The inhibition of acetylcholine synthesis in brain by a hemicholinium

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Abstract
The inhibition by HC3 of acetylcholine synthesis in minced mouse brain has been confirmed. The inhibition was observed also in minced guinea-pig brain. The synthesis of acetylcholine by homogenates of guinea-pig brain or by particles obtained from them was inhibited by HC3 only if the concentration of choline was low. When these preparations were treated with ether the increased synthesis of acetylcholine that occurred was activated by HC3. This effect was more marked with the cruder preparations. It was concluded that HC3 does not inhibit choline acetylase directly but that it competes with choline for access to the enzyme through structural barriers in the cell. The relation of these findings in vitro to the high toxicity of HC3 is discussed.