Correction: Synthesis and evaluation of nuciferine and roemerine enantiomers as 5-HT2 and α1 receptor antagonists
| العنوان: | Correction: Synthesis and evaluation of nuciferine and roemerine enantiomers as 5-HT2 and α1 receptor antagonists |
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| المؤلفون: | Hui Li Heng, Chin Fei Chee, Sek Peng Chin, Yifan Ouyang, Hao Wang, Michael J. C. Buckle, Deron R. Herr, Ian C. Paterson, Stephen W. Doughty, Noorsaadah Abd. Rahman, Lip Yong Chung |
| المصدر: | MedChemComm |
| بيانات النشر: | Royal Society of Chemistry, 2018. |
| سنة النشر: | 2018 |
| مصطلحات موضوعية: | Pharmacology, Chemistry, Drug Discovery, Organic Chemistry, Pharmaceutical Science, Molecular Medicine, Biochemistry |
| الوصف: | 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-HT(2) and adrenergic α(1) 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-HT(2) and α(1) receptors. (R)-roemerine was the most potent compound at 5-HT(2A) and 5-HT(2C) receptors (pK(b) = 7.8–7.9) with good selectivity compared to (S)-roemerine at these two receptors and compared to its activity at 5-HT(2B), α(1A), α(1B) and α(1D) receptors. |
| اللغة: | English |
| تدمد: | 2040-2511 2040-2503 |
| الوصول الحر: | https://explore.openaire.eu/search/publication?articleId=doi_dedup___::1e96d643ae87762136ecf37733c019dcTest http://europepmc.org/articles/PMC6144813Test |
| حقوق: | OPEN |
| رقم الانضمام: | edsair.doi.dedup.....1e96d643ae87762136ecf37733c019dc |
| قاعدة البيانات: | OpenAIRE |
| تدمد: | 20402511 20402503 |
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