Inhibition of XXXX uptake by a new psychostimulant mesocarb (Sydnocarb).

@entity1063 @entity935 @entity4478 @entity750 @entity35 @entity4944 @entity2661 @entity2955
The effect of a new psychostimulant, mesocarb was determined on the in vitro uptake of biogenic @entity4478 into synaptosomes prepared from whole @entity35 brain and various cerebral regions. @entity4944 was also examined as reference compound. On the other hand, the effects of mesocarb and @entity4944 were compared in vivo on the uptake of @entity2661 (CA) using an indirect method based on the inhibiton of cerebral CA depletion caused by intraventricularly injected @entity2955 ( @entity2955 ). Mesocarb was found to block the synaptosomal uptake of @entity935 (DA) in the striatum and whole brain more effectively than @entity4944 , but inhibited the @entity1063 (NA) uptake into hypothalamus much less than @entity4944 . The effect of mesocarb on @entity750 ( @entity750 ) uptake was not significant, similarly as that of @entity4944 . On the other hand, mesocarb inhibited the decrease of brain DA levels but had no protecting effect against NA depletion caused by @entity2955 , in vivo. @entity4944 dose-dependently inhibited NA depletion caused by @entity2955 but did not inhibit DA depletion. These findings indicate that mesocarb is a specific inhibitor of in vitro synaptosomal CA uptake, with an activity for striatal and whole brain DA uptake blockade much higher than that of @entity4944 . The results also show that mesocarb is a selective inhibitor of DA uptake in vivo, in contrast to @entity4944 , which preferentially blocks the uptake of NA in the brain. This difference may presumably be responsible for the different psychostimulatory action of the two compounds.
