局所麻酔作用を有する新しい1-Aroyloxy-2-dialkylaminocycloalkane誘導体の薬理作用

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Local anesthetic activites and other pharmacological actions of dl-cis-1-benzoyloxy-2-dimethylamino-1,2,3,4-tetrahydronaphthalene (III) and its related compounds, including different types of chemical structures and stereoisomers, were examined. 1) The new series of compounds (I-VI) were found to have potent local anesthetic effect in guinea-pigs. Among them, III and a 4-aminobenzoloxy derivative (V) were more active than reference substances (procaine, lidocaine, and cocaine). 2) Introduction of an amino group into 4-position of the lipophilic benzoyloxy group of III intensified the local anesthetic activity. In IV, which is a trans-isomer of the cis-compound (III), positional interchange of benzoyloxy and dimethylamino groups on the tetraline ring resulted in complete loss of the activity. Accordingly, it was considered that the position of benzoyloxy and dimethylamino groups on the tetraline ring was of great importance for their local anesthetic activities. On the other hand, replacement of the ester group by ether group in III reduced the activity slightly. Another compound (VIII) substituted by phenyl group at 1-carbon atom of 2-diethylaminoethanol chain of procaine was more active than the original substance but less potent than the cyclic structured III. 3) Activity of the cis-form (III) exceeded that of the trans-isomer (IV) in corneal anesthesia. Similarly. dl-cis-1-benzoyloxy-2-dimethylaminoindane (I) was more potent than the corresponding trans-compound (II). 4) Highly significant relationship was found to exist between the intracutaneous anesthetic activity in guinea-pigs and the intravenous acute toxicity in mice for compounds I-V, VIII, procaine, lidocaine, and cocaine. However, no corrleation could be established between the anesthetic activity and the spasmolytic effect in isolated ileum of guinea-pigs.
社団法人日本薬学会の論文
1976-01-25

局所麻酔作用を有する新しい1-Aroyloxy-2-dialkylaminocycloalkane誘導体の薬理作用

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