Octopamine uptake and metabolism in the insect nervous system.

Several insect tissues were examined for their ability to take up octopamine in the presence and absence of sodium ions. The cockroach Malpighian tubules, ovary, and ventral nerve cord showed the highest level of sodium-dependent uptake. The adult firefly lantern exhibited substantial sodium-independent uptake. Some of these tissues were also examined for their ability to metabolize octopamine by N-acetylation. Measurable N-acetyltransferase activity was present in the cockroach ventral nerve cord, tobacco hornworm CNS, and firefly light organ. N-Acetylation is proposed to be the major metabolic pathway for octopamine in the cockroach (Periplaneta americana) nervous system. Several classes of compounds, including octopamine receptor agonists, tricyclic antidepressants, amphetamines, chloroethylbenzylamines, and some experimental insecticides, were tested for their ability to inhibit octopamine uptake and metabolism. The sodium-insensitive component of uptake was not inhibited by most compounds tested, but the sodium-sensitive component was strongly inhibited by xylamine, N-ethyl-N-chloroethyl-o-bromobenzylamine, and their aziridinium ions (60-100%). These compounds also effectively inhibited N-acetyl-transferase (IC50 values at or below 1 microM). Other good inhibitors of N-acetyltransferase included desipramine, synephrine, and an experimental insecticide, CGA 132427. Formamidine pesticides had limited effect on both processes, and neither action seems likely to be involved in their octopaminergic actions in vivo. Cocaine was unique in stimulating N-acetyltransferase activity. When inhibition of sodium-sensitive uptake is compared with inhibition of N-acetyltransferase in the cockroach ventral nerve cord, two groups of inhibitors are discernible. Type 1 compounds inhibit uptake without an effect on N-acetyltransferase, whereas type 2 compounds inhibit both processes. These results suggest a functional linkage between the uptake and acetylation of octopamine.