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Inhibition of [3H]acetylcholine active transport by tetraphenylborate and other anions

DC Anderson, SC King and SM Parsons

The effects of tetraphenylborate and other anions on the active uptake of [3H]acetylcholine by synaptic vesicles isolated from Torpedo californica electric organ were studied. Tetraphenylborate completely inhibits active uptake with a half-inhibitory concentration of 0.3 microM. Dipicrylaminate also half-inhibits at 0.3 microM, phenyldicarbaundecaborane at 14 microM, fluoride at 2 mM, thiocyanate at 3 mM, and azide at 16 mM. Tetraphenylborate had no effect on the vesicle ATPase activity or the transmembrane electric potential at low concentrations where it inhibits [3H]acetylcholine active transport. The mechanism for tetraphenylborate inhibition is uncertain, but it might be similar to that of its action as a mitochondrial uncoupler. Solubility products for the acetylcholine, choline, and potassium salts of the tetraphenylborate and dipicrylaminate anions also were measured. The inhibition results confirm the hypothesis of Marshall and Parsons [Br. J. Pharmacol. 54:333-338 (1975)] that tetraphenylborate acts on intact neuromuscular preparations to inhibit transmitter storage, and constitute new pharmacological evidence that evoked release of acetylcholine is mediated by synaptic vesicles.

Volume 24, Issue 1, pp. 55-59, 07/01/1983
Copyright © 1983 by American Society for Pharmacology and Experimental Therapeutics






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