Nalmefene hydrochlorideOpioid receptor antagonist CAS# 58895-64-0 |
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Quality Control & MSDS
Number of papers citing our products
Chemical structure
3D structure
| Cas No. | 58895-64-0 | SDF | Download SDF |
| PubChem ID | 5388881 | Appearance | Powder |
| Formula | C21H26ClNO3 | M.Wt | 375.89 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble to 100 mM in water and to 100 mM in DMSO | ||
| Chemical Name | (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 | ||
| SMILES | C=C1CCC2(C3CC4=C5C2(C1OC5=C(C=C4)O)CCN3CC6CC6)O.Cl | ||
| Standard InChIKey | GYWMRGWFQPSQLK-OPHZJPRHSA-N | ||
| Standard InChI | InChI=1S/C21H25NO3.ClH/c1-12-6-7-21(24)16-10-14-4-5-15(23)18-17(14)20(21,19(12)25-18)8-9-22(16)11-13-2-3-13;/h4-5,13,16,19,23-24H,1-3,6-11H2;1H/t16-,19+,20+,21-;/m1./s1 | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Opioid receptor antagonist; displays a longer half life than Naloxone. Exhibits neuroprotective effects after traumatic brain injury in the rat. Deuterated version, Nalmefene d3, also available. |
Nalmefene hydrochloride Dilution Calculator
Nalmefene hydrochloride Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.6604 mL | 13.3018 mL | 26.6035 mL | 53.2071 mL | 66.5088 mL |
| 5 mM | 0.5321 mL | 2.6604 mL | 5.3207 mL | 10.6414 mL | 13.3018 mL |
| 10 mM | 0.266 mL | 1.3302 mL | 2.6604 mL | 5.3207 mL | 6.6509 mL |
| 50 mM | 0.0532 mL | 0.266 mL | 0.5321 mL | 1.0641 mL | 1.3302 mL |
| 100 mM | 0.0266 mL | 0.133 mL | 0.266 mL | 0.5321 mL | 0.6651 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Stability of Revex, nalmefene hydrochloride injection.[Pubmed:8846056]
PDA J Pharm Sci Technol. 1996 Jan-Feb;50(1):35-9.
The stability of Revex, Nalmefene hydrochloride injection, has been studied at several temperatures for periods up to 36 months. The data were obtained using a HPLC method for the potency determination, and for the level of the sole degradation product (2,2'-bisnalmefene). These methods were found to be characterized by excellent precision, linearity, and accuracy over the analyte concentration ranges established. The stability data were found to be interpretable using first-order kinetics, and essentially comparable rate constants were calculated for both the potency loss and the formation of 2,2'-bisnalmefene. Applying the Arrhenius equation to these data, a rate constant of 0.00441 month-1 was deduced for the reactions taking place at 25 degrees C. This low value is consistent with the excellent stability exhibited by the product, and amply justifies its shelf life.
Stability of revex, nalmefene hydrochloride injection, in injectable solutions.[Pubmed:8933423]
J Pharm Biomed Anal. 1996 Nov;15(2):221-6.
The short-term stability of Revex, Nalmefene hydrochloride injection, was determined in a number of diluents commonly employed for intravenous use. An HPLC method was used to follow the potency of the diluted solutions, and was fully validated for its intended concentration range prior to its use. Dilutions of Revex were prepared separately in 0.9% sodium chloride injection, 0.45% sodium chloride injection, 5% dextrose injection, 5% dextrose and 0.45% sodium chloride injection, lactated Ringer's injection, 5% dextrose and lactated Ringer's injection and 5% sodium hydrogencarbonate injection. Each admixture was stored at 4 degrees C, room temperature (21 degrees C) and 40 degrees C, with samples being tested after storage at each temperature for 0, 24, 48 and 72 h. Defining stability as the retention of at least 95% of the initial drug concentration at the end of the storage period, it was concluded that the diluted solutions of Revex were uniformly stable for up to 72 h in all of the injectable solutions maintained at either 4, 21 or 40 degrees C.
The permeation of nalmefene hydrochloride across different regions of ovine nasal mucosa.[Pubmed:17139110]
Chem Pharm Bull (Tokyo). 2006 Dec;54(12):1722-4.
The permeability of Nalmefene hydrochloride (NH) across different regions of ovine nasal mucosa was investigated in vitro. Five different regions of ovine nasal mucosa (superior turbinate mucosa, middle turbinate mucosa, inferior turbinate mucosa, posterior septum mucosa, and anterior septum mucosa) were studied. The results showed that the permeability coefficients of NH through different regions of nasal mucosa were different, and the suitable regions for the absorption of NH were the middle turbinate mucosa, the posterior septum mucosa and the superior turbinate. At the same time, the middle turbinate mucosa was the largest region among the five regions, thus it was the main absorption region for NH. The high uniformity of the middle turbinate mucosa also made it the most suitable model for the permeation of NH in vitro.
Opiate antagonist nalmefene improves intracellular free Mg2+, bioenergetic state, and neurologic outcome following traumatic brain injury in rats.[Pubmed:2230942]
J Neurosci. 1990 Nov;10(11):3524-30.
Treatment of CNS trauma with the opiate antagonist naloxone improves outcome, though the mechanisms of action remain speculative. Nalmefene is another opiate-receptor antagonist, but it has substantially greater potency and duration of action than naloxone. It also has increased activity at kappa opiate receptors and has recently been shown to limit histological changes and neurological dysfunction after traumatic spinal cord injury. The present study examined the effects of treatment with nalmefene on outcome after fluid-percussion-induced traumatic brain injury in rats, using magnetic resonance spectroscopy to monitor acute metabolic changes and behavioral tests to determine chronic neurological recovery. Single-dose treatment with nalmefene (100 micrograms/kg, i.v.) at 30 min after trauma significantly improved (p less than 0.05) neurological outcome (up to 4 weeks) as compared to saline-treated controls. Early changes in intracellular free-magnesium concentration, adenosine diphosphate concentration, and cytosolic phosphorylation potential were all significantly improved by nalmefene treatment, reflecting improved bioenergetic state. We suggest that the ability of nalmefene to improve cellular bioenergetics after trauma may in part account for the neuroprotective effects of this and related compounds.
