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Naloxonazine dihydrochloride 

Cat. No. M30799
Naloxonazine dihydrochloride  Structure
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Biological Activity

Naloxonazine dihydrochloride is a specific μ-opioid receptor antagonist with an IC50 of 5.4 nM. Naloxonazine dihydrochloride also shows anti-leishmanial activity.

Chemical Information
Molecular Weight 723.69
Formula C38H44Cl2N4O6
CAS Number 880759-65-9
Form Solid
Storage 4°C, dry, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Shaul Schreiber, et al. Cell Mol Neurobiol. The Opioid Interactions of the Antipsychotic Medications Risperidone and Amisulpride in Mice and Their Potential Use in the Treatment of Other Non-Psychotic Medical Conditions

[2] Menghang Xia, et al. Cell Mol Neurobiol. Inhibition of morphine-induced cAMP overshoot: a cell-based assay model in a high-throughput format

[3] Nicolas Joly, et al. Rapid Commun Mass Spectrom. Structural determination of the novel fragmentation routes of zwitteronic morphine opiate antagonists naloxonazine and naloxone hydrochlorides using electrospray ionization tandem mass spectrometry

[4] G S Ling, et al. Science. Separation of morphine analgesia from physical dependence

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Keywords: Naloxonazine dihydrochloride  supplier, Opioid Receptor, inhibitors, activators


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