作者: David E. Nichols
DOI: 10.1007/978-1-60327-333-6_4
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摘要: A survey is presented of the development dopamine D1 receptor-selective drugs, including agonists and antagonists. It noted that there are presently no ligands specific for vs D5 receptor isoforms. general discussion on structure–activity features D1/D5 selective agents, with conclusions developed all known full must contain a catechol moiety and, in addition, require presence hydrophobic (typically phenyl ring) region adjacent to beta side chain carbon embedded fragment. This latter structural feature so crucial when added noncatechol ergoline it gave D1-selective partial agonist. Present evidence indicates may be therapeutically useful treatment Parkinson’s disease, as well improving cognition working memory schizophrenia age-related cognitive decline. No agonist has yet been commercialized, seems largely due difficulties oral bioavailability catechol-containing drugs.