毛地黃屬植物的衍生物具有悠久的醫療用途歷史。 英國植物學家尼古拉斯·卡爾佩珀(英語:Nicholas Culpeper)在其於1652年出版的著作《英國醫生(English physician)》中提到毛地黃的各種醫療用途[41]。而威廉·威靈被認為是在其1785年出版的著作《毛地黃及其一些醫療用途及其對水腫和其他疾病的實用評論(An Account of the Foxglove and some of its Medical Uses With Practical Remarks on Dropsy and Other Diseases)》中首次發表對毛地黃衍生物的系統性應用描述[42]。在蘇格蘭心臟學家詹姆士·麥肯錫(英語:James Mackenzie (cardiologist))爵士發現心房顫動現像以及毛地黃對其作用之前,它曾被零星應用[43]。此藥物的功效首先由蘇格蘭藥學家阿瑟·羅伯遜·庫什尼(英語:Arthur Robertson Cushny)提出解釋[44]。
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