title: Identification of N-propylnoraporphin-11-yl 5-(1,2-dithiolan-3-yl)pentanoate as a new anti-Parkinson's agent possessing a dopamine D2 and serotonin 5-HT1A dual-agonist profile.
abstract: 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-HT(1A) 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-HT(1A) and D(2) dual-receptor agonist (-)-15 may present a novel candidate drug in the treatment of PD and LID.
authors: Department of Pharmacology, Soochow University College of Pharmaceutical Sciences, Suzhou, China.
authors: Hai
authors: H
authors: Zhang
authors: Na
authors: N
authors: Ye
authors: Shanglin
authors: S
authors: Zhou
authors: Lin
authors: L
authors: Guo
authors: Longtai
authors: L
authors: Zheng
authors: Zhili
authors: Z
authors: Liu
authors: Bo
authors: B
authors: Gao
authors: Xuechu
authors: X
authors: Zhen
authors: Ao
authors: A
authors: Zhang