Abstract
A series of compounds structurally related to pramipexole were designed, synthesized, and evaluated as ligands for the dopamine 3 (D3) receptor. Compound 12 has a K(i) value of 0.41 nM to D3 and a selectivity of >30000- and 800-fold over the D1-like and D2 receptors, respectively. Our in vivo functional assays showed that this compound is a partial agonist at the D3 receptor with no detectable activity at the D2 receptor.
Publication types
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Research Support, N.I.H., Extramural
MeSH terms
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Animals
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Behavior, Animal / drug effects*
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Benzothiazoles / chemical synthesis*
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Benzothiazoles / chemistry
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Benzothiazoles / pharmacology*
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Binding Sites / drug effects
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Binding, Competitive / drug effects
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Dopamine Agonists / chemical synthesis*
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Dopamine Agonists / chemistry
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Dopamine Agonists / pharmacology*
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Dose-Response Relationship, Drug
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Drug Design
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Humans
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Hydrogen Bonding
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Hypothermia / chemically induced
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Ligands
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Models, Molecular
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Molecular Conformation
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Pramipexole
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Rats
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Receptors, Dopamine D1 / agonists
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Receptors, Dopamine D2 / agonists
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Receptors, Dopamine D3 / agonists*
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Sensitivity and Specificity
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Solubility
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Stereoisomerism
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Structure-Activity Relationship
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Yawning / drug effects
Substances
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Benzothiazoles
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Dopamine Agonists
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Ligands
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Receptors, Dopamine D1
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Receptors, Dopamine D2
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Receptors, Dopamine D3
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Pramipexole