Further characterization of structural requirements for ligands at the dopamine D(2) and D(3) receptor: exploring the thiophene moiety

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)...

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Published inJournal of medicinal chemistry Vol. 45; no. 14; pp. 3022 - 3031
Main Authors Dijkstra, Durk, Rodenhuis, Nienke, Vermeulen, Erik S, Pugsley, Thomas A, Wise, Lawrence D, Wikström, Håkan V
Format Journal Article
LanguageEnglish
Published United States 04.07.2002
Subjects
Animals
Binding, Competitive
Biological Availability
CHO Cells
Cricetinae
Dopamine Agonists - chemical synthesis
Dopamine Agonists - chemistry
Dopamine Agonists - pharmacology
Humans
Magnetic Resonance Spectroscopy
Microdialysis
Radioligand Assay
Rats
Receptors, Dopamine D2 - metabolism
Receptors, Dopamine D3
Structure-Activity Relationship
Thiophenes - chemical synthesis
Thiophenes - chemistry
Thiophenes - pharmacology
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Summary: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.
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SourceType-Scholarly Journals-1
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ISSN:0022-2623