Acetylcholinesterase inhibition by pitofenone: a spasmolytic compound. |
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Authors: | N S Punekar A V Kulkarni |
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Institution: | Chemistry Department, Indian Institute of Technology, Powai, Bombay. |
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Abstract: | Pitofenone, a spasmolytic compound, inhibited the acetylcholinesterase activity from bovine erythrocytes and from electric eel. It is a potent inhibitor of this enzyme from the two sources, with Ki values of 36 and 45 microM, respectively. Of the five compounds structurally related to pitofenone, only those containing a piperidine moiety show acetylcholinesterase inhibition. All these inhibitions are reversible, linear, and noncompetitive in nature. A qualitative correlation between the anticholinesterase and the corresponding antimuscarinic activity for some of these compounds was apparent. Good separation of these two effects would be a desirable feature for newer muscarinic antagonists. |
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