Naloxonazine dihydrochloride 是一种特异性的μ-opioid receptor拮抗剂，IC50为 5.4 nM。Naloxonazine dihydrochloride 也具有抗利什曼原虫活性。
| 生物活性 | Naloxonazine dihydrochloride is a specificμ-opioid receptorantagonist with anIC50of 5.4 nM. Naloxonazine dihydrochloride also shows anti-leishmanial activity[1][2][3]. |
| IC50& Target | μ Opioid Receptor/MOR 5.4 nM (IC50) |
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体外研究
(In Vitro) | Naloxonazine is relatively stable in solution[2].
Naloxonazine (72 h) is active against the intracellular amastigote stage ofLeishmania donovaniwith a half maximal inhibitory concentration (GI50) of 3.45 μM[3].
Naloxonazine (10 μM; 0-72 h) is active at early stages ofLeishmania donovaniinfection[3].
Naloxonazine affects acidic compartments of the host cell which in turn limitL. donovaniintracellular growth[3].
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体内研究
(In Vivo) | Naloxonazine (20 mg/kg; i.p.; once) attenuates the increment of locomotor activity induced by acute methamphetamine in mice[1]
| Animal Model: | Male ICR mice, methamphetamine (METH)-induced locomotor activity model[1] | | Dosage: | 20 mg/kg | | Administration: | Intraperitoneal injection, once, 60 min before injecting saline (i.p.) or METH (1 mg/kg, i.p.) | | Result: | Significantly attenuated the acute METH-induced increase in locomotor activity and phosphor-Thr75 DARPP-32 levels. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
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