Naltrexone HCl

Alias: Naltrexone, EN-1639A, EN 1639A, EN1639A; Revia, Depade, Vivitrol, Celupan
Cat No.:V3777 Purity: ≥98%
Naltrexone HCl is a potentopioid receptor antagonist used mainly in the management of alcohol dependence and opioid dependence.
Naltrexone HCl Chemical Structure CAS No.: 16676-29-2
Product category: Opioid Receptor
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
100mg
250mg
500mg
1g
2g
Other Sizes

Other Forms of Naltrexone HCl:

  • Naltrexone
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Naltrexone HCl is a potent opioid receptor antagonist used mainly in the management of alcohol dependence and opioid dependence. Naltrexone is a drug that reverses the effects of opioids and should not be confused with naloxone or nalorphine, which are used in emergency cases of opioid overdose. Opioid receptor is a group of G protein-coupled receptors with opioids as ligands (e.g. proenkephalin, prodynorphin, pronociceptin etc, functioning in regulating pain perception, hormonal secretion and affecting temperature control etc.

Biological Activity I Assay Protocols (From Reference)
ln Vitro

In vitro activity: Naltrexone (0.32 mg/kg) reduces ethanol-reinforced responding at the concentration that maintained the most responding (1% or 2%) in rhesus monkeys. Naltrexone (0.1 mg/kg) reduces ethanol-reinforced responding, both at a low ethanol concentration (0.25%) that produced little ethanol intake (g/kg), and at a higher concentration (4%) with an appreciable intake. Naltrexone (1-3 mg/kg) potently and dose-dependently inhibits reinstatement of ethanol-seeking produced by non-contingent deliveries of the liquid dipper filled with 8% ethanol. Naltrexone elicits optimal enhancement of morphines antinociceptive potency in mice when co-administered (i.p.) at about 100 ng/kg together with morphine (3 mg/kg). Naltrexone (10 ng/kg i.p.) augments the antinociception produced by an acute submaximal dose of intrathecal (5 mg) or systemic (7.5 mg/kg i.p.) morphine in the tail-flick test in rats. Naltrexone combined with Morphine inhibits the decline in morphine antinociception and prevented the loss of morphine potency in rats. Naltrexone significantly suppresses ethanol self-administration and prevents ethanol-induced increases in dialysate dopamine levels. Naltrexone completely prevents the reduction in anogenital distance in prenatally stressed (PS) males and restores the growth rate of both sexes. Naltrexone also decreases the anxiety of PS rats in the plus-maze, increases the opioid component of exploration to control levels, but increases anxiety in control males


Kinase Assay:


Cell Assay:

ln Vivo
In adult male Sprague-Dawley rats, ultra-low doses of naltrexone (16.7, 20.0, and 25.0 ng/kg) with morphine (1mg/kg) extended the duration of the morphine-induced conditioned place preference. In male Wistar rats, naltrexone significantly inhibited ethanol self-adminnistration and prevented ethanol-activated increases in dialysate dopamine amount. Subchronic treatment with naltrexone caused progressive decrease of ethanol self-administration. Single doses of naltrexone increased extinction and attenuated cue-induced reinstatement of ethanol-reinforced behavior. In rhesus monkeys, naltrexone lowered behavior kept non-selectively by either ethanol or sucrose.
Animal Protocol
16.7, 20.0, and 25.0 ng/kg
Male Sprague-Dawley rats,
References
:Psychopharmacology (Berl).1998 Sep;139(1-2):53-61;Eur J Pharmacol.1999 Jun 25;374(3):321-7.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C20H23NO4.HCL
Molecular Weight
377.86
CAS #
16676-29-2
Related CAS #
16590-41-3 (free);16676-29-2 (HCl);
SMILES
Cl[H].O1C2=C(C([H])=C([H])C3C([H])([H])[C@]4([H])[C@@]5(C([H])([H])C([H])([H])C([C@@]1([H])[C@@]5(C=32)C([H])([H])C([H])([H])N4C([H])([H])C1([H])C([H])([H])C1([H])[H])=O)O[H])O[H]
Synonyms
Naltrexone, EN-1639A, EN 1639A, EN1639A; Revia, Depade, Vivitrol, Celupan
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 14 mg/mL (37.1mM)
Water:14 mg/mL (37.1mM)
Ethanol:<1 mg/mL
Solubility (In Vivo)
C1CC1CN2CC[C@]34[C@@H]5C(=O)CC[C@]3([C@H]2CC6=C4C(=C(C=C6)O)O5)O
 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.6465 mL 13.2324 mL 26.4648 mL
5 mM 0.5293 mL 2.6465 mL 5.2930 mL
10 mM 0.2646 mL 1.3232 mL 2.6465 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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