Choline inhibits acetylcholine release via presynaptic muscarine receptors

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Abstract
Summary The effect of exogenous choline on the outflow of 3H-acetylcholine evoked by field stimulation was studied on the myenteric plexus-longitudinal muscle preparation of the guinea pig. Choline at concentrations of 100 μM and higher depressed the evoked outflow of 3H-acetylcholine in a concentration-dependent manner. The EC 50 for the inhibitory action was 300 μM. Scopolamine (10 nM) antagonized the effect of choline which indicates that the inhibition of 3H-acetylcholine outflow is mediated by muscarine receptors. The findings imply that choline at high concentrations does not improve cholinergic synaptic neurotransmission in tissues that are endowed with presynaptic muscarine receptors (e.g. myenteric and central cholinergic neurones). Furthermore, it is suggested that the increase in tissue acetylcholine content that has been observed after choline administration is probably due to the depression of acetylcholine release.