Abstract
Summary MK-212 inhibited the uptake of 3H-serotonin in cerebral cortical tissue with an EC50 of about 10 μM. At 10 μM, MK-212 did not affect the uptake of 3H-norepinephrine. Inhibition of serotonin and catecholamine uptake in vivo was assessed by determining the effect of pretreatment with MK-212 on the ability of p-chloroamphetamine and H 77/77 to decrease, respectively, the concentration of serotonin and catecholamines in rat brain. MK-212, 2.5–10 mg/kg i.p., produced a dose-related antagonism of the serotonin-lowering action of p-chloroamphetamine, while the H 77/77-induced reductions in norepinephrine and dopamine were not inhibited by prior administration of MK-212. Inhibition of the neuronal reuptake system for serotonin may contribute to the previously described serotoninmimetic action of MK-212 in the central nervous system.
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