Abstract
Publisher Summary This chapter discusses the mechanism of action of crotoxin on the postsynaptic membrane. It has been shown that crotoxin very efficiently and irreversibly blocks the cholinergic postsynaptic response of isolated electroplaque from electrophorus electricus and of subcellular microsacs from Torpedo marmorata. This postsynaptic effect has been investigated by studying the binding of crotoxin and of its components to acetylcholine receptor rich membrane fragments from Torpedo and by analyzing the relationship between its catalytic activity and its pharmacological effect on electrophorus electroplaque. The chapter describes two distinct steps were recognized in the action of crotoxin: a quasi irreversible binding step of the catalytic subunit, which has no blocking effect by itself, and a catalytic step, which is responsible for the postsynaptic blockade of the electroplaque response. The results suggest that the acidic component of crotoxin enhances the pharmacological action of the phospholipase subunit by preventing its absorbtion to nonsaturable membrane sites and, thus, restricting its binding to specific critical target sites.
Published Version
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