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Journal ArticleDOI

Pharmacologic properties of (-)-3PPP (preclamol) in man.

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TLDR
This study suggests that (−)-3PPP/preclamol is a safe drug for study in the treatment of schizophrenia and may have antipsychotic efficacy.
Abstract
The dopamine (DA) autoreceptor agonist (−)-3PPP (preclamol) was tested in male schizophrenic volunteers for safety. The drug was administered intramuscularly in a single rising dose design, crossed with a similar “rising dose” placebo period; all evaluations and raters were blind to drug or placebo administration. Pharmacokinetic, endocrine, safety, and mental status outcome measures were completed before and after each single dose of drug or placebo. Pharmacokinetic analysis showed blood levels between 200–500 pmoles/ml after the intramuscular drug doses of 30–40 mg. Drug half life is 2–2.5 hrs. Growth hormone (GH) levels were elevated in a linear fashion to the 30 mg dose; whereafter, the drug failed to affect GH at all. All safety evaluations were negative, including any untoward effects on the major organ systems. After single dose drug administration, evidence of antipsychotic action occurred in two of the four subjects. This study suggests that (−)-3PPP/preclamol is a safe drug for study in the treatment of schizophrenia and may have antipsychotic efficacy.

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Cross‐Coupling of Heteroarenes by CH Functionalization: Recent Progress towards Direct Arylation and Heteroarylation Reactions Involving Heteroarenes Containing One Heteroatom

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Mechanisms of action of atypical antipsychotic drugs: a critical analysis

TL;DR: This review discusses salient distinctions predominantly between prototypic atypical and typical antipsychotic drugs such as clozapine and haloperidol, respectively.
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Third Generation Antipsychotic Drugs: Partial Agonism or Receptor Functional Selectivity?

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Dopamine receptors - physiological understanding to therapeutic intervention potential

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A paradigm shift in brain research.

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References
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Journal ArticleDOI

The Brief Psychiatric Rating Scale

TL;DR: The Brief Psychiatric Rating Scale (BRS) as mentioned in this paper was developed to provide a rapid assessment technique particularly suited to the evaluation of patient change, and it is recommended for use where efficiency, speed, and economy are important considerations.
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Negative Symptoms in Schizophrenia: Definition and Reliability

TL;DR: The developed Scale for the Assessment of Negative Symptoms has excellent interrater reliability and the five symptom complexes defined by the scale have good internal consistency, which indicates that the conceptual organization of the scale is also cohesive.
Journal ArticleDOI

Dopamine receptor binding predicts clinical and pharmacological potencies of antischizophrenic drugs

TL;DR: Clinical potencies of butyrophenones, phenothiazines, and related drugs correlate closely with their ability to inhibit tritiated haloperidol binding, providing a simple in vitro means for evaluating new drugs as potential antischizophrenic agents.
Journal ArticleDOI

Schizophrenic symptoms improve with apomorphine

TL;DR: Eighteen chronic schizophrenic patients received subcutaneous doses of apomorphine, a dopamine receptor agonist, and of placebo in separate trials and a significant improvement in psychotic symptoms occurred after apomorphicine compared to placebo.
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