The ABC's of dopamine receptor partial agonists - aripiprazole, brexpiprazole and cariprazine: the 15-min challenge to sort these agents out

Citrome, Leslie

doi:10.1111/ijcp.12752

Cited by 96 publications

(95 citation statements)

References 34 publications

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“…All three of these atypical antipsychotics contain characteristic (4-arylpiperazin-1-yl)alkyl groups. The differences and similarities of these drugs as dopamine receptor partial agonists have been systematically reviewed [119]. In this article, we will focus on the comparisons of aripiprazole ( 5 ), a representative antipsychotic drug from this class, with other classes of typical and atypical antipsychotics.…”

Section: Development Of Antipsychotics For the Treatment Of Schizophrmentioning

confidence: 99%

Dopamine Targeting Drugs for the Treatment of Schizophrenia: Past, Present and Future

Snyder²,

Vanover³

2016

CTMC

219

141

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Schizophrenia is a chronic and debilitating neuropsychiatric disorder affecting approximately 1% of the world’s population. This disease is associated with considerable morbidity placing a major financial burden on society. Antipsychotics have been the mainstay of the pharmacological treatment of schizophrenia for decades. The traditional typical and atypical antipsychotics demonstrate clinical efficacy in treating positive symptoms, such as hallucinations and delusions, while are largely ineffective and may worsen negative symptoms, such as blunted affect and social withdrawal, as well as cognitive function. The inability to treat these latter symptoms may contribute to social function impairment associated with schizophrenia. The dysfunction of multiple neurotransmitter systems in schizophrenia suggests that drugs selectively targeting one neurotransmission pathway are unlikely to meet all the therapeutic needs of this heterogeneous disorder. Often, however, the unintentional engagement of multiple pharmacological targets or even the excessive engagement of intended pharmacological targets can lead to undesired consequences and poor tolerability. In this article, we will review marketed typical and atypical antipsychotics and new therapeutic agents targeting dopamine receptors and other neurotransmitters for the treatment of schizophrenia. Representative typical and atypical antipsychotic drugs and new investigational drug candidates will be systematically reviewed and compared by reviewing structure-activity relationships, pharmacokinetic properties, drug metabolism and safety, pharmacological properties, preclinical data in animal models, clinical outcomes and associated side effects.

show abstract

Section: Development Of Antipsychotics For the Treatment Of Schizophrmentioning

confidence: 99%

Dopamine Targeting Drugs for the Treatment of Schizophrenia: Past, Present and Future

Snyder²,

Vanover³

2016

CTMC

219

141

View full text Add to dashboard Cite

show abstract

“…27 In a previous publication, we described the synthesis and biological activity of a series of new 3β-acylamine derivatives of tropane, among which compound A ( Ref. 28 ) drew our particular attention as it displayed a very high (in the nM range) affinity for each of the investigated receptors (i.e.…”

Section: Introductionmentioning

confidence: 99%

Synthesis and biological investigation of new equatorial (β) stereoisomers of 3-aminotropane arylamides with atypical antipsychotic profile

Stefanowicz

Słowiński

Wróbel

et al. 2016

Bioorganic & Medicinal Chemistry

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“…Of interest are the rates of akathisia, which are 5.5% for the pooled doses of brexpiprazole 1–4 mg/day versus 4.6% for placebo, yielding a number needed to harm (NNH) of 112, and consistent with what was observed on the Barnes Akathisia Rating Scale for both studies. This is different from the rates of akathisia observed with aripiprazole, which are 8% for aripiprazole versus 4% for placebo, yielding a NNH of 25 4. Given the NNT for response for aripiprazole 10–30 mg/day versus placebo is 8, and that for brexpiprazole 2–4 mg/day is 7, for the person with schizophrenia being treated with aripiprazole but experiencing akathisia, brexpiprazole is a potential alternative.…”

Section: Do These Results Change Your Practices and Why?mentioning

confidence: 90%

Which role for brexpiprazole, a new dopamine D2 partial agonist, in the treatment of schizophrenia?

Citrome

2016

Evid Based Mental Health

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The ABC's of dopamine receptor partial agonists - aripiprazole, brexpiprazole and cariprazine: the 15-min challenge to sort these agents out

Cited by 96 publications

References 34 publications

Dopamine Targeting Drugs for the Treatment of Schizophrenia: Past, Present and Future

Dopamine Targeting Drugs for the Treatment of Schizophrenia: Past, Present and Future

Synthesis and biological investigation of new equatorial (β) stereoisomers of 3-aminotropane arylamides with atypical antipsychotic profile

Which role for brexpiprazole, a new dopamine D2 partial agonist, in the treatment of schizophrenia?

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