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Loxapine Succinate is a D2DR and D4DR inhibitor, serotonergic receptor antagonist and also a dibenzoxazepine anti-psychotic agent [1].

In vitro: Loxapine was a typical neuroleptic that showed great structural and functional homology to the atypical antipsychotic clozapine. Chronic loxapine treatment was usually associated with extrapyramidal symptoms (EPS). Loxapineexihibited an extremely strong binding affinity fordopamineD4 andserotonin5-HT2receptors, suggesting that both serotonergic and dopaminergic mechanisms contributed to the antipsychotic drug action and EPS associated with loxapine in the treatment of schizophrenia [1]. In frontal cortex of brain in human and bovine, in the presence of Loxapine, [3H]ketanserin bound to 5-HT2 receptor with ki value of 6.2 nM and 6.6 nM, respectively. In comparing competition experiments involving the human membranes, loxapine exihibited the rank order of potency for the various receptors as follows: 5-HT2≥D4>>>D1>D2 [1]. Loxapine administration at 0.2, 2 and 20 μMafter 1 and 3 days of exposure reduced IL-1βand IL-2 secretion by LPS-activated mixed glia cultures. Loxapine also decreased IL-1βand IL-2 secretion in LPS-induced microglia cultures [2].

In vivo: Chronic administration of loxapine(5 mg/kg) in rats for 4 weeks or 10 weeks significantly reduced more than 50% of serotonin (S2) receptor density. Loxapine (5 mg/kg) didn’t change dopamine receptor density but greatly reduced serotonin receptor density by 47% in the brain of rats [3].

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