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Loxapine succinate

CAS No. : 27833-64-3

MCE 国际站：Loxapine succinate

产品活性：Loxapine succinate 是一种具有口服活性的多巴胺（dopamine） 抑制剂和 5-HT 受体拮抗剂，有抗精神病活性。Loxapine 还能抑制细菌外排泵的活性，抑制巨噬细胞内多重耐药肠道鼠伤寒沙门氏菌。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：5-HT Receptor  |  Dopamine Receptor

In Vitro: In the presence of Loxapine, [³H]ketanserin binds to 5-HT₂ receptor in Frontal cortex of brain in human and bovine with K_i value of 6.2 nM and 6.6 nM, respectively. Loxapine has the rank order of potency for the various receptors appears to be as follows: 5-HT₂≥D₄>>>D₁>D₂ in comparing competition experiments involving the human membranes.
Loxapine (0-20 μM, 24 h or 72 h) reduces IL-1β secretion by LPS-activated mixed glia cultures, reduces IL-2 secretion in mixed glia cultures, and decreases IL-1β and IL-2 secretion in LPS-induced microglia cultures.
Loxapine (4 μM, 24 h) is active against multiple-antibiotic-resistant or Fluoroquinolone-resistant S. Typhimurium.
Loxapine (1, 2, 4 and 8 μM) suppresses intracellular Methicillin-resistant S. aureus (MRSA), Y. enterocolitica and S. flexneri in RAW264.7.

In Vivo: Loxapine (5 mg/kg; i.p.; daily for 4 or 10 weeks) decreases serotonin (S₂) but does not elevate dopamine (D2) receptor numbers in the rat brain.

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