| Bioactivity | Naloxonazine dihydrochloride is a specific μ-opioid receptor antagonist with an IC50 of 5.4 nM. Naloxonazine dihydrochloride also shows anti-leishmanial activity[1][2][3]. |
| Invitro | Naloxonazine is relatively stable in solution[2].Naloxonazine (72 h) is active against the intracellular amastigote stage of Leishmania donovani with a half maximal inhibitory concentration (GI50) of 3.45 μM[3].Naloxonazine (10 μM; 0-72 h) is active at early stages of Leishmania donovani infection[3].Naloxonazine affects acidic compartments of the host cell which in turn limit L. donovani intracellular growth[3]. |
| In Vivo | Naloxonazine (20 mg/kg; i.p.; once) attenuates the increment of locomotor activity induced by acute methamphetamine in mice[1] Animal Model: |
| Name | Naloxonazine dihydrochloride |
| CAS | 880759-65-9 |
| Formula | C38H44Cl2N4O6 |
| Molar Mass | 723.69 |
| Appearance | Solid |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| Reference | [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. |