Compounds > 11-hydroxy-n-(n-propyl)noraporphine-hydrochloride--(r)-isomer

11-hydroxy-n-(n-propyl)noraporphine-hydrochloride--(r)-isomer and Dyskinesia--Drug-Induced

11-hydroxy-n-(n-propyl)noraporphine-hydrochloride--(r)-isomer has been researched along with Dyskinesia--Drug-Induced* in 1 studies

Other Studies

1 other study(ies) available for 11-hydroxy-n-(n-propyl)noraporphine-hydrochloride--(r)-isomer and Dyskinesia--Drug-Induced

Article	Year
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. Journal of medicinal chemistry, 2011, Jul-14, Volume: 54, Issue:13 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. Topics: Animals; Antiparkinson Agents; Aporphines; Binding, Competitive; CHO Cells; Corpus Striatum; Cricetinae; Cricetulus; Dyskinesia, Drug-Induced; HEK293 Cells; Humans; Levodopa; Oxidopamine; Parkinson Disease; Proto-Oncogene Proteins c-fos; Radioligand Assay; Rats; Receptors, Adrenergic; Receptors, Dopamine D2; Serotonin 5-HT1 Receptor Agonists; Stereoisomerism; Structure-Activity Relationship; Thioctic Acid	2011

Article

Year

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.

Journal of medicinal chemistry, 2011, Jul-14, Volume: 54, Issue:13

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.

Topics: Animals; Antiparkinson Agents; Aporphines; Binding, Competitive; CHO Cells; Corpus Striatum; Cricetinae; Cricetulus; Dyskinesia, Drug-Induced; HEK293 Cells; Humans; Levodopa; Oxidopamine; Parkinson Disease; Proto-Oncogene Proteins c-fos; Radioligand Assay; Rats; Receptors, Adrenergic; Receptors, Dopamine D2; Serotonin 5-HT1 Receptor Agonists; Stereoisomerism; Structure-Activity Relationship; Thioctic Acid

2011