Abstract
A series of novel 1H-pyrazolo-[3,4-c]cyclophepta[1,2-c]thiophenes was prepared and screened at selected dopamine receptor subtypes. Compound 4 (NGB 4420) displayed high affinity and selectivity (>100-fold) for the D(4) over D(2) and other CNS receptors. This compound was identified as a D(4) antagonist via its attenuation of dopamine agonist-induced GTPgamma(35)S binding at D(4) receptor.
MeSH terms
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Dopamine Antagonists / metabolism
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Dopamine Antagonists / pharmacology
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Humans
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Ligands
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Protein Binding
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Receptors, Dopamine D2 / metabolism*
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Receptors, Dopamine D4
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Structure-Activity Relationship
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Thiophenes / chemistry
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Thiophenes / metabolism*
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Thiophenes / pharmacology
Substances
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DRD4 protein, human
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Dopamine Antagonists
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Ligands
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Receptors, Dopamine D2
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Thiophenes
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Receptors, Dopamine D4