Nalmefene hydrochloride
Nalmefene hydrochloride Basic information
- Product Name:
- Nalmefene hydrochloride
- Synonyms:
-
- Morphinan-3,14-diol, 17-(cyclopropylmethyl)-4,5-epoxy-6-methylene-, hydrochloride, (5alpha)-
- Revex
- Unii-K7K69qc05x
- (5α)-17-(Cyclopropylmethyl)-4,5-epoxy-6-methylenemorphinan-3,14-diolhydrochloride
- (5a)-17-(CyclopropylMethyl)-6-Methylene-4,5-epoxyMorphinan-3,14-diol
- Morphinan-3,14-diol,17-(cyclopropylMethyl)-4,5-epoxy-6-Methylene-, hydrochloride (1:1), (5a)-
- (4R,4aS,7aS,12bS)-3-(cyclopropylmethyl)-7-methylidene-2,4,5,6,7a,13-hexahydro-1H-4,12-methanobenzofuro[3,2-e]isoquinoline-4a,9-diol,hydrochloride
- Nalmefene Impurity 2
- CAS:
- 58895-64-0
- MF:
- C21H26ClNO3
- MW:
- 375.89
- EINECS:
- 232-572-4
- Product Categories:
-
- Inhibitors
- 58895-64-0
- Mol File:
- 58895-64-0.mol
Nalmefene hydrochloride Chemical Properties
- Melting point:
- 180-185°
- storage temp.
- Desiccate at RT
- solubility
- Soluble in Water (up to 25 mg/ml).
- form
- solid
- pka
- 7.63(at 25℃)
- color
- White
- Stability:
- Stable for 2 years from date of purchase as supplied. Solutions in distilled water may be stored at -20°C for up to 1 month.
- InChIKey
- GYWMRGWFQPSQLK-GGPQROQHNA-N
- SMILES
- O[C@]12CCC(=C)[C@]3([H])OC4C(=CC=C5C[C@@]1([H])N(CC1CC1)CC[C@@]23C=45)O.Cl |&1:1,6,15,24,r|
- CAS DataBase Reference
- 58895-64-0
Nalmefene hydrochloride Usage And Synthesis
Description
Nalmefene hydrochloride has been introduced in the U.S.A. for opioid reversal following surgery, and in the reversal of opioid overdoses and epidurally administered narcotics. Nalmefene is an opioid antagonist that inhibits respiratory, analgesic and subjective effects of opioids. It has a higher potency, a longer duration of action, and superior bioavailability than the structurally related naltrexone. Nalmefene has a wide spectrum of biological activity and is in clinical trials for the treatment of interstitial cystitis, recalcitrant pruritus of cholestasis, stroke, rheumatoid arthritis, shock, CNS trauma, and alcoholism. Studies indicate that nalmefene does not induce morphine-like effects and has no apparent abuse potential.
Originator
IVAX (U.S.A.)
Uses
Nalmefene Hydrochloride is a structural analog of Naltrexone (N285780) with opiate antagonist activity used in pharmaceutical treatment of alcoholism. Other pharmacological applications of this compound aim to reduce food cravings, drug abuse and pulmonary disease in affected individuals. Used as an opioid-induced tranquilizer on large animals in the veterinary industry. Narcotic antagonist
brand name
Revex
storage
Desiccate at RT
References
[1] MELISSA D. OSBORN . In vivo characterization of the opioid antagonist nalmefene in mice[J]. Life sciences, 2010, 86 15: Pages 624-630. DOI:10.1016/j.lfs.2010.02.013
[2] EDUARDO R BUTELMAN. Unconditioned behavioral effects of the powerful kappa-opioid hallucinogen salvinorin A in nonhuman primates: fast onset and entry into cerebrospinal fluid.[J]. Journal of Pharmacology and Experimental Therapeutics, 2009, 328 2: 588-597. DOI:10.1124/jpet.108.145342
[3] EDUARDO R BUTELMAN. The effects of herkinorin, the first mu-selective ligand from a salvinorin A-derived scaffold, in a neuroendocrine biomarker assay in nonhuman primates.[J]. Journal of Pharmacology and Experimental Therapeutics, 2008, 327 1: 154-160. DOI:10.1124/jpet.108.140079
[4] MICHAEL SOYKA Susanne R. Opioid antagonists for pharmacological treatment of alcohol dependence - a critical review.[J]. Current drug abuse reviews, 2008, 1 3: 280-291. DOI:10.2174/1874473710801030280
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