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PMID: 1060115 Published · ppublish English Journal Article

Brain receptors for antipsychotic drugs and dopamine: direct binding assays.

Proceedings of the National Academy of Sciences of the United States of America ·Vol. 72 ·No. 11 ·1975-11-00 ·Pages 4376-80

Seeman P, Chau-Wong M, Tedesco J, Wong K

Abstract

In order to test the suggestion that antipsychotic drugs act by blocking dopamine receptors in the brain, the direct effects of such neuroleptic drugs were tested on the stereospecific binding of [3H]dopamine and of [3H]haloperidol to rat brain striata and their subfractions. The stereospecific component of binding was defined as that amount of [3h]dopamine or [3H]haloperidol bound in the presence of (-)-butaclamol (an inactive drug) minus that bound in the presence of (+)-butaclamol (a potent neuroleptic drug); 100 nM butaclamol was used for the [3H]haloperidol assay, while 1 muM butaclamol was used for the [3H]dopamine assay. Various antipsychotic drugs inhibited this stereospecific component in both the dopamine and haloperidol assays. These inhibitory potencies correlated with the clinical doses used for controlling schizophrenia.

MeSH Terms
Animals Binding Sites Corpus Striatum/metabolism Dopamine/metabolism Haloperidol/metabolism Humans Male Rats Receptors, Drug Schizophrenia/drug therapy Synaptosomes/metabolism Tranquilizing Agents/metabolism,therapeutic use
Chemicals
Receptors, Drug Tranquilizing Agents Haloperidol Dopamine
Authors & Affiliations
4 authors, click to expand affiliations / ORCID
Seeman P
Chau-Wong M
Tedesco J
Wong K
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33 references, click to expand
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Article Info
Journal
Proceedings of the National Academy of Sciences of the United States of America
Abbr.
Proc Natl Acad Sci U S A
ISSN
0027-8424
DOI
10.1073/pnas.72.11.4376
Published
1975-11-00
Pages
4376-80
Language
English
Region
United States
NLM ID
7505876
PMCID
PMC388724
Subset
IM
External Links
PubMed source DOI: 10.1073/pnas.72.11.4376 PMC Full Text View journal details
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