Acetylcholinesterase therapeutic applications

The special case of the endogenous transmitter acetylcholine illustrates well the high velocity of ester hydrolysis. Acetylcholine is broken down at its sites of release and action by acetylcholinesterase (pp. 100,102) so rapidly as to negate its therapeutic use. Hydrolysis of other esters catalyzed by various esterases is slower, though relatively fast in comparison with other biotransformations. The local anesthetic, procaine, is a case in point it exerts its action at the site of application while being largely devoid of undesirable effects at other locations because it is inactivated by hydrolysis during absorption from its site of application. 

Galanthamine also blocks acetylcholine estaase activity. One of the new applicaticms of galanthamine is in a treatment of Alzheimer s disease (AD). Moreover, this natural (and presently also synthetically driven) alkaloid can be used in decreasing negative side effects caused by applications of nondepolarizing alkaloids, for example, those of tubocurarine. Acetylcholinesterase activity is reported to depress and inhibit by lycorine and its derivatives. Lycorine is an object of therapeutic approaches to cure AD and decrease a level of esterase activity, Other alkaloids from the Amaiyllidaceae plant family are probably useful for these purposes and are being researched. 

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