Lignocaine: inhibitory effect on synaptosomal and erythrocyte membrane-bound acetylcholinesterase activity.
Lignocaine (5-20 mM) reversibly inhibits (in vitro) AChE activity of rat brain synaptosome (33-66%) and erythrocyte membrane (10-54%) in a concentration dependent manner. Lineweaver-Burk plots indicate that lignocaine-induced inhibition of AChE activity in synaptosome is competitive, whereas in erythrocyte membrane inhibition of AChE is non-competitive in nature. Arrhenius plots show that transition temperatures of both synaptosomal and erythrocyte membrane-bound AChE are significantly reduced in the presence of lignocaine. These results suggest that lignocaine increases the lipid fluidity of synaptosomal and erythrocyte membrane which may be a cause of inhibition of membrane-bound AChE activity.
D000110:Acetylcholinesterase / Q000378:metabolism*; D000818:Animals; D001921:Brain / Q000201:enzymology; D002800:Cholinesterase Inhibitors / Q000494:pharmacology*; D004910:Erythrocyte Membrane / Q000201:enzymology*; D008012:Lidocaine / Q000494:pharmacology*; D008297:Male; D051381:Rats; D013574:Synaptosomes / Q000201:enzymology*; D013816:Thermodynamics
D002800:Cholinesterase Inhibitors; D008012:Lidocaine; D000110:Acetylcholinesterase