我的账户 7×24小时客服热线:400-829-7929 语言:
热门产品: 原人参二醇,雷公藤甲素,虫草素,6-姜酚,中药成分化合物库
产品分类
在线咨询
联系电话:
销售:
400-829-7929(7*24小时)
028-82633860
028-82633397 
028-
82633165
技术服务和产品定制:
028-82633987
在线服务:  
沈帅 点击这里给我发消息 
文静  点击这里给我发消息
文献信息

Synthesis and evaluation of nuciferine and roemerine enantiomers as 5-HT2 and α1 receptor antagonists

期刊名:MedChemComm
文献编号:
文献地址: http://pubs.rsc.org/en/content/articlelanding/2018/md/c7md00629b/unauth#!divAbstract
发表日期:26 Feb 2018
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 α1receptors. (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.


… Experimental. Chemicals. (S)-Nuciferine and (S)-roemerine were prepared as described in the supplementary information. (R)-Nuciferine and (R)-roemerine were obtained from Chengdu Biopurify Phytochemicals Ltd. (Chengdu, China) and Pharmeks Ltd … 
相关产品
在线客服系统