Abstract
The baculovirus system has been used to express the rat dopamine D1 receptors in Spodoptera frugiperda (Sf9) cells. A panel of typical antipsychotics including, alpha-flupenthixol, fluphenazine and thioridizine were found to inhibit dopamine-dependent stimulation of adenylyl cyclase. However, these compounds were also found to inhibit adenylyl cyclase activity in the absence of agonist in Sf9 cells expressing dopamine D1-like receptors. Therefore, these nonselective dopamine receptor compounds displayed negative intrinsic or inverse agonist activity. None of the compounds tested were neutral antagonists.
Publication types
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Research Support, Non-U.S. Gov't
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Adenylyl Cyclases / drug effects
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Adenylyl Cyclases / metabolism
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Animals
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Antipsychotic Agents / pharmacology*
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Baculoviridae / genetics
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Binding, Competitive
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Cell Line
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Dopamine / pharmacology
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Dopamine Agonists / pharmacology*
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Dose-Response Relationship, Drug
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Gene Expression
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Genetic Vectors / genetics
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Ligands
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Radioligand Assay
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Rats
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Receptors, Dopamine D1 / agonists
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Receptors, Dopamine D1 / genetics
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Receptors, Dopamine D1 / physiology*
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Receptors, Dopamine D5
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Spodoptera
Substances
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Antipsychotic Agents
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Dopamine Agonists
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Drd5 protein, rat
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Ligands
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Receptors, Dopamine D1
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Receptors, Dopamine D5
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Adenylyl Cyclases
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Dopamine