Abstract

The effect of X537A on acetylcholine (ACh) release was examined in vitro in superfused slices of rat cerebrum and striatum. The ionophore (30 μM) induced a transient release of ACh which was not dependent on calcium in the medium. Also in contrast to K +-stimulated release, X537A-induced release was not sustained by 10 −5M choline in the superfusion medium and not inhibited by 5 × 10 −4M pentobarbital. The ionophore did not transport ACh or choline from an aqueous to an organic phase. Both K + and X537A inhibited 1 μM ( 3H) choline uptake into striatal synaptosomes but this effect of X537A was more extensive and less reversible than that caused by K +. X537A did not inhibit choline acetyltransferase activity.

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