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

@article{Jordan2002TheAA,
  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},
  year={2002},
  volume={441 3},
  pages={
          137-40
        }
}
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393 Citations
Highly Influential Citations
5
Background Citations
136
Methods Citations
4
Results Citations
9

393 Citations

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.

Distinct functional profiles of aripiprazole and olanzapine at RNA edited human 5-HT2C receptor isoforms.

Aripiprazole's low intrinsic activities at human dopamine D2L and D2S receptors render it a unique antipsychotic.

Geissoschizine methyl ether has third-generation antipsychotic-like actions at the dopamine and serotonin receptors.

Synthesis and biological investigation of potential atypical antipsychotics with a tropane core. Part 1.

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.

Pharmacological, neurochemical, and behavioral profile of JB-788, a new 5-HT1A agonist

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.
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