Amoxapine, a tricyclic dibenzoxazepine antidepressant, inhibits GLYT2a transport activity with IC50 of 92 μM.
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Amoxapine is a tricyclic antidepressant that inhibits norepinephrine and serotonin transport by binding to respective receptors with KD values of 16 and 58 nM, respectively[3]. Amoxapine also showed a selective inhibitory effect on glycine transporter 2a (GlyT2a) transport with an IC50 value of 92 ± 8 μM[4]. In mice bearing CT-26 cells, oral administration of amoxapine twice per day for 12 days successfully delayed or suppressed CPT-11-induced diarrhea and suppressed tumor growth at a dose of 1 or 5 mg/kg/day[5].
作用机制
Amoxapine is a tricyclic antidepressant that selectively inhibits GlyT2a. It also acts as a competitive inhibitor for both glycine and chloride[4].
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