Title : The inhibition of acetylcholinesterase by dantrolene and ondansetron.

Pub. Date : 2015 Jan

PMID : 24764253






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1 The inhibition of acetylcholinesterase by dantrolene and ondansetron. Dantrolene acetylcholinesterase (Cartwright blood group) Homo sapiens
2 PURPOSE: A virtual screening study has suggested that the skeletal muscle relaxant, dantrolene, and the antiemetic drug, ondansetron, may act as inhibitors of the enzyme acetylcholinesterase (AChE). Dantrolene acetylcholinesterase (Cartwright blood group) Homo sapiens
3 PURPOSE: A virtual screening study has suggested that the skeletal muscle relaxant, dantrolene, and the antiemetic drug, ondansetron, may act as inhibitors of the enzyme acetylcholinesterase (AChE). Dantrolene acetylcholinesterase (Cartwright blood group) Homo sapiens
4 METHODS AND FINDINGS: Using AChE from human erythrocytes as enzyme source, it is shown that dantrolene and ondansetron inhibit AChE with IC(50) values of 12.8 microM and 37.1 microM, respectively. Dantrolene acetylcholinesterase (Cartwright blood group) Homo sapiens
5 METHODS AND FINDINGS: Using AChE from human erythrocytes as enzyme source, it is shown that dantrolene and ondansetron inhibit AChE with IC(50) values of 12.8 microM and 37.1 microM, respectively. Dantrolene acetylcholinesterase (Cartwright blood group) Homo sapiens
6 By measuring the recoveries of enzyme activities after dilution of enzyme-inhibitor mixtures, it is further shown that dantrolene and ondansetron act as reversible AChE inhibitors. Dantrolene acetylcholinesterase (Cartwright blood group) Homo sapiens
7 CONCLUSIONS: By considering the typical plasma concentrations of dantrolene and ondansetron in humans at therapeutic doses, the pharmacological relevance of the AChE inhibitory potencies of these drugs is discussed. Dantrolene acetylcholinesterase (Cartwright blood group) Homo sapiens
8 In contrast, after intravenous administration of dantrolene to humans, the typical plasma concentrations reached are similar to the recorded IC(50) value for the inhibition of AChE, and dantrolene may thus produce pharmacological significant inhibition of AChE. Dantrolene acetylcholinesterase (Cartwright blood group) Homo sapiens
9 In contrast, after intravenous administration of dantrolene to humans, the typical plasma concentrations reached are similar to the recorded IC(50) value for the inhibition of AChE, and dantrolene may thus produce pharmacological significant inhibition of AChE. Dantrolene acetylcholinesterase (Cartwright blood group) Homo sapiens
10 In contrast, after intravenous administration of dantrolene to humans, the typical plasma concentrations reached are similar to the recorded IC(50) value for the inhibition of AChE, and dantrolene may thus produce pharmacological significant inhibition of AChE. Dantrolene acetylcholinesterase (Cartwright blood group) Homo sapiens
11 In contrast, after intravenous administration of dantrolene to humans, the typical plasma concentrations reached are similar to the recorded IC(50) value for the inhibition of AChE, and dantrolene may thus produce pharmacological significant inhibition of AChE. Dantrolene acetylcholinesterase (Cartwright blood group) Homo sapiens
12 Further investigation is necessary to clarify the pharmacological relevance of the AChE inhibitory effect of dantrolene. Dantrolene acetylcholinesterase (Cartwright blood group) Homo sapiens