Loxapine succinate | MedChemExpress (MCE)

Loxapine succinate | MedChemExpress (MCE)

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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 Ki 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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