Abstract
The (+)-and (-)-enantiomer of compounds 4 and 5 were synthesized and tested for central dopamine (DA) receptor stimulating activity, using biochemical and behavioral tests in rats. Based on the available data the (-)-enantiomers of 4 and 5 are characterized as centrally acting DA autoreceptor antagonists with oral activity. They display a similar pharmacological profile as the prototype DA autoreceptor antagonists (+)-1 and (+)-2 and show a certain preference for the D3 DA receptor antagonist binding site.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Binding Sites / drug effects
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Biological Availability
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Brain / drug effects
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Brain / metabolism
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Dopamine / biosynthesis
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Dopamine / metabolism
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Dopamine Antagonists*
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Male
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Motor Activity / drug effects
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Piperidines / chemical synthesis*
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Piperidines / pharmacokinetics*
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Piperidines / pharmacology
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Rats
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Rats, Sprague-Dawley
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Receptors, Dopamine / metabolism
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Stereoisomerism
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Structure-Activity Relationship
Substances
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Dopamine Antagonists
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Piperidines
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Receptors, Dopamine
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Dopamine