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东莨菪碱是洋金花的主要有效成分,是中枢 M-胆碱能受体的阻滞剂,能阻抑人们的意识活动,与氯丙嗪合用于中药麻醉,存在镇痛不全、肌松作用不强等缺点,不能充分满足外科手术的要求。为了克服这些缺点,进行了构效关系的研究。已知东莨菪碱的氧桥和α-H 是必需的,否则会明显减弱中枢作用,故我所合成室从醇基做成酯类衍生物(见下图)。我们观察家兔翻正反射(脑室注射)和肌张力减弱、拮抗颤抖素的镇痛作用(M-胆碱能中枢激动作用)和扩瞳表现,比较它们的作用情况,发现化合物Ⅵ和Ⅷ的中枢作用较强。所有衍生物均能拮抗颤抖素的中枢作用和扩瞳现象。现正合成新化合物,进一步开展受体结合试验。
Scopolamine is the main active ingredient of the flower, is a central blockers of M-cholinergic receptors, can inhibit people’s awareness activities, and chlorpromazine used in traditional Chinese medicine anesthesia, there is incomplete analgesic, muscle relaxant effect Strong shortcomings, can not fully meet the requirements of surgery. In order to overcome these shortcomings, the structure-activity relationship has been studied. The scopolamine oxygen bridge and a-H are known to be essential, otherwise the central action is significantly diminished, so my synthesis chamber is ester derivative of alcohol (see below). We observed that the rabbit reflex (intracerebroventricular injection) and hypotonia, antagonism of the analgesic effect of tretinoin (M-cholinergic central stimuli) and dilated pupil performance comparison of their role and found that compounds VI and VIII Central role of strong. All derivatives can antagonize the central role of dandruff and dilation phenomenon. New compounds are being synthesized to further carry out receptor binding experiments.