Naloxonazine (hydrochloride)

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