Abstract
A series of 1-phenyl-3-(aminomethyl)pyrroles were prepared in two steps from aniline and their affinities for D2, D3, and D4 dopamine receptor subtypes determined. A 15-fold selectivity for cloned human D4 receptors over cloned African Green monkey D2 receptors was observed with 1-(2-pyridyl)-4-[[3-(1-phenylpyrrolyl)]methyl]piperazine.
MeSH terms
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Animals
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Antipsychotic Agents / chemistry
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Antipsychotic Agents / metabolism
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Antipsychotic Agents / pharmacology*
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Chlorocebus aethiops
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Cloning, Molecular
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Humans
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Hydrogen Bonding
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Magnetic Resonance Spectroscopy
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Pyrroles / chemical synthesis
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Pyrroles / metabolism
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Pyrroles / pharmacology*
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Receptors, Dopamine / classification
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Receptors, Dopamine / genetics
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Receptors, Dopamine / metabolism*
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Recombinant Proteins / genetics
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Recombinant Proteins / metabolism
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Structure-Activity Relationship
Substances
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Antipsychotic Agents
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Pyrroles
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Receptors, Dopamine
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Recombinant Proteins