Formulation: A solid
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
Purity: ≥98%
Formula Markup: C38H42N4O6 • 2HCl
Formula Weight: 723,7
Shelf life (days): 1460
CAS Number: 880759-65-9
Notes: Naloxonazine is a μ-opioid receptor antagonist (Ki = 0.054 nM in a radioligand binding assay).{25533} 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).{25533,67381} Naloxonazine (0.16 mg/kg) reverses sufentanil-induced antinociception, as well as hypercapnia and hypoxia, markers of respiratory depression, in rats.{67382} It reduces ethanol self-administration and food intake in rats when administered at a dose of 10 mg/kg.{67383} Naloxonazine (20 mg/kg) inhibits cocaine-induced place preference in rats.{67384}
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