New, centrally acting dopaminergic agents with an improved oral bioavailability: synthesis and pharmacological evaluation
作者： Nieske Rodenhuis
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摘要: This chapter describes the synthesis and in vitro pharmacology of a novel series dopamine receptor ligands, which classical phenylethylamine pharmacophore is replaced by thienylethylamine moiety. In general, compounds showed moderate affinity for D2 D3 receptors. The results that moiety can act as on these When fixed rigid system increased, however, tricyclic hexahydrothianaphthoxazine structure, receptors diminished. * based on: Rodenhuis, N.; Vermeulen, E.S.; Wikstrom, H.V.; Pugsley, T.A.; Wise, L.D.; Dijkstra, D. (2000) Further characterization structural requirements ligands at receptor: studies with thienylethylamines possible pharmacophore. J. Med. Chem. submitted.
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