- Synthesis and evaluation of nuciferine and roemerine enantiomers as 5-HT2 and α1 receptor antagonists
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In this study, the (S)-enantiomers of the aporphine alkaloids, nuciferine and roemerine, were prepared via a synthetic route involving catalytic asymmetric hydrogenation and both stereoisomers were evaluated in vitro for functional activity at human 5-HT2 and adrenergic α1 receptor subtypes using a transforming growth factor-α shedding assay. Both enantiomers of each of the compounds were found to act as antagonists at 5-HT2 and α1 receptors. (R)-roemerine was the most potent compound at 5-HT2A and 5-HT2C receptors (pKb = 7.8-7.9) with good selectivity compared to (S)-roemerine at these two receptors and compared to its activity at 5-HT2B, α1A, α1B and α1D receptors.
- Heng, Hui Li,Chee, Chin Fei,Chin, Sek Peng,Ouyang, Yifan,Wang, Hao,Buckle, Michael J.C.,Herr, Deron R.,Paterson, Ian C.,Doughty, Stephen W.,Abd Rahman, Noorsaadah,Chung, Lip Yong
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p. 576 - 582
(2018/03/28)
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- ALKALOIDS OF FORMOSAN FISSISTIGMA AND GONIOTHALAMUS SPECIES
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Separation of the basic fractions from Formosan Fissistigma glaucescens, F. oldhamii and Goniothalamus amuyron afforded one new quaternary phenanthrene alkaloid, N-methylatherosperminium (15), along with the known alkaloids, (-)-discretamine (1), (-)-tetrahydropalmatine (2), palmatine (3), (-)-asimilobine (4), (-)-norannuradhapurine (5), (-)-crebanine (6), (-)-calycinine (fissoldine, fissistigine A) (7a), (-)-anolobine (8), (-)-xylopine (9), (-)-anonaine (10a), oxocrebanine (11), liriodenine (12), atherosperminine (13), N-noratherosperminine (14) and (+)-O-methylflavinantine (O-methylpallidine) (16) Key Word Index - Fissistigma glaucescens; F. oldhamii; Goniothalamus amuyron; Annonaceae; alkaloids; quaternary phenanthrene alkaloid; N-methylatherosperminium.
- Lu, Sheng-Teh,Wu, Yang-Chang,Leou, Shiow-Piaw
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p. 1829 - 1834
(2007/10/02)
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