Naltriben (mesylate)

Naltriben is an inverse agonist of delta2-opioid receptors (Ki = 0.013 nM in CHO-DG44 cells expressing the mouse receptor). It is selective for delta2-opioid receptors over kappa- and µ-opioid receptors (Kis = 13 and 12 nM in PC12 and COS-7 cells expressing the mouse and rat receptors, respectively). Naltriben (1 and 10 µM) induces axonal retraction in primary mouse hippocampal neurons under both normoxic and hypoxic conditions. It is also an activator of transient receptor potential melastatin 7 (TRPM7) and induces calcium influx in HEK293 cells expressing mouse TRPM7 (EC50 = 20.7 µM). It reduces self-administration of alcohol or alcohol mixed with saccharin or quinine in alcohol-preferring rats when administered at a dose of 6 mg/kg.Formal Name: (4bS,8R,8aS,14bR)-7-(cyclopropylmethyl)-5,6,7,8,9,14b-hexahydro-4,8-methano-8aH-bisbenzofuro[3,2-e:2',3'-g]isoquinoline-1,8a-diol, methanesulfonate. CAS Number: 122517-78-6. Synonyms: NIH 10924, NTB. Molecular Formula: C26H25NO4 . CH3SO3H. Formula Weight: 511.6. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMSO: Soluble. SMILES: O[C@@]12[C@@]([C@](O3)([H])C(OC4=CC=CC=C54)=C5C2)(CC6)C(C3=C7O)=C(C=C7)C[C@@]1([H])N6CC8CC8.C[S](=O)(O)=O. InChi Code: InChI=1S/C26H25NO4.CH4O3S/c28-18-8-7-15-11-20-26(29)12-17-16-3-1-2-4-19(16)30-22(17)24-25(26,21(15)23(18)31-24)9-10-27(20)13-14-5-6-14,1-5(2,3)4/h1-4,7-8,14,20,24,28-29H,5-6,9-13H2,1H3,(H,2,3,4)/t20-,24+,25+,26-,/m1./s1. InChi Key: XRRFZOCDAWPIBB-IDRHMUJXSA-N.