title: Cinchocaine and amethocaine inhibit activation and activity of superoxide production in human neutrophils.
abstract: Local anaesthetics, cinchocaine and amethocaine, inhibited superoxide production in human neutrophils stimulated by phorbol ester, with IC50 (concentration of a drug giving 50% activity of control) values of 0.2 and 0.6 mmol litre-1, respectively. These anaesthetics inhibited protein (de)phosphorylation and mobilization of membrane-associated calcium, both of which are probable signal transmission mechanisms for the induction of superoxide production. Local anaesthetics also inhibited NADPH oxidase, responsible for superoxide production, with IC50 = 0.3 and 0.9 mmol litre-1, respectively. The results indicate that cinchocaine and amethocaine inhibit superoxide production in human neutrophils by affecting not only the catalytic activity, but also the activation, of NADPH oxidase.
mesh_terms: D001798:Blood Proteins / Q000378:metabolism; D002118:Calcium / Q000378:metabolism; D003864:Depression, Chemical; D003992:Dibucaine / Q000494:pharmacology*; D006801:Humans; D066298:In Vitro Techniques; D009247:NADH, NADPH Oxidoreductases / Q000037:antagonists & inhibitors; D019255:NADPH Oxidases; D009504:Neutrophils / Q000187:drug effects* / Q000378:metabolism; D010766:Phosphorylation; D013481:Superoxides / Q000378:metabolism*; D013748:Tetracaine / Q000494:pharmacology*
chemical_list: D001798:Blood Proteins; D013748:Tetracaine; D013481:Superoxides; D009247:NADH, NADPH Oxidoreductases; D019255:NADPH Oxidases; D003992:Dibucaine; D002118:Calcium