Regulation of high affinity choline uptake.

High affinity uptake of choline, the rate-limiting, regulatory step for the synthesis of acetylcholine (ACh), was found to be regulated via presynaptic auto- and heteroreceptors. The transport rate was reduced by a muscarinic agonist and neuropeptides, but was significantly enhanced by octopamine. Intracellular messengers, including cyclic nucleotides, appear to modulate the transport activity, apparently by activating specific protein kinases.