Anticholinesterase Activity of Some Degradation Products of Physostigmine

The anticholinesterase activities of four degradation products of physostigmine have been determined in vitro using biochemical and biological assay techniques and in vivo by means of the rat chromodacryorrhea response. The degradation products are at least 100 times less active than the parent comp...

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Bibliographic Details
Published in:Journal of pharmaceutical sciences 1970-01, Vol.59 (1), p.118-120
Main Authors: Hemsworth, B.A., West, G.B.
Format: Article
Language:English
Subjects:
Animals
Anticholinesterase activity-physostigmine degradation products
Biological Assay
Biological assay-physostigmine degradation products
Chemical Phenomena
Chemistry
Cholinesterase Inhibitors - pharmacology
In vitro assay-physostigmine degradation products activity
Male
Manometry
Physostigmine - metabolism
Physostigmine-degradation products
Rats
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Summary:The anticholinesterase activities of four degradation products of physostigmine have been determined in vitro using biochemical and biological assay techniques and in vivo by means of the rat chromodacryorrhea response. The degradation products are at least 100 times less active than the parent compound as anticholinesterase agents. Eseroline, rubreserine, and eserine blue are effective in high concentrations against the cholinesterase of horse and rabbit plasma but are much less active against the red blood cell cholinesterase; they exert no inhibitory action on the two human cholinesterase enzymes. In vivo, the degradation products are at least 1000 times less active than physostigmine. Lack of coloration of solutions of physostigmine does not necessarily indicate full anticholinesterase activity because a colorless product of hydrolysis, eseroline, possesses little or no anticholinesterase activity.
ISSN:0022-3549
1520-6017
DOI:10.1002/jps.2600590128