Lecithin-cholesterol acyltransferase: inhibition by local anesthetics in plasma from man and experimental animals in vitro.
Lecithin-cholesterol acyltransferase (LCAT, EC 2.3.1.43) was assayed in vitro in plasma from normal man, rat, rabbit and dog by following the formation of 14C-cholesteryl esters subsequent to labeling the plasma with 14C-cholesterol in vitro. In all species examined, various local anesthetics were found to inhibit LCAT when studied over the concentration range of 1 to 5 mM. The order of inhibition was dibucaine>benzocaine>tetracaine>lidocaine>procaine. Since LCAT activity represents the combined effect of a deacylation step and an esterification step, inhibition of LCAT by local anesthetics could theoretically involve either or both steps.
D000328:Adult; D000779:Anesthetics, Local / Q000494:pharmacology*; D000818:Animals; D002788:Cholesterol Esters / Q000096:biosynthesis; D004285:Dogs; D004305:Dose-Response Relationship, Drug; D004951:Esterification; D006801:Humans; D008012:Lidocaine / Q000494:pharmacology; D008297:Male; D007862:Phosphatidylcholine-Sterol O-Acyltransferase / Q000037:antagonists & inhibitors / Q000097:blood*; D011817:Rabbits; D051381:Rats; D013748:Tetracaine / Q000494:pharmacology
D000779:Anesthetics, Local; D002788:Cholesterol Esters; D013748:Tetracaine; D008012:Lidocaine; D007862:Phosphatidylcholine-Sterol O-Acyltransferase