5-HT1A receptor activation contributes to ziprasidone-induced dopamine release in the rat prefrontal cortex

  title={5-HT1A receptor activation contributes to ziprasidone-induced dopamine release in the rat prefrontal cortex},
  author={Hans Rollema and Yi Lu and Anne W. Schmidt and Jeffrey S. Sprouse and Stevin H. Zorn},
  journal={Biological Psychiatry},
  • H. Rollema, Yi Lu, S. Zorn
  • Published 1 August 2000
  • Biology, Psychology, Medicine
  • Biological Psychiatry

5‐HT2A and D2 receptor blockade increases cortical DA release via 5‐HT1A receptor activation: a possible mechanism of atypical antipsychotic‐induced cortical dopamine release

The results suggest that the atypical APDs via 5‐HT2A and D2 receptor blockade, regardless of intrinsic 5-HT1A affinity, may promote the ability of 5- HT1A receptor stimulation to increase mPFC DA release, and provide additional evidence that coadministration of 5‐ HT2A antagonists and typical APDs, which are D2 antagonists, may facilitate 5‐ht1A agonist activity.

Novel antipsychotics activate recombinant human and native rat serotonin 5-HT1A receptors: affinity, efficacy and potential implications for treatment of schizophrenia.

The data indicate that aripiprazole has low efficacy and modest affinity at 5-HT1A receptors, whereas bifeprunox has low affinity but high efficacy, and SSR181507 has intermediate efficacy but high affinity, and is likely to have more prominent 5- HT1A receptor agonist properties.

Occupancy of Agonist Drugs at the 5-HT1A Receptor

It is concluded that 5-HT1A receptor agonists produce detectable occupancy only at higher doses that would produce unacceptable levels of side effects in man, although lower doses are sufficient to produce pharmacological effects.

Differential Effects of Antipsychotic Drugs on Serotonin-1A Receptor-Mediated Disruption of Prepulse Inhibition

Little in vivo interaction is shown of several atypical antipsychotic drugs with the disruption of PPI mediated by 5-HT1A receptor stimulation, which suggests a major involvement of dopamine D2 receptors in this effect, possibly downstream from the initial serotonergic stimulation.

Putative antipsychotics with pronounced agonism at serotonin 5-HT1A and partial agonist activity at dopamine D2 receptors disrupt basal PPI of the startle reflex in rats

It is demonstrated that some putative antipsychotics with pronounced 5-HT1A agonists activity, coupled with partial agonist activity at DA D2 receptors, markedly diminish PPI of the startle reflex in rats, raising the issue of the influence of such compounds on sensorimotor gating in humans.

Role of serotonin-1A receptors in the action of antipsychotic drugs: comparison of prepulse inhibition studies in mice and rats and relevance for human pharmacology

The present PPI results suggest that 5-HT1A receptors are involved in the action of some antipsychotic drugs in mice, and downstream dopamine D2 receptor activation seems to be an important mediator.

Dopamine release induced by atypical antipsychotics in prefrontal cortex requires 5-HT(1A) receptors but not 5-HT(2A) receptors.

Results indicate that (1) 5-HT(1A)Rs are necessary for the APD-induced elevation in cortical DA transmission, and (2) this effect does not require 5- HT(2A)R blockade by APDs.



Ziprasidone (CP-88,059): a new antipsychotic with combined dopamine and serotonin receptor antagonist activity.

The prediction of antipsychotic efficacy without severe motor side effects is supported by the relatively weak potency of ziprasidone to produce catalepsy in animals, contrasted with its potent antagonism of conditioned avoidance responding and dopamine agonist-induced locomotor activation and stereotypy.

Ritanserin administration potentiates amphetamine-stimulated dopamine release in the rat prefrontal cortex

  • E. PehekY. Bi
  • Biology, Psychology
    Progress in Neuro-Psychopharmacology and Biological Psychiatry
  • 1997

BIMG 80, a Novel Potential Antipsychotic Drug: Evidence for Multireceptor Actions and Preferential Release of Dopamine in Prefrontal Cortex

BIMG 80 appears to be a potential antipsychotic compound active on negative symptoms of schizophrenia with a low incidence of extrapyramidal side effects.