期刊
JOURNAL OF MEDICINAL CHEMISTRY
卷 54, 期 13, 页码 4324-4338出版社
AMER CHEMICAL SOC
DOI: 10.1021/jm200347t
关键词
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资金
- Chinese National Science Foundation [30772625, 81072528, 30825042]
- Ministry of Science and Technology of China [2009CB522000]
- Shanghai Commission of Science and Technology [10410702600, 10JC1417100, 10dz1910104]
- National Science and Technology Major Project on Key New Drug Creation and Manufacturing Program [2009ZX09301-001, 2009ZX09103-062, 2009ZX09102]
A series of new aporphine analogues (aporlogues) were synthesized bearing a C-, N-, or O-linkage at the C11 position. Lipoic ester (-)-15 was identified as a full agonist at the dopamine D-2 and serotonin 5-HT1A receptors with K-i values of 174 and 66 nM, respectively. It elicited antiparkinsonian action on Parkinsin's disease (PD) rats with minor dyskinesia. Chronic use of (-)-15 reduced L-DOPA-induced dyskinesia (LID) without attenuating the antiparkinsonian effect. These results suggest that 5-HT1A and D-2 dual-receptor agonist (-)-15 may present a novel candidate drug in the treatment of PD and LID.
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