Naloxone hydrochloride is an opioid inverse agonist compound used to counter the effects of opiate overdose.
|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.|
|Incubation time||24 h|
|Animal models||adult male C57BL/6J-Bom mice|
|Dosages||0.01, 0.1, or 1 mg/kg|
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
|Solubility||DMSO 60 mg/mL|
|Source||J Pharmacol Exp Ther (2016). Figure 2. Naloxone hydrochloride|
|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|
|Source||J Pharmacol Exp Ther (2016). Figure 1. Naloxone hydrochloride|
|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|
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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