1954
DOI: 10.1038/173033a0
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Inhibition of Esterases by the Fluorides of Organic Acids

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Cited by 88 publications
(37 citation statements)
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“…A fact that does not support this suggestion is that it is possible to obtain 50% inhibition of the true cholinesterase of rat brain with 4 x 10-M dimethylcarbamoyl fluoride Fig. 1 (Myers & Kemp, 1954); since this represents the maximum possible value of KI and the minimum value calculated above is about 1 x 10-7M, it is evident that k2 could not in any case be much greater than kD.…”
Section: Discussionmentioning
confidence: 87%
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“…A fact that does not support this suggestion is that it is possible to obtain 50% inhibition of the true cholinesterase of rat brain with 4 x 10-M dimethylcarbamoyl fluoride Fig. 1 (Myers & Kemp, 1954); since this represents the maximum possible value of KI and the minimum value calculated above is about 1 x 10-7M, it is evident that k2 could not in any case be much greater than kD.…”
Section: Discussionmentioning
confidence: 87%
“…The aliesterases of serum and brain were determined with a 0-2% (v/v) emulsion of tributyrin stabilized with 0-1% gum acacia (final concentrations). Although the activities of these two ali-esterases are measured in the same way, it should be noted that the ali-esterase of serum is a different enzyme from that found in brain Mendel, Myers, Uyldert, Ruys & Bruyn, 1953;Myers & Kemp, 1954). The cholinesterases present in serum, on the other hand, appear to be identical with those found in other tissues (Ord & Thompson, 1952;Myers, 1953;Davison, 1953).…”
Section: Methodsmentioning
confidence: 98%
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“…We calculated the total it electron density and the superdelocalizability for a nucleo philic reactivity on various positions of several substituted phenyl N-metyl carbamates and found that the total it electron density of the ethereal oxygen atoms and, though in the lesser degree, that of the carbonyl oxygen atoms had almost linear correlation with the house-fly brain cholinesterase inhibitory potency observed by Kolbezen et al There have been some indications that the binding of some of the phenyl carbamates such as prostigmine requires the basic group in the esteratic site of the enzyme (14), and furthermore, that some of the carbamates might form the carbamoyl derivatives of the cholinesterase at its esteratic site (5,11,12,(15)(16)(17)(18) in a manner similar to that in which the dialkyl phosphates phosphorylate the enzyme.…”
Section: Resultsmentioning
confidence: 99%
“…There is scope, however, for a number of parameters to be altered in these attempts. It is intcresting that some sulfonyl halides of this type are potent anti-cholinesterases (193). It would be useful to examine these inhibitions further to see if they differ in any way from phosphoryl ones, and to see whether these cornpounds have any effect on the fluorophosphatases.…”
Section: G a Note On Applicationsmentioning
confidence: 99%