A μ- and κ-opioid receptor antagonist
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Nalmefene (hydrochloride)

Item No. 28266

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(5α)-17-(cyclopropylmethyl)-4,5-epoxy-6-methylene-morphinan-3,14-diol, monohydrochloride
CAS Number
58895-64-0
Synonyms
  • NIH 10365
Molecular Formula
C21H25NO3 • HCl
Formula Weight
375.9
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: Slightly Soluble: 0.1-1 mg/mlDMSO: Soluble: ≥10 mg/mlWater: Slightly Soluble: 0.1-1 mg/ml
SMILES
O[C@]12[C@]3(CCN(CC4CC4)[C@@H]2C5)[C@](OC6=C3C5=CC=C6O)([H])C(CC1)=C.Cl
InChi Code
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
InChi Key
GYWMRGWFQPSQLK-OPHZJPRHSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    10 mg

    $28

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    25 mg

    $65

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    50 mg

    $97

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    100 mg

    $138

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    Product Description

    Nalmefene is an antagonist of μ- and κ-opioid receptors (Kis = 0.91 and 1.03 nM, respectively, in CHO membranes expressing the human receptors).1 It is selective for μ- and κ-opioid receptors over δ-opioid receptors (Ki = 13.26 nM in CHO membranes expressing the human receptors). Nalmefene decreases self-administration of alcohol in non-alcohol- and alcohol-dependent rats.2 It reduces food and water intake and body weight in obese and lean rats when administered at a dose of 25 mg/kg per day.3 Nalmefene (32 mg/kg) inhibits morphine-induced scratching behavior and increases in the latency to tail withdrawal in a warm water tail withdrawal assay in rhesus monkeys.4 Formulations containing nalmefene have been used in the treatment of opioid overdose.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Ghirmai, S., Azar, M.R., Polgar, W.E., et al. Synthesis and biological evaluation of α- and β-6-amido derivatives of 17-cyclopropylmethyl-3, 14β-dihydroxy-4, 5α-epoxymorphinan: Potential alcohol-cessation agents. J. Med. Chem. 51(6), 1913-1924 (2008).

    2. Walker, B.M., and Koob, G.F. Pharmacological evidence for a motivational role of κ-opioid systems in ethanol dependence. Neuropsychopharmacology 33(3), 643-652 (2008).

    3. McLaughlin, C.L., and Baile, C.A. Nalmefene decreases meal size, food and water intake and weight gain in Zucker rats. Pharmacol. Biochem. Behav. 19(2), 235-240 (1983).

    4. Ko, M.C., and Naughton, N.N. An experimental itch model in monkeys: Characterization of intrathecal morphine-induced scratching and antinociception. Anesthesiology 92(3), 795-805 (2000).