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由4-正-烷氧基-正-烷氧基-3-乙基苯乙酮生成的β-氨基酮化合物是一类长效、低毒、水溶性好的强力表面麻醉剂。其中效能最好的是:β-六氢吡啶乙基-[4-δ-正-丁氧基-正-丁氧基-3-乙基苯基]酮盐酸盐(Ⅰ_a)。 4-δ-正-丁氧基-正-丁氧基这个基团对于获得这些优良性能起着决定性作用:β-六氢吡啶乙基-[4-正-丁氧基-3-乙基苯基]酮盐酸盐(Ⅰ_b)的麻醉作用强,吸收快,但作用时间中等;增大烷氧基至辛氧基(即化合物Ⅰ_c)虽能延长作用时间,但却降低吸收速度和麻醉作用。在化合物Ⅰ_c的辛氧基中间引入氧原子,即得化合物Ⅰ_a,它兼具化合物Ⅰ_b及Ⅰ_c的优点。化合物Ⅰ_a的表面麻醉作用与市售麻醉药的比较(角膜法):
The 4-n-alkoxy-n-alkoxy-3-ethylacetophenone-generated β-aminoketone compounds are a class of powerful surface anesthetics with long-lasting, low toxicity and water-solubility. Among them, the best performance is: β-piperidine ethyl- [4-δ-n-butoxy-n-butoxy-3-ethylphenyl] ketone hydrochloride (Ⅰ_a). 4-δ-n-Butoxy-n-butoxy This group plays a decisive role in achieving these excellent properties: β-piperidine-ethyl- [4-n-butoxy-3-ethylbenzene (Ⅰ_b) has a strong anesthetic effect and fast absorption, but the action time is moderate. Increasing the alkoxy group to octyloxy group (ie compound I_c) prolongs the action time but decreases the absorption rate and the anesthetic effect . The oxygen atom is introduced into the octyloxy group of compound I_c to obtain compound I_a, which has the advantages of compound Ⅰ_b and Ⅰ_c. Comparison of topical anesthetic effects of Compound I_a with commercially available anesthetics (corneal method):