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Relationship between the effects of dexamphetamine on locomotion and on striatal [3H]GBR 12783 binding in vivo

Abstract : In mice, low doses (1-2-4 mg/kg s.c.) of dexamphetamine stimulated locomotor activity in a dose-dependent manner. Over the same range of doses the drug dose dependently inhibited the in vivo striatal binding of the dopamine uptake inhibitor, [3H]GBR 12783. At 3 mg/kg dexamphetamine, the stimulant effect and the inhibition of the striatal binding of [3H]GBR 12783 displayed a similar time course. Pretreatments that either increased (L-DOPA 200 mg/kg, benserazide 50 mg/kg i.p.) or decreased (reserpine 5 mg/kg s.c., alpha-methyl-p-tyrosine 200 mg/kg) striatal dopamine levels did not modify the inhibition by dexamphetamine of [3H]GBR 12783 binding in vivo. This suggests that the inhibition is due to a direct effect of dexamphetamine, not mediated by endogenous dopamine, and further that a unique site is responsible for the neuronal uptake of dexamphetamine and for the binding of pure dopamine uptake inhibitors.
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https://hal-normandie-univ.archives-ouvertes.fr/hal-02186997
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Submitted on : Wednesday, July 17, 2019 - 3:30:25 PM
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J. M. Vaugeois, J J Bonnet, J Costentin. Relationship between the effects of dexamphetamine on locomotion and on striatal [3H]GBR 12783 binding in vivo. European Journal of Pharmacology, 1990, 178 (2), pp.221-7. ⟨10.1016/0014-2999(90)90478-o⟩. ⟨hal-02186997⟩

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