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Naloxone hydrochloride is an opioid inverse agonist compound used to counter the effects of opiate overdose.
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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 |
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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 |
| 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. |
| Molecular Weight | 363.84 |
| Formula | C19H21NO4.HCl |
| CAS Number | 357-08-4 |
| Solubility (25°C) | DMSO 50 mg/mL Water 50 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Opioid Receptor Products |
|---|
| ADL5859 Hydrochloride
ADL5859 is a potent, selective and orally bioavailable δ-opioid receptor agonist (Ki = 0.84 nM, EC50 = 20 nM). |
| JTC-801
JTC-801 is a novel opioid receptor-like1 (ORL1) receptor antagonist with IC50 of 94 nM. |
| Meptazinol hydrochloride
Meptazinol is a unique centrally active opioid analgesic, which inhibits [3H]dihydromorphine binding with IC50 of 58 nM. |
| Nalmefene hydrochloride
Nalmefene is an opioid receptor antagonist, it is used primarily in the management of alcohol dependence. |
| 6-Alpha Naloxol
6-Alpha Naloxol |
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