Diclofensine

Diclofensine (Ro 8-46500) is an orally active neuronal monoamine uptake inhibitor. Diclofensine blocks the uptake of dopamine, noradrenaline, and serotonin by rat brain synaptosomes with IC₅₀ values of 0.74, 2.3 and 3.7 nM, respectively. Diclofensine potentiates norepinephrine-induced hypertension and attenuates Tyramine (HY-W007606)-induced hypertension. Diclofensine produces psychostimulant and mood-elevating effects without causing sudden disappearance or withdrawal reactions. Diclofensine can be used in the research of moderate to severe depression^[1][2][3]. In Vitro:Diclofensine (0.01-1 μM; 13 min) potently inhibits ³H-DA uptake in synaptosomes isolated from the arcuate nucleus-periventricular nucleus-median eminence of rats^[3].
Diclofensine (50 μM; 10 min) does not alter the basal endogenous dopamine release from tuberoinfundibular dopaminergic (TIDA) neurons in rats^[3].
Diclofensine (50 μM; 20 min) increases the K⁺-stimulated release of endogenous dopamine by 3-fold in rat tuberoinfundibular dopaminergic (TIDA) neurons^[3]. In Vivo:Diclofensine (10-50 mg/kg; p.o.; single administration) significantly reduces basal serum prolactin levels in rats^[3].