Pub. Date : 2015 Jan
PMID : 24764253
12 Functional Relationships(s)Download |
Sentence | Compound Name | Protein Name | Organism |
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 |