Dopamine Receptor Binding Predicts Clinical and Pharmacological Potencies of Antischizophrenic Drugs
Abstract
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.
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Medications that have proven successful for treating schizophrenia/psychosis are drugs that primarily antagonize D2 receptors.
“the medications that have proven successful for treating schizophrenia/psychosis are drugs that primarily antagonize D2 receptors [76,358]”
From Reward circuitry dysfunction in psychiatric and neurodevelopmental disorders and genetic syndromes: animal models and clinical findings (2012) · cites this paper as [358]
First-generation compounds such as chlorpromazine and haloperidol work primarily as D2 receptor antagonists.
“First-generation compounds, such as chlorpromazine and haloperidol, work primarily as D2 receptor antagonists [358].”
From Reward circuitry dysfunction in psychiatric and neurodevelopmental disorders and genetic syndromes: animal models and clinical findings (2012) · cites this paper as [358]
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- Authors
- Creese, I., Burt, D. R., & Snyder, S. H.
- Affiliations
- Johns Hopkins University (US)
- ORCID
- Snyder, Solomon H.
- Venue
- Science
- Published
- 1976-04-30
- Volume
- 192
- Issue
- 4238
- Pages
- 481-483
- ISSN
- 0036-8075 (ISSN-L)
- 1095-9203
- OpenAlex
- W2009447429
- Cited by
- 2,220
- References
- 25
- Citations by year
- 2026: 11 · 2025: 24 · 2024: 30 · 2023: 24 · 2022: 39 · 2021: 27 · 2020: 32 · 2019: 39 · 2018: 25 · 2017: 36 · 2016: 43 · 2015: 53 · 2014: 44 · 2013: 47 · 2012: 55
- FWCI
- 88.70
- Type
- journal article
- Language
- en
- Open access
- closed
- Locations
- Science (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Health Sciences › Medicine › Psychiatry and Mental health › Schizophrenia research and treatment
- Life Sciences › Neuroscience › Cellular and Molecular Neuroscience › Neurotransmitter Receptor Influence on Behavior
- Life Sciences › Biochemistry, Genetics and Molecular Biology › Molecular Biology › Receptor Mechanisms and Signaling
- Keywords
- dopamine receptors, receptor binding, antipsychotic drugs, haloperidol, butyrophenones, phenothiazines, drug potency, postsynaptic dopamine receptors, drug evaluation
- MeSH terms
- Adenylyl Cyclases, Animals, Binding, Competitive, Butyrophenones, Corpus Striatum, Dopamine, Haloperidol, Humans, Olfactory Bulb, Phenothiazines, Receptors, Drug, Schizophrenia, Structure-Activity Relationship, Antipsychotic Agents, Dopamine Antagonists
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