Abstract
A novel series of arylsulfonamides was prepared either by automated parallel or by traditional solution-phase synthesis. Several members of this compound library were identified as high-affinity dopamine D3 and D2 receptor ligands. The most interesting representative, compound 2, showed potent antipsychotic behaviour coupled with a beneficial cognitive and EPS profile.
MeSH terms
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Animals
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Antipsychotic Agents / chemical synthesis*
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Antipsychotic Agents / metabolism
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Antipsychotic Agents / pharmacology*
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Apomorphine / pharmacology
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Avoidance Learning / drug effects
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Binding, Competitive / drug effects
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Biological Availability
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Brain / metabolism
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Catalepsy / chemically induced
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Cognition / drug effects*
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Humans
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Indicators and Reagents
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Male
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Maze Learning / drug effects
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Memory Disorders / chemically induced
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Quantitative Structure-Activity Relationship
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Rats
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Rats, Wistar
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Receptors, Dopamine D2 / metabolism*
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Receptors, Dopamine D3 / metabolism*
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Stereotyped Behavior / drug effects
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Sulfonamides / chemical synthesis*
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Sulfonamides / metabolism
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Sulfonamides / pharmacology*
Substances
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Antipsychotic Agents
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Indicators and Reagents
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Receptors, Dopamine D2
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Receptors, Dopamine D3
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Sulfonamides
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Apomorphine