抗局所麻醉薬の化学的及び薬理学的研究 (第3報)

β-Diallylaminoethyl p-aminobenzoateの合成と薬理作用

抄録

In order to find an antagoinist for the toxicity of procaine, β-diallylaminoethyl p-aminobenzoate was prepared. The free base has b.p₉ 218-220° and gives two kinds of hydrochlorides, monohydrochloride of m.p. 158-160° and dihydrochloride of m.p. 200-20° (decomp.). Lethal dose, LD₅₀, of this compound is 21.8mg./10g. by subcutaneous injection in mouse (Behrens-Kärber method), being far weaker in toxicity than procaine or cocaine. The toxic symptoms are the same as those of procaine. Though no antagonism against procaine was detected, its local anesthetic action was strong, being 2 times that of procaine and about 1/2 that of cocaine in surface anesthesia, and twice that of procaine and 1/5 to 1/2 of cocaine in filtration anesthesia. The toxicity of this compound against respiration, blood pressure, and heart action in rabbits is 1/3 to 1/2 that of procaine. Its concentrated solution effected contraction of the blood vessels while a diluted solution effected dilation, and the addition of epinephrine always effected contraction of the blood vessels. The aqueous solution of this compound was unchanged by high-temperature sterilization.