Inhibition effects of benactyzine and drofenine on human serum butyrylcholinesterase.
Benactyzine and drofenine are widely used anticholinergic drugs. Benactyzine is used to treat organophosphate poisoning and drofenine acts on smooth muscle to stop muscle spasms. Both of these drugs are esters. After they enter the bloodstream, they will interact with butyrylcholinesterase (BChE; acylcholine acyl hydrolase: EC 3.1.1.8), which has an ability to hydrolyze a wide variety of esters. Therefore, the kinetic analysis of their inhibitory effects on human serum BChE was examined using butyrylthiocholine as substrate. Both drugs were competitive inhibitors of BChE and the Ki values of benactyzine and drofenine were calculated to be 0.010 +/- 0.001 and 0.003 +/- 0.000 mM, respectively, using the Systat (version 5.03, 1991) nonlinear regression analysis software package. According to these parameters, drofenine is a more potent competitive inhibitor of BChE than benactyzine.
Bodur
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Department of Biochemistry, Faculty of Medicine, Hacettepe University, Ankara, Turkey.
Cokuğraş
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AN
Tezcan
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EF
D001535:Benactyzine / Q000494:pharmacology*; D001667:Binding, Competitive; D002091:Butyrylcholinesterase / Q000097:blood* / Q000378:metabolism*; D002800:Cholinesterase Inhibitors / Q000494:pharmacology*; D006801:Humans; D007700:Kinetics; D016014:Linear Models; D008956:Models, Chemical; D010648:Phenylacetates / Q000494:pharmacology*; D011485:Protein Binding; D011487:Protein Conformation
D002800:Cholinesterase Inhibitors; D010648:Phenylacetates; C007183:cycloadiphenine; D001535:Benactyzine; D002091:Butyrylcholinesterase