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

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Dijkstra D, Rodenhuis N, Vermeulen ES, Pugsley TA, Wise LD, Wikstrom HV

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

J Med Chem. 2002 Jul 4;45(14):3022-31.

PubMed ID

12086487 [ View in PubMed

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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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Rotigotine	Dopamine D2 receptor	Ki (nM)	0.06	N/A	N/A	Details
Rotigotine	Dopamine D3 receptor	Ki (nM)	4	N/A	N/A	Details