Naloxonazine (dihydrochloride)

MCE 国际站：Naloxonazine (dihydrochloride)

CAS：880759-65-9

品牌：MedChemExpress (MCE)

存储条件：Please store the product under the recommended conditions in the Certificate of Analysis.

生物活性：Naloxonazine dihydrochloride 是一种特异性 μ-opioid receptor 拮抗剂，IC₅₀ 为 5.4 nM。 Naloxonazine dihydrochloride 还具有抗利什曼原虫活性^[1][2][3]。

体外：Naloxonazine 在溶液中相对稳定^[2]。Naloxonazine (72 h) 对 Leishmania donovani 细胞内无鞭毛体阶段有活性，半数最大抑制浓度 ( GI₅₀) 为 3.45 μM^[3]。纳洛嗪（10 μM；0-72 小时）在杜氏利什曼原虫<的早期阶段具有活性/i> 感染^[3]。纳洛嗪影响宿主细胞的酸性区室，进而限制L。 donovani 细胞内生长^[3]。

体内：Naloxonazine（20 mg/kg；ip；一次）减弱小鼠急性甲基苯丙胺诱导的运动活动增加^[1]

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研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：Opioid Receptor

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参考文献：[1]. Chien CC, et al. Naloxonazine, a specific mu-opioid receptor antagonist, attenuates the increment of locomotor activity induced by acute methamphetamine in mice. Toxicol Lett. 2012 Jul 7;212(1):61-5.

[2]. Hahn EF, et al. Naloxonazine, a potent, long-lasting inhibitor of opiate binding sites. Life Sci. 1982 Sep 20-27;31(12-13):1385-8.

[3]. De Muylder G, et al. Naloxonazine, an Amastigote-Specific Compound, Affects Leishmania Parasites through Modulation of Host-Encoded Functions. PLoS Negl Trop Dis. 2016 Dec 30;10(12):e0005234.