Abstract
Flunarizine dose dependently inhibits the binding of both [3H]spiperone and [3H]SCH 23390 with Ki values of 112 +/- 9 and 532 +/- 39 nM, respectively. The inhibition of [3H]spiperone binding by flunarizine was competitive as revealed by the Schild plot. The results indicate that flunarizine is a fairly potent dopamine D2 receptor antagonist and offer a possible explanation for the extrapyramidal side-effects observed in patients treated with the drug.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Benzazepines / metabolism
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Binding, Competitive
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Corpus Striatum / drug effects
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Corpus Striatum / metabolism
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Flunarizine / metabolism
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Flunarizine / pharmacology*
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In Vitro Techniques
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Kinetics
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Male
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Rats
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Rats, Inbred Strains
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Receptors, Dopamine / drug effects*
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Receptors, Dopamine / metabolism
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Receptors, Dopamine D1
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Receptors, Dopamine D2
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Spiperone / metabolism
Substances
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Benzazepines
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Receptors, Dopamine
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Receptors, Dopamine D1
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Receptors, Dopamine D2
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Spiperone
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Flunarizine