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  • Title: The ionic channel of the nicotinic acetylcholine receptor is unable to differentiate between the optical antipodes of perhydrohistrionicotoxin.
    Author: Spivak CE, Maleque MA, Takahashi K, Brossi A, Albuquerque EX.
    Journal: FEBS Lett; 1983 Nov 14; 163(2):189-93. PubMed ID: 6315487.
    Abstract:
    The enantiomers of perhydrohistrionicotoxin were studied in their effects on endplate currents recorded at the junctional region of sartorius muscles of Rana pipiens. The two optical antipodes progressively decreased the peak amplitude of the endplate currents and were indistinguishable from each other at all times. The enantiomers shortened equally the time constants for endplate current decay, but did not alter their voltage sensitivities. Although perhydrohistrionicotoxin contains 4 chiral centers, complete steric inversion does not alter its effects on the acetylcholine receptor-ion channel complex. By contrast the recognition site of the AcChR is extremely sensitive to any change in the chirality of agonists.
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