Abstract
The present study describes the synthesis and in vitro pharmacology of a novel series of dopaminergic agents in which the classical phenylethylamine pharmacophore is replaced by a thienylethylamine moiety. In general, the novel compounds showed a moderate affinity for the dopamine (DA) D(2) and D(3) receptors. When the thienylethylamine moiety is fixed in a rigid system, the affinity for the DA receptor is significantly increased. However, in the tricyclic hexahydrothianaphthoxazine structure, the affinity for the DA receptors is diminished.
MeSH terms
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Animals
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Binding, Competitive
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Biological Availability
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CHO Cells
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Cricetinae
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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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Humans
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Magnetic Resonance Spectroscopy
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Microdialysis
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Radioligand Assay
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Rats
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Receptors, Dopamine D2 / metabolism*
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Receptors, Dopamine D3
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Structure-Activity Relationship
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Thiophenes / chemical synthesis*
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Thiophenes / chemistry
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Thiophenes / pharmacology
Substances
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DRD3 protein, human
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Dopamine Agonists
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Drd3 protein, rat
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Receptors, Dopamine D2
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Receptors, Dopamine D3
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Thiophenes
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dopamine D2L receptor