Cebranopadol

Cebranopadol is an agonist of nociceptin-, µ-, ?-, and delta-opioid receptors (Kis = 0.9, 0.7, 2.6, and 18 nM, respectively). It is greater than 100-fold selective for these receptors over a panel of more than 100 ion channels, neurotransmitter transporters, receptors, and enzymes, but does bind to the serotonin (5-HT) receptor subtype 5-HT5A with a Ki value of 8.7 nM. Cebranopadol inhibits nociceptin-, DAMGO-, and SNC 80-induced GTP?S binding in CHO cells expressing nociceptin-, µ-, and delta-opioid receptors, respectively (EC50s = 13, 1.2, and 110 nM, respectively), as well as U69,593-induced GTP?S binding in HEK293 cells expressing the ?-opioid receptor (EC50 = 17 nM). It increases the paw withdrawal threshold in rat models of bone cancer pain and streptozotocin-induced diabetic neuropathy (ED50s = 3.6 and 0.5 µg/kg, respectively, i.v.). Cebranopadol also increases paw weight bearing on the ipsilateral side in a rat model of arthritis induced by complete Freund's adjuvant (CFA) and M. tuberculosis (ED50 = 5.5 µg/kg, i.v.).Formal Name: (1alpha,4beta)-6'-fluoro-4',9'-dihydro-N,N-dimethyl-4-phenyl-spiro[cyclohexane-1,1'(3'H)-pyrano[3,4-b]indol]-4-amine. CAS Number: 863513-91-1. Synonyms: GRT6005. Molecular Formula: C24H27FN2O. Formula Weight: 378.5. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: DMF: 2mg/mL, DMSO: 0.2mg/mL. lambdamax: 225, 287 nm. SMILES: FC1=CC=C2C(C(CCO[C@]34CC[C@](C5=CC=CC=C5)(N(C)C)CC4)=C3N2)=C1. InChi Code: InChI=1S/C24H27FN2O/c1-27(2)23(17-6-4-3-5-7-17)11-13-24(14-12-23)22-19(10-15-28-24)20-16-18(25)8-9-21(20)26-22/h3-9,16,26H,10-15H2,1-2H3/t23-,24-. InChi Key: CSMVOZKEWSOFER-RQNOJGIXSA-N.