Studies on Local Anesthetics. Pharmacological Properties of Homologaes and Isomeres of Xylocnin (Alkyl Amino‐Acyl Derivatives)

作者：Leonard Goldberg · 发表于：Acta Physiologica Scandinavica · 年份：1949 · DOI：10.1111/j.1748-1716.1949.tb00591.x · 被引用次数：147 · 研究领域：Olfactory and Sensory Function Studies、Essential Oils and Antimicrobial Activity、Photochromic and Fluorescence Chemistry

Summary. Pharmacological properties of fifteen homologues and isonieres of xylocain, being alkyl‐amino‐acyl derivatives (table 1) were investigated. All compounds were tested in a 2 % solution, pH adjusted to 5.8–5.9. The convulsive dose (CD50) varied between 0.25 and 0.5 g/kg, the lethal dose (LD50) between 0.3 and 2 g/kg; both were established in white mice. All compounds caused a fall in the rabhit's blood pressure. In combination with adrenaline a concentration of more than 1: 333,000 (3 μg/ml) increased blood pressure. The compounds were potent local anesthetics, causing a surface anesthesia on the rabbit's eye with an absolute duration of 12–70 minutes and a total demotion of 4–7 hours. The infiltration anesthesia in dermal wheals in guinea‐pigs lasted in a 1 % and 2 % solution up to 300 minutes; addition of adrenaline 1: 50,000 (20 μg/ml) caused a marked increase, showing the compatibility with adrenaline. The irritant effect varied for the different compounds, xylocain and LL 31 (2,4,6) being not irritant neither in the rabbit's ear nor in man. A relation between chemical constitution and pharmacological action was assumed and varied for each property studied.