Dopamine receptor binding predicts clinical and pharmacological potencies of antischizophrenic drugs

@article{Creese1976DopamineRB,
  title={Dopamine receptor binding predicts clinical and pharmacological potencies of antischizophrenic drugs},
  author={Ian Creese and David R. Burt and Solomon H. Snyder},
  journal={Science},
  year={1976},
  volume={192},
  pages={481 - 483}
}
Tritiated haloperidol and tritiated dopamine label postsynaptic dopamine receptors in mammalian brain. Clinical potencies of butyrophenones, phenothiazines, and related drugs correlate closely with their ability to inhibit tritiated haloperidol binding. These binding methods provide a simple in vitro means for evaluating new drugs as potential antischizophrenic agents. 

Relationship of neuroleptic drug effects at brain dopamine, serotonin, alpha-adrenergic, and histamine receptors to clinical potency.

The authors examined the potencies of 22 neuroleptic drugs competing for binding sites associated with dopamine, serotonin, alpha-adrenergic, and histamine receptors in brain membranes. They found

Neuroleptic Binding to Human Brain Receptors: Relation to Clinical Effects a

  • E. Richelson
  • Psychology, Biology
    Annals of the New York Academy of Sciences
  • 1988
TLDR
The pharmacological effects of neuroleptics at receptors in brain and elsewhere in the body are likely responsible for therapeutic and certain adverse effects as well as some drug-drug interactions.

Dopamine receptors, neuroleptics, and schizophrenia.

  • S. Snyder
  • Psychology, Biology
    The American journal of psychiatry
  • 1981
TLDR
The binding of 3H-butyrophenones to dopamine receptors can be used for a radioreceptor assay that detects blood levels of all clinically used neuroleptics and their pharmacologically active metabolites and may facilitate routine monitoring of blood levels.

Stereospecificity of interaction of neuroleptic drugs with neurotransmitters and correlation with clinical potency

TLDR
If optical or geometrical isomers of a drug have markedly different clinical potencies, the most relevant biochemical effect should also exhibit isomeric specificity.

Dopaminergic D2 receptor binding of phenothiazine drugs and their metabolites

TLDR
As a screening of their possible pharmacological activities, phenothiazine drug metabolites were examined for their binding affinities to dopamine D2 receptors in rat brain using radioligand binding techniques and the 7-hydroxy- and N-desmethyl metabolites had the highest binding affinity.

Receptor pharmacology of neuroleptics: relation to clinical effects.

  • E. Richelson
  • Psychology
    The Journal of clinical psychiatry
  • 1999
TLDR
This article reviews the receptor pharmacology of neuroleptics, with a focus on newer drugs (e.g., risperidone, olanzapine, sertindole, quetiapines, and ziprasidone) in contrast to older compounds, based upon certain criteria, which are reviewed.

Striatal Dopamine Receptors: Dose-Dependent Occupation by, and Rapid Washout of, Orally Given Neuroleptics in Humans

TLDR
Neuroleptic drugs are effective anti-psychotic agents, but the relationship between dosage and clinical response still is unclear and the usefulness of maintenance therapy is debated.

New drugs for the treatment of schizophrenic patients

  • W. Fleischhacker
  • Psychology, Medicine
    Acta psychiatrica Scandinavica. Supplementum
  • 1995
TLDR
New strategies for treating schizophrenia include the development of dopamine antagonists with high selectivity for different subtypes of dopamine receptors, dopamine partial agonists, antagonists at different serotonin (5–hydroxytryptamine; 5–HT) receptor subtypes, drugs with mixed pharmacological profiles and drugs which modify transmission via amino acids or peptides in the brain.

The Interaction of Atypical Neuroleptics with Monoamine Receptor Subtypes

TLDR
The modern „atypical neuroleptic“ must have beneficial effects on both the positive and negative symptoms of schizophrenia and the ability to improve cognitive function in patients that are otherwise resistant to drug intervention.
...

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