Interrelations between drug and receptor for N-aminoacylephedrine local anesthetics

Abstract

The ability of N-(L-N-dimethylphenylalanyl)-D-ephedrine, N-(D-N-dimethylphenylalanyl)-L-ephedrine, N-(L-N-dimethylphenyl-alanyl)-L-ephedrine, N-(D-N-dimethylphenylalanyl)-D-ephedrine, N(L-N-dimethylphenylalanyl)-D-y-ephedrine, N-(D-N-dimethylphenylalanyl)-L-y-ephedrine, N-(L-N-dimethylphenylalanyl)-L-y-ephedrine, and N-(D-N-dimethylphenylalanyl)-D-y-ephedrine to block the isolated ischiadic nerve of the frog (Rana esculenta) was studied. Derivs. contg. L-phenylalanine showed the strongest anesthetic activity. Hypothetical representation of the drug-receptor binding of the anantiomers as well as a hypothetical receptor were proposed. 28 references.