Acetylcholinesterase inhibition by pitofenone: a spasmolytic compound.
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.
Punekar
N S
NS
Chemistry Department, Indian Institute of Technology, Powai, Bombay.
Kulkarni
A V
AV
D000110:Acetylcholinesterase / Q000378:metabolism*; D000818:Animals; D001577:Benzophenones / Q000737:chemistry / Q000494:pharmacology*; D002417:Cattle; D002800:Cholinesterase Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D004593:Electrophorus; D004912:Erythrocytes / Q000201:enzymology; D015394:Molecular Structure; D010276:Parasympatholytics / Q000737:chemistry / Q000494:pharmacology*; D010880:Piperidines; D013329:Structure-Activity Relationship
D001577:Benzophenones; D002800:Cholinesterase Inhibitors; D010276:Parasympatholytics; D010880:Piperidines; D000110:Acetylcholinesterase; C015454:pitofenone