[Local anesthetics. VXII. Preparation and effectiveness of dibasic alkylesters of 2-, and 3-alkoxy-substituted phenylcarbamic acids].

In a series of 24 compounds of the type of dibasic alkylesters of 2-, and 3-alkoxy substituted phenylcarbamic acids, esterified alcohols 1-dipropylamino-3-pyrrolidino (piperidino or perhydroazepino)-2-propanol were used. It follows from the results of pharmacological evaluation that these compounds possess a high index of effectiveness in surface and infiltration anaesthesia compared to the standards of cocaine and procaine. Maximum effectiveness in surface anaesthesia was shown by [1-dipropylaminomethyl)-2- (piperidino)ethyl]-ester of 3-butoxyphenylcarbamic acids whose activity is as much as 180 times higher than that of cocaine.

Effect of carbanilate local anesthetics on granulation tissue formation.

The effect of local anesthetics pentacaine ((+/-)-trans N-/2-(3-pentyloxy-phenylcarbamoyloxy)-cyclohexyl/- pyrrolidinium chloride), heptacaine (N-/2-(2-heptyloxy-phenyl-carbamoyloxy)-ethyl/-piperidini um chloride) and trimecaine (2, 4, 6-trimethylphenylcarbamoyl)-methyldiethylammonium chloride) on granulation tissue formation in open skin wounds was examined in rats. The anesthetics applied on the wounds 3 times a day for 5 days caused increase in granulation tissue weight, in DNA and hydroxyproline contents. Pentacaine had the most pronounced effects (190% dry weight, 253% DNA and 148% hydroxyproline content when compared to saline-treated controls).