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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
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
50mg
100mg
250mg
500mg
1g
2g
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Other Forms of Naltrexone HCl:

  • Naltrexone
Official Supplier of:
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Top Publications Citing lnvivochem Products
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,
Toxicity/Toxicokinetics
Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation
Limited data indicate that naltrexone is minimally excreted into breastmilk. If the mother requires naltrexone, it is not a reason to discontinue breastfeeding.
◉ Effects in Breastfed Infants
A 1.5-month-old breastfed infant of a mother who was taking 50 mg of oral naltrexone daily during pregnancy and lactation was reportedly healthy with no naltrexone-related adverse effects.
◉ Effects on Lactation and Breastmilk
Relevant published information was not found as of the revision date.
References
:Psychopharmacology (Berl).1998 Sep;139(1-2):53-61;Eur J Pharmacol.1999 Jun 25;374(3):321-7.
Additional Infomation
Naltrexone hydrochloride is a hydrochloride obtained by reaction of oxycodone with one molar equivalent of hydrochloric acid. it is a mu-opioid receptor antagonist that is used to treat alcohol dependence. It has a role as a mu-opioid receptor antagonist, an antidote to opioid poisoning and a central nervous system depressant. It contains a naltrexone(1+).
Naltrexone Hydrochloride is the hydrochloride salt of naltrexone, a noroxymorphone derivative with competitive opioid antagonistic activity. Naltrexone and its metabolite 6-beta-naltrexol reverse the effects of opioids by binding to various opioid receptors in the central nervous system CNS), including the mu-, kappa- and gamma-opioid receptors; opioid effects of analgesia, euphoria, sedation, respiratory depression, miosis, bradycardia, and physical dependence are inhibited. Naltrexone is longer-acting and more potent compared to naloxone.
Derivative of noroxymorphone that is the N-cyclopropylmethyl congener of NALOXONE. It is a narcotic antagonist that is effective orally, longer lasting and more potent than naloxone, and has been proposed for the treatment of heroin addiction. The FDA has approved naltrexone for the treatment of alcohol dependence.
See also: Naltrexone (has active moiety); Morphine Sulfate; Naltrexone Hydrochloride (component of); Bupropion Hydrochloride; Naltrexone Hydrochloride (component of) ... View More ...
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C20H23NO4.HCL
Molecular Weight
377.86
Exact Mass
377.139
CAS #
16676-29-2
Related CAS #
16590-41-3 (free);16676-29-2 (HCl);
PubChem CID
5485201
Appearance
Typically exists as solid at room temperature
Density
1.47 g/cm3
Boiling Point
558.1ºC at 760 mmHg
Melting Point
274-2760C
Flash Point
291.4ºC
Vapour Pressure
2.71E-13mmHg at 25°C
LogP
2.265
Hydrogen Bond Donor Count
3
Hydrogen Bond Acceptor Count
5
Rotatable Bond Count
2
Heavy Atom Count
26
Complexity
621
Defined Atom Stereocenter Count
4
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]
InChi Key
RHBRMCOKKKZVRY-ITLPAZOVSA-N
InChi Code
InChI=1S/C20H23NO4.ClH/c22-13-4-3-12-9-15-20(24)6-5-14(23)18-19(20,16(12)17(13)25-18)7-8-21(15)10-11-1-2-11;/h3-4,11,15,18,22,24H,1-2,5-10H2;1H/t15-,18+,19+,20-;/m1./s1
Chemical Name
(4R,4aS,7aR,12bS)-3-(cyclopropylmethyl)-4a,9-dihydroxy-2,4,5,6,7a,13-hexahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinolin-7-one;hydrochloride
Synonyms
Naltrexone, EN-1639A, EN 1639A, EN1639A; Revia, Depade, Vivitrol, Celupan
HS Tariff Code
2934.99.9001
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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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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Calculation results

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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Clinical Trial Information
Optimizing Retention, Duration and Discontinuation Strategies for Opioid Use Disorder Pharmacotherapy (RDD)
CTID: NCT04464980
Phase: Phase 2    Status: Recruiting
Date: 2024-11-05
Study of PF614 Compared to OxyContin® in Healthy Volunteers (PF614-101)
CTID: NCT02454712
Phase: Phase 1    Status: Completed
Date: 2024-10-02
Pharmacokinetics of Oxycodone and PF614 Co-Administered with Nafamostat (PF614-MPAR-101)
CTID: NCT05090280
Phase: Phase 1    Status: Completed
Date: 2024-09-24
Evaluation of Oral PF614 Relative to OxyContin (PF614-102)
CTID: NCT05043766
Phase: Phase 1    Status: Completed
Date: 2024-09-24
Extended Release Naltrexone Versus Extended Release Buprenorphine with Individuals Leaving Jail
CTID: NCT04408313
Phase: Phase 2/Phase 3    Status: Recruiting
Date: 2024-09-19
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Naltrexone Treatment for Prolonged Grief Disorder (PGD)
CTID: NCT04547985
Phase: Phase 4    Status: Terminated
Date: 2024-08-28


Long-acting Buprenorphine vs. Naltrexone Opioid Treatments in CJS-involved Adults
CTID: NCT04219540
Phase: Phase 4    Status: Recruiting
Date: 2024-06-21
Oral Naltrexone In Pediatric Eating Disorders
CTID: NCT05073679
Phase: Phase 2/Phase 3    Status: Terminated
Date: 2024-06-10
Low Dose Naltrexone to Improve Physical Health in Patients With Vasculitis
CTID: NCT03482479
Phase: Phase 2    Status: Recruiting
Date: 2024-05-21
Under
Naltrexone Enhanced Addiction Treatment (NEAT): A randomised controlled trial of the clinical and cost-effectiveness of extended-release naltrexone and oral naltrexone.
CTID: null
Phase: Phase 3    Status: Prematurely Ended
Date: 2014-11-06
A multi-center, randomized, double-blind, placebo-controlled study to evaluate the efficacy and safety of certolizumab pegol in combination with methotrexate for inducing and sustaining clinical response in the treatment of dmard-naïve adults with early active rheumatoid arthritis.
CTID: null
Phase: Phase 3    Status: Completed
Date: 2012-03-05
Mejora de la efectividad de los tratamientos de mantenimiento con naltrexona en adictos a opiáceos con la adicción de buprenorfina sublingual. Improvement of naltrexone maintenance treatment effectivity in opiate addict patients adding buprenorphine.
CTID: null
Phase: Phase 4    Status: Ongoing
Date: 2009-08-12
An open-label, prospective, multicentric pilot study evaluating safety and symptomatics effects of low dose Naltrexone in patients with primary progressive multiple sclerosis.
CTID: null
Phase: Phase 2    Status: Ongoing
Date: 2006-06-28
Effect of Naltrexone on cue-induced craving for Amphetamine in amphetamine dependent individuals
CTID: null
Phase: Phase 2    Status: Completed
Date: 2006-06-07
Metotreksaatti aksiaalisen spondyloartropatian hoidossa
CTID: null
Phase: Phase 4    Status: Ongoing
Date: 2005-05-26

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