Naloxonazine 

Naloxonazine is a potent and selective opiate mu-1 antagonist that can also affect leishmania by regulating host coding function^[1].

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^[1].
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^[1].
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^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

650.76

C₃₈H₄₂N₄O₆

82824-01-9

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• [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.   [Content Brief]

  [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.   [Content Brief]