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Naloxonazine

CAS No. : 82824-01-9

MCE 站：Naloxonazine

产品活性：Naloxonazine 是一种有效的选择性阿片类 mu-1拮抗剂，同时也能够通过调节宿主编码功能影响利什曼原虫。

研究领域：GPCR/G Protein  |  Neuronal Signaling  |  Anti-infection

作用靶点：Opioid Receptor  |  Parasite

In Vitro: Naloxonazine(0-50 μM, 24-72 h) shows inhibitory activity against the astigmatic phase of Leishmania donovani, ａnd its maximum inhibitory concentration the GI₅₀ value is 3.45 μM. The GI₅₀ of THP-1 host cells is 34 μM.
Naloxonazine(10 μM, 4-72 h) inhibits the intracellular growth of the parasite by 70% after 24 h treatment ａnd 95% after 72 h treatment.
Naloxonazine(10 μM, 4 or 24-72 h) leads to upregulation of vATPase subunits (ATP6V0C ａnd TCIRG1) ａnd actin (ACTB) genes ａnd proteins, ａnd affects the intracellular acid compartment of host cells.

In Vivo: Naloxonazine (0-15 mg/kg, i.p., 20 h) results that (olfactory discriminative stimulus)S+/CS+ correlated responses are significantly reduced by about 55% at a dose of 15 mg/kg, from 14.63 to 6.82. However, greater behavioral inhibition is observed in the (olfactory stimulus)S/CS stimulus condition, with a 66% reduction in response rate from 9.00 to 3.00 in male Wistar rats.

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