| Bioactivity | Naloxonazine is a potent and selective opiate mu-1 antagonist that can also affect leishmania by regulating host coding function[1]. |
| Invitro | Naloxonazine(0-50 μM, 24-72 h) 对细胞内 Leishmania donovani 的无鞭毛体阶段具有抑制活性，其最大抑制浓度 GI50为3.45 μM。而对 THP-1 宿主细胞的 GI50为 34 μM[1]。Naloxonazine(10 μM, 4-72 h)可以抑制寄生虫细胞内生长，处理 24 h 可以抑制 70%，处理 72 h可以抑制 95%[1]。Naloxonazine(10 μM, 4 or 24-72 h)导致 vATPase亚基 (ATP6V0C和TCIRG1) 和肌动蛋白 (ACTB) 基因及蛋白表达水平上调，并且影响了宿主细胞的细胞内酸性区室[1]。 |
| In Vivo | Naloxonazine (0-15 mg/kg, i.p., 20 h)在雄性 Wistar大鼠中，当剂量为 15 mg/kg 时，(olfactory discriminative stimulus)S+/CS+ 相关反应显著降低约 55%，由 14.63 降至 6.82。而在(olfactory stimulus)S-/CS-刺激条件下观察到更大的行为抑制，反应率降低 66%，从 9.00 降至 3.00[2]。 |
| Name | Naloxonazine |
| CAS | 82824-01-9 |
| Formula | C38H42N4O6 |
| Molar Mass | 650.76 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Géraldine De Muylder, 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. [2]. Roberto Ciccocioppo, et al. Effect of selective blockade of mu(1) or delta opioid receptors on reinstatement of alcohol-seeking behavior by drug-associated stimuli in rats. Neuropsychopharmacology. 2002 Sep;27(3):391-9. |
Naloxonazine
CAS: 82824-01-9 F: C38H42N4O6 W: 650.76
Naloxonazine is a potent and selective opiate mu-1 antagonist that can also affect leishmania by regulating host coding
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