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Naloxone hydrochloride

Cat. No. M2876
Naloxone hydrochloride Structure
Size Price Availability Quantity
100mg USD 90 In stock
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Quality Control
Biological Activity

Naloxone hydrochloride is an opioid inverse agonist compound used to counter the effects of opiate overdose.

Protocol
Cell Experiment
Cell lines BV‐2 cells
Preparation method The phagocytic activity of BV‐2 cells was measured by Vybrant phagocytosis assay kit according to the manufacturer's instructions. Briefly, BV‐2 cells were treated with LPS (200 ng·mL−1) and (+)‐naltrexone/(+)‐naloxone for 24 h.
Concentrations 20 μM
Incubation time 24 h
Animal Experiment
Animal models adult male C57BL/6J-Bom mice
Formulation saline
Dosages 0.01, 0.1, or 1 mg/kg
Administration s.c.
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 363.84
Formula C19H21NO4.HCl
CAS Number 357-08-4
Purity >99%
Solubility DMSO 60 mg/mL
Storage at -20°C
Customer Product Validations & Biological Datas
Source J Pharmacol Exp Ther (2016). Figure 2. Naloxone hydrochloride
Method Pharmacokinetics
Cell Lines C57BL/6J-Bom mice
Concentrations 0.01, 0.1, 1, 10, or 50 mg/kg
Incubation Time 90 min
Results Mice administered a higher 50-mg/kg (1)-naloxone dose in combination with heroin demonstrated a clear reduction in locomotor activity (41% reduction in maximal distance run), as did mice given this dose of (1)-naloxone in combination with 6-AM
Rating
Source J Pharmacol Exp Ther (2016). Figure 1. Naloxone hydrochloride
Method Locomotor Activity
Cell Lines C57BL/6J-Bom mice
Concentrations 0.01, 0.1, or 1 mg/kg
Incubation Time 60 min
Results Thereafter, locomotor activity increased until approximately 90 minutes after morphine administration, displaying an almost 40% reduction of the maximal distance run (P,0.01), before it declined. The lowest dose of (2)-naloxone showed no effect on morphine-induced locomotor activity
Rating
References

Comparison of (+)- and (-)-Naloxone on the Acute Psychomotor-Stimulating Effects of Heroin, 6-Acetylmorphine, and Morphine in Mice.
Eriksen GS, et al. J Pharmacol Exp Ther. 2016 Aug;358(2):209-15. PMID: 27278234.

Pharmacological characterization of the opioid inactive isomers (+)-naltrexone and (+)-naloxone as antagonists of toll-like receptor 4.
Wang X, et al. Br J Pharmacol. 2016 Mar;173(5):856-69. PMID: 26603732.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Naloxone hydrochloride supplier, Opioid Receptor, inhibitors

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