Dopamine partial agonists: a discrete class of antipsychotics

Taylor, David; Chithiramohan, R. N.; Grewal, Jasdev; Gupta, Avirup; Hansen, Lars; Reynolds, Gavin P.; Pappa, Sofia

doi:10.1080/13651501.2022.2151473

Cited by 6 publications

(2 citation statements)

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“…The results of this study also support the existing evidence ( 21 , 24 , 25 ) that cariprazine could be considered as a viable alternative to other antipsychotics associated with tolerability issues. Its unique pharmacological profile, which includes partial agonism of dopamine receptors with preferential binding to D3 over D2 receptors and low/absent affinity to histaminergic and cholinergic receptors ( 26 , 27 ) has been associated with an improvement in negative symptoms ( 15 , 28 ) and low rates of adverse events, including metabolic side effects ( 29 ) and hyperprolactinaemia ( 15 , 30 ).…”

Section: Discussionmentioning

confidence: 99%

Cariprazine for negative symptoms in early psychosis: a pilot study with a 6-month follow-up

2023

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BackgroundCariprazine, a novel antipsychotic drug that is a partial agonist with preferential binding to the D3 receptor, has demonstrated efficacy in clinical trials across all symptom domains, including negative symptoms, which can occur early in the course of psychotic illness. However, evidence, to date regarding its effects in early psychosis patients with primary negative symptoms has been limited.ObjectivesTo evaluate the efficacy of cariprazine for negative symptoms in early psychosis patients.MethodsDemographic and clinical information of the study population were collected from the electronic records and PANSS scale administered at baseline, 3 and 6 months. Tolerability and discontinuation reasons, where applicable, were also recorded.ResultsTen patients with early psychosis (four men and six women, mean age – 25.5 years) with prominent or predominant negative symptoms were treated with cariprazine (range 1.5 – 3 mg). Three patients discontinued cariprazine within the first 3 months due to patient choice, lack of response and non-compliance, respectively. In the remaining patients, there was a significant reduction in the mean negative PANSS score from baseline to 6 months (from 26.3 to 10.6), mean total PANSS score (from 81.4 to 43.3) and in the mean positive PANSS score (from 14.4 to 9.9) which correspond to a 53.1, 41.5, and 28.5% mean score reduction.ConclusionThis pilot study suggests that cariprazine is a safe and effective treatment in early psychosis, particularly for the alleviation of negative symptoms which remains an area of unmet treatment need.

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Section: Discussionmentioning

confidence: 99%

Cariprazine for negative symptoms in early psychosis: a pilot study with a 6-month follow-up

2023

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“…Despite antipsychotic drugs of the first-generation being D2 postsynaptic antagonists, the underlying dopamine perturbation of the disorder is one of release; also, different neural pathways are differentially affected in people with schizophrenia (Howes and Kapur, 2009; McCutcheon et al, 2019). It has been hypothesised that partial agonism of D2 receptors could ‘modulate’ dopamine perturbations in schizophrenia (Mailman and Murthy, 2010; Taylor et al, 2022) and thus the ‘third generation’ of antipsychotics were synthesised (Naber et al, 2015).…”

Section: Beyond D2 Receptor Blockadementioning

confidence: 99%

Seven decades of antipsychotic drugs: Why is the life of Australians with schizophrenia still so suboptimal?

Castle,

Copolov,

Singh

et al. 2023

Aust N Z J Psychiatry

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The advent of dopamine (D2) receptor-blocking medications over 70 years ago, ushered in a new era of biological treatment for schizophrenia. However, we argue that little subsequent progress has been made in translating this into fulfilled and fulfilling lives for people with schizophrenia. This Viewpoint asks why this is the case, and suggests ways forward for capitalising on extant and emerging new treatments for psychotic disorders, to the betterment of the lives of people living with schizophrenia.

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Bioactive Molecules from Lignocellulose‐Derived Platform Chemicals

Qiang,

Ansari,

Sun

et al. 2024

Adv Synth Catal

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The ever‐increasing prevalence of diseases and inadequate resources on Earth are threats to society. Biomass is an abundant resource, and bioactive compounds produced from biomass are environmentally benign in contrast to conventional chemical synthesis methods, which frequently depend on non‐renewable resources. In addition, the functionalized monomers from biomass allow the atom economical synthesis of bioactive molecules. This review aims to provide insight into the synthesis of bioactive molecules from the lignocellulose‐derived platform chemicals. Existing methodology and catalytic systems are summarized for the synthesis of targeted bioactive molecules from cellulose, hemicellulose, and lignin‐derived platform chemicals. The biological activities of bioactive molecules obtained from biomass, such as antioxidant, anti‐inflammatory, and anticancer properties, are discussed.

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Dopamine partial agonists: a discrete class of antipsychotics

Cited by 6 publications

References 130 publications

Cariprazine for negative symptoms in early psychosis: a pilot study with a 6-month follow-up

Cariprazine for negative symptoms in early psychosis: a pilot study with a 6-month follow-up

Seven decades of antipsychotic drugs: Why is the life of Australians with schizophrenia still so suboptimal?

Bioactive Molecules from Lignocellulose‐Derived Platform Chemicals

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