Dezocine

Dezocine is a partial agonist of the µ- and kappa-opioid receptors. It is selective for µ- and kappa-opioid receptors (Kis = 1.46 and 22.01 nM, respectively) over the delta-opioid receptor (Ki = 398.6 nM). Dezocine inhibits the norepinephrine transporter (NET) and serotonin transporter (SERT) with Ki values of 0.001 and 109 nM, respectively. It stimulates [35S]GTPgammaS binding to CHO membranes expressing the human µ- and kappa-opioid receptors with Emax values of 45.8 and 33.6% compared to the µ- and kappa-agonists DAMGO and U50,488 H, respectively, when used at a concentration of 10 µM. It has antinociceptive effects in mice in the acetic acid abdominal constriction test (ED50 = 0.02 mg/kg) and the formalin test (ED50s = 0.4 mg/kg for both phases). Dezocine (10 mg/kg) increases the latency to tail withdrawal in the tail-flick test in rats. It also decreases the number of lung metastases in a 4T1 murine mammary cancer model when administered at doses ranging from 0.75 to 2 mg/kg. Formulations containing dezocine have been used in the treatment of post-operative pain.Formal Name: (5R,11S,13S)-amino-5,6,7,8,9,10,11,12-octahydro-5-methyl-5,11-methanobenzocyclodecen-3-ol. CAS Number: 53648-55-8. Synonyms: Wy 16225. Molecular Formula: C16H23NO. Formula Weight: 245.4. Purity: >95%. Formulation: (Request formulation change), A solid. Solubility: DMSO: slightly soluble, Methanol: slightly soluble. SMILES: C[C@@]12C3=CC(O)=CC=C3C[C@H](CCCCC2)[C@@H]1N. InChi Code: InChI=1S/C16H23NO/c1-16-8-4-2-3-5-12(15(16)17)9-11-6-7-13(18)10-14(11)16/h6-7,10,12,15,18H,2-5,8-9,17H2,1H3/t12-,15-,16+/m0/s1. InChi Key: VTMVHDZWSFQSQP-VBNZEHGJSA-N.