Abstract
Data are presented on the corneal anesthetic activity and systemic toxicity of 22 local anesthetics, including cocaine, tetracaine, dibucaine, procaine and Thiocaine® and 2-alkoxy derivatives of the last two compounds.In the procaine as well as in the Thiocaine® series, 2-propoxy or higher alkoxy substitution greatly increased activity and toxicity with the increase in length of the alkoxy side chain.The thiolbenzo- ates were considerably more active and toxic than the corresponding benzoates.WIN 4510, the 2-hexyloxy analog of Thiocaine®, was found to be approximately 500 times as active as cocaine.The intravenous toxicity of this compound in mice was only 60 times greater than that of cocaine.
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