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| | Naltrexone hydrochloride Basic information |
| Product Name: | Naltrexone hydrochloride | | Synonyms: | N-CYCLOPROPYLMETHYL-14-HYDROXYDI-HYDROMORPHINONE HYDROCHLORIDE;NALTREXONE HYDROCHLORIDE;(5alpha)-17-(cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxymorphinan-6-one hydrochloride;(5A)-17-(CYCLOPROPYLMETHYL)-4,5-EPOXY-3,14-DIHYDROMORPHINAN-6-ONE HYDROCHLORIDE;17-(cyclopropylmethyl)-4,5-alpha-epoxy-3,14-dihydroxy-morphinan-6-onehydroch;17-(cyclopropylmethyl)-4,5-alpha-epoxy-3,14-dihydroxy-morphinan-6-onhydr;17-(cyclopropylmethyl)-4,5-alpha-oxy-3,14-dihydoxy-morphinan-6-onhydrochlo;17-(cyclopropylmethyl)-4,5-epoxy-3,14-dihydroxy-morphinan-6-onhydrochlor | | CAS: | 16676-29-2 | | MF: | C20H24ClNO4 | | MW: | 377.87 | | EINECS: | 240-723-0 | | Product Categories: | Chiral Reagents;Intermediates & Fine Chemicals;Pharmaceuticals;Antagonists;Opioids;Pharmacologicals;Enzyme Inhibitors;Enzyme Inhibitors by Type;Other;Opioid receptor and opioid-like receptor | | Mol File: | 16676-29-2.mol |  |
| | Naltrexone hydrochloride Chemical Properties |
| Melting point | 274-2760C | | storage temp. | 2-8°C | | solubility | H2O: 50 mg/mL, clear, colorless | | form | neat | | color | White to Off-White | | Water Solubility | Soluble in water at 50mg/ml. | | Sensitive | Light Sensitive | | Merck | 13,6389 | | BRN | 3580333 | | CAS DataBase Reference | 16676-29-2(CAS DataBase Reference) |
| Hazard Codes | Xn | | Risk Statements | 22 | | Safety Statements | 22-36 | | WGK Germany | 3 | | RTECS | QD2160000 | | F | 8-10 | | HS Code | 2932.99.7000 | | Toxicity | guinea pig,LD50,oral,1490mg/kg (1490mg/kg),Medicamentos de Actualidad. Vol. 21, Pg. 264, 1985. |
| | Naltrexone hydrochloride Usage And Synthesis |
| Description | Naltrexone hydrochloride is a potent, long-acting, orally-effective narcotic
antagonist useful in the management of narcotic addiction. | | Chemical Properties | White Crystalline Powder | | Originator | Endo (USA) | | Uses | Nonselective opioid receptor antagonist; congener of naloxone | | Uses | Naltrexone hydrochloride has been used:
as an opioid antagonist, to analyse its effect on ethanol preference using Caenorhabditis elegans as a model.
to determine its effectiveness in reducing the preference for substance of abuse (SOA) like nicotine and cocaine using Caenorhabditis elegans as a model.
in the preparation of combinatorial drug, PXT3003 for treating Charcot-Marie-Tooth disease 1A (CMT1A) transgenic rat model Pmp22. | | Uses | sulfonamide, carbonic anhydrase inhibitor, anti-glaucoma agent | | Uses | Narcotic antagonist, In treatment of?alcoholism | | Definition | ChEBI: 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+). | | Brand name | TREXAN | | Biological Activity | Opioid antagonist. | | Biochem/physiol Actions | Competitive antagonist for μ, κ, δ, and σ-opioid receptors; has greater oral efficacy and longer duration of action than naloxone. | | Clinical Use | Opioid antagonist:
Adjunctive prophylactic treatment in patient’s
previously opioid dependant
Treatment of alcohol dependence | | Drug interactions | Potentially hazardous interactions with other drugs
Opioids: Avoid concomitant use. | | Metabolism | Naltrexone is well absorbed from the gastrointestinal
tract but is subject to considerable first-pass metabolism
and may undergo enterohepatic recycling. It is extensively
metabolised in the liver and the major metabolite,
6-β-naltrexol, may also possess weak opioid antagonist
activity.
It is excreted mainly in the urine, <5% is excreted in the
faeces.
The renal clearance for naltrexone ranges from 30-127
mL/min and suggests that renal elimination is primarily
by glomerular filtration | | storage | Room temperature | | Purification Methods | This narcotic antagonist has been purified by recrystallisation from MeOH and dried in air. The free base has m 168-170o after recrystallisation from Me2CO. [Cone et al. J Pharm Sci 64 618 1975, Gold et al. Med Res Rev 2 211 1982.] |
| | Naltrexone hydrochloride Preparation Products And Raw materials |
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