the 5‐ HT receptor subtypes as candidates for the somatodendritic autoreceptor of dorsal raphes neurons.

In vivo microdialysis evidence for central serotonin1A and serotonin1B autoreceptor blocking properties of the beta adrenoceptor antagonist (-)penbutolol.

  • S. HjorthT. Sharp
  • Biology, Chemistry
    The Journal of pharmacology and experimental therapeutics
  • 1993
The data indicate that (-)penbutolol possesses 5-HT1A and 5-ht1B autoreceptor antagonist properties, and may be a useful tool in studies of central 5- HT receptor-mediated function.