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将单咖啡因酒石酸(I;R=H)和双咖啡因酒石酸(I;R=Ⅱ),首次用作止痛剂。(Ⅰ)可以从植物资源中分得。单咖啡因酒石酸存于葡萄科,菊科和鼠李科植物。双咖啡因酒石酸存于菊科,蕨类植物和眼子菜科植物。LD_(50)≥5g/kg(小鼠po)。而阿斯匹林的LD_(50)=1.75g/kg(小鼠po)。口服剂量为每天0.3～2.5g或作其他非胃肠道给药方式剂量为0.3～2g。该药的优势在于作为止痛剂与阿斯匹林作用相当而毒性较低,且没有致溃疡作用。
For the first time, single caffeine tartaric acid (I; R = H) and dual caffeine tartrate (I; R = II) were used as analgesics. (I) can be derived from plant resources. Monocain caffeine tartrate exists in the grape family, Compositae and rhamnaceae. Double caffeine tartrate exists in Asteraceae, ferns and octopus plants. LD_ (50) ≥5 g / kg (mouse po). While LD_ (50) of aspirin = 1.75 g / kg (mouse po). Oral doses of 0.3 ~ 2.5g per day or for other parenteral administration dose of 0.3 ~ 2g. This medicine has the advantage of being as analgesic equivalent to aspirin with low toxicity and without causing ulcer.