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The effects of quipazine on serotonin metabolism in rat brain.
Authors:R W Fuller  H D Snoddy  K W Perry  B W Roush  B B Molloy  F P Bymaster  D T Wong
Institution:The Lilly Research Laboratories, Eli Lilly and Company Indianapolis, Indiana 46206, USA
Abstract:Quipazine, 2-(1-piperazinyl)-quinoline, is a drug that has been reported to stimulate serotonin receptors in brain. We therefore studied the effect of quipazine on several parameters of serotonin metabolism in rat brain. Quipazine caused a slight, dose-related elevation of serotonin levels and decrease in 5-hydroxyindoleacetic acid levels for 2–4 hrs after it was administered. The decrease in 5-hydroxyindoleacetic acid levels was probably due primarily to a depression of 5-hydroxyindole synthesis, since quipazine also decreased the rate of 5-hydroxytryptophan accumulation after NSD 1015, the rate of serotonin decline after α-propyldopacetamide, and the rate of 5-hydroxyindoleacetic acid accumulation after probenecid. The elevation of serotonin was probably due to weak inhibition of monoamine oxidase. Quipazine reversibly inhibited the oxidation of serotonin by rat brain monoamine oxidase invitro and protected against the irreversible inactivation of the enzyme invivo. Quipazine also was a potent inhibitor of serotonin uptake into brain synaptosomes invitro and attained concentrations in brain higher than the invitro IC50. However, quipazine did not prevent the depletion of brain serotonin by p-chloroamphetamine invivo. In addition to stimulating serotonin receptors in brain, quipazine may inhibit monoamine oxidase and serotonin reuptake invivo.
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