Abstract
HEMICHOLINIUM (HC-3) has been shown to possess a strong inhibitory effect on acetylcholine (ACh) synthesis in nervous tissue which can be effectively antagonized by choline1–6. Similar activity, though to a lesser degree, has been demonstrated in tetraethylammonium (TEA)7,8. Replacement of the ethyl group of TEA by methyl, propyl or butyl results in a significant reduction of the inhibitory activity. Recently, we have demonstrated that troxy-pyrrolidinium (ethyl-2(3,4,5- trimethoxybenzoyloxy) ethyl pyrrolidinium iodide) possesses hemicholinium-like activity but is less toxic9. In the work recorded here, a series of trimethoxybenzoic acid esters are compared to determine the structure/activity relationship.
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BHATNAGAR, S., LAM, A. & MCCOLL, J. Inhibition of Synthesis of Acetylcholine by Some Esters of Trimethoxybenzoic Acid. Nature 204, 485–486 (1964). https://doi.org/10.1038/204485b0
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DOI: https://doi.org/10.1038/204485b0
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