A μ-opioid receptor antagonist
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Naloxonazine (hydrochloride)

Item No. 21950

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(5α)-[(5α)-4,5-epoxy-3,14-dihydroxy-17-(2-propenyl)morphinan-6-ylidene]hydrazone, 4,5-epoxy-3,14-dihydroxy-17-(2-propenyl)-morphinan-6-one, dihydrochloride
CAS Number
880759-65-9
Synonyms
  • NLXZ
Molecular Formula
C38H42N4O6 • 2HCl
Formula Weight
723.7
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
PBS (pH 7.2): Slightly soluble
SMILES
O[C@]12[C@]3(CCN(CC=C)[C@@H]2C4)[C@](OC5=C3C4=CC=C5O)([H])/C(CC1)=N/N=C(CC[C@@]6(O)[C@H]7CC8=CC=C9O)/[C@@]%10([H])[C@]6(CCN7CC=C)C8=C9O%10.Cl.Cl
InChi Code
InChI=1S/C38H42N4O6.2ClH/c1-3-15-41-17-13-35-29-21-5-7-25(43)31(29)47-33(35)23(9-11-37(35,45)27(41)19-21)39-40-24-10-12-38(46)28-20-22-6-8-26(44)32-30(22)36(38,34(24)48-32)14-18-42(28)16-4-2;;/h3-8,27-28,33-34,43-46H,1-2,9-20H2;2*1H/b39-23+,40-24+;;/t27-,28-,33+,34+,35+,36+,37-,38-;;/m1../s1
InChi Key
VIAIHLLKDJKEKM-DCBBKWFGSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    10 mg

    $81

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    25 mg

    $181

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    50 mg

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    Product Description

    Naloxonazine is a μ-opioid receptor antagonist (Ki = 0.054 nM in a radioligand binding assay).1 It is selective for μ-opioid over κ- and δ-opioid receptors (Kis = 11 and 8.6 nM, respectively, in radioligand binding assays) and selectively binds to high-affinity µ1-opioid over μ- and δ-opioid receptors (Kds = 0.1, 2, and 5 nM, respectively).1,2 Naloxonazine (0.16 mg/kg) reverses sufentanil-induced antinociception, as well as hypercapnia and hypoxia, markers of respiratory depression, in rats.3 It reduces ethanol self-administration and food intake in rats when administered at a dose of 10 mg/kg.4 Naloxonazine (20 mg/kg) inhibits cocaine-induced place preference in rats.5

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Raynor, K., Kong, H., Chen, Y., et al. Pharmacological characterization of the cloned κ-, δ-, and μ-opioid receptors. Mol. Pharm. 45(2), 330-334 (1994).

    2. Cruciani, R.A., Lutz, R.A., Munson, P.J., et al. Naloxonazine effects on the interaction of enkephalin analogs with mu-1, mu and delta opioid binding sites in rat brain membranes. J. Pharmacol. Exp. Ther. 242(1), 15-20 (1987).

    3. Verborgh, C., and Meert, T.F. Antagonistic effects of naloxone and naloxonazine on sufentanil-induced antinociception and respiratory depression in rats. Pain 83(1), 17-24 (1999).

    4. Mhatre, M., and Holloway, F. μ1-opioid antagonist naloxonazine alters ethanol discrimination and consumption. Alcohol 29(2), 109-116 (2003).

    5. Rademacher, D.J., and Steinpreis, R.E. Effects of the selective μ1-opioid receptor antagonist, naloxonazine, on cocaine-induced conditioned place preference and locomotor behavior in rats. Neurosci. Lett. 332(3), 159-162 (2002).