Mathematical model of the cut-off effect in the homologous series of tertiary amine local anesthetics

• Published in: Pharmazie Vol. 48; no. 6; p. 446
• Main Authors: Uhríková, D, Cherezov, V, Yaradaikin, S, Balgavý, P
• Format: Journal Article
• Language: English
• Published: Germany 01.06.1993
• Subjects: Amines - chemical synthesis; Amines - pharmacology; Anesthetics, Local - chemical synthesis; Anesthetics, Local - pharmacology; Carbamates - chemistry; Models, Theoretical; Phosphatidylcholines - chemistry; Piperidines - chemistry; Structure-Activity Relationship; X-Ray Diffraction

It is proposed a simple mathematical model explaining the quasi parabolic dependence of the local anesthetic activity on the length of hydrophobic substituent in the homologous series of tertiary amines (TA). It is suggested that the molecules of TA intercalate between the lipid molecules in bilayer...