The antipsychotic aripiprazole is a potent, partial agonist at the human 5-HT1A receptor.

  title={The antipsychotic aripiprazole is a potent, partial agonist at the human 5-HT1A receptor.},
  author={Shaun Jordan and Vuk Koprivica and Ruoyan Chen and Katsura Tottori and Tetsuro Kikuchi and C. Anthony Altar},
  journal={European journal of pharmacology},
  volume={441 3},

Interaction of the novel antipsychotic aripiprazole with 5-HT1A and 5-HT2A receptors: functional receptor-binding and in vivo electrophysiological studies

Results support a partial agonist activity for aripiprazole at 5-HT1A receptors in vitro and in vivo, and suggest important interactions with other 4-HT-receptor subtypes and this receptor activity profile may contribute to the antipsychotic activity of aripine in humans.

Aripiprazole, a Novel Antipsychotic, Is a High-Affinity Partial Agonist at Human Dopamine D2 Receptors

These results, together with previous studies demonstrating partial agonist activity at serotonin 5-hydroxytryptamine (5-HT)1A receptors and antagonist activity at 5-HT2A receptors, support the identification of aripiprazole as a dopamine-serotonin system stabilizer.

Trazodone and its active metabolite m-chlorophenylpiperazine as partial agonists at 5-HT1A receptors assessed by [35S]GTPγS binding

The agonist properties of trazodone and its active metabolite, m-chlorophenylpiperazine (m-CPP), at 5-HT1A receptors are elucidated by means of the guanosine-5′-O-(3-[ 35S]thio)-triphosphate ([35S]GTPγS) binding assay.

Effects of Aripiprazole, Risperidone, and Olanzapine on 5-HT1A Receptors in Patients With Schizophrenia

A significant reduction of [18F]MPPF BPND was found in treated schizophrenic patients compared to age- and sex-matched healthy subjects, and modifications were mainly localized in the frontal and orbitofrontal cortex and may reflect either the pathophysiology of schizophrenia or medication effects.

Differential effects of aripiprazole on D(2), 5-HT(2), and 5-HT(1A) receptor occupancy in patients with schizophrenia: a triple tracer PET study.

Aripiprazole exhibits a unique occupancy profile as compared with other conventional and atypical antipsychotics, and the threshold for response appears to be higher than 60%, extrapyramidal side effects appear to be uncommon even at occupancies that exceed the conventional extrapYramidal Side effects threshold of 80%, and 5-HT(2) occupancy is lower than D( 2) occupancy.



Effects of the novel antipsychotic agent 7-(4-[4-(2,3-dichlorophenyl)-1-piperazinyl]butyloxy)-3,4-dihydro -2(1H)-quinolinone (OPC-14597) on prolactin release from the rat anterior pituitary gland.

The results suggest that OPC-14597 has a mixed agonist/antagonist profile at D2 receptors on lactotroph cells and thereby exerts either an antagonistic or an agonistic action, depending on the preexisting tone of the dopaminergic neuronal activities.

Improving the treatment of schizophrenia: focus on serotonin (5-HT)(1A) receptors.

  • M. Millan
  • Psychology, Biology
    The Journal of pharmacology and experimental therapeutics
  • 2000
Clinical studies of antipsychotics interacting with 5-HT(1A) receptors are required to establish their genuine pertinence to the-hopefully improved-treatment of schizophrenia.

Interactions between neuroleptics and 5-HT1A ligands in preclinical behavioral models for antipsychotic and extrapyramidal effects

The present data suggest that 5-HT1A agonists with intermediate or high, but not low, intrinsic activity may abolish the extrapyramidal effects of neuroleptics.

Interactions of (+)- and (-)-8- and 7-hydroxy-2-(di-n-propylamino)tetralin at human (h)D3, hD2 and h serotonin1A receptors and their modulation of the activity of serotoninergic and dopaminergic neurones in rats.

For these substituted aminotetralins, stereospecificity is a more marked feature of interactions at hD3 and, at higher concentrations, hD2 receptors.

Effect of gepirone and ipsapirone on the stimulated and unstimulated secretion of prolactin in the rat.

  • J. NashH. Meltzer
  • Biology, Medicine
    The Journal of pharmacology and experimental therapeutics
  • 1989
It is hypothesized that GEP and perhaps IPS are partial dopamine agonists which may contribute to their antianxiety and/or antidepressant properties.

Stimulated [35S]GTPγS binding by 5-HT1A receptor agonists in recombinant cell lines Modulation of apparent efficacy by G-protein activation state

G-protein activation by different 5-HT receptor ligands was investigated in h5-HT1A receptor-transfected C6-glial and HeLa cells using agonist-stimulated [35S]GTPγS binding to membranes in the presence of excess GDP, suggesting that the activity state of G-proteins can affect the maximal response.

Antipsychotic drug doses and neuroleptic/dopamine receptors

It is reported here that all clinically effective antipsychotic drugs (tested so far) block the stereo-specific binding of 3H-haloperidol at concentrations which correlate directly with the clinical potencies.