SR 17018

SR 17018 is an orally bioavailable and brain-penetrant agonist of µ-opioid receptors. It is functionally selective for G protein-coupled receptor signaling (EC50 = 97 nM for GTPgammaS binding in CHO cells expressing µ-opioid receptors) over beta-arrestin 2 recruitment (EC50 = >10,000 nM) at the µ-opioid receptor. SR 17018 increases latency to withdraw in the hot plate and warm water tail-flick assay (ED50s = 6.9 and 7.7 mg/kg, respectively) without inducing respiratory depression in mice when administered at doses up to 48 mg/kg. SR 17018 was designed for this biased agonism at the µ-opioid receptor to potentially widen the therapeutic window and reduce adverse effects of µ-opioid receptors, such as respiratory depression.Formal Name: 5,6-dichloro-1-[1-[(4-chlorophenyl)methyl]-4-piperidinyl]-1,3-dihydro-2H-benzimidazol-2-one. CAS Number: 2134602-45-0. Molecular Formula: C19H18Cl3N3O. Formula Weight: 410.7. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 1 mg/ml, DMSO: 1 mg/ml, DMSO:PBS (pH 7.2) (1:2): 0.33 mg/ml, Ethanol: slightly soluble. lambdamax: 216, 302 nm. SMILES: ClC(C=C1)=CC=C1CN2CCC(N3C(NC4=C3C=C(Cl)C(Cl)=C4)=O)CC2. InChi Code: InChI=1S/C19H18Cl3N3O/c20-13-3-1-12(2-4-13)11-24-7-5-14(6-8-24)25-18-10-16(22)15(21)9-17(18)23-19(25)26/h1-4,9-10,14H,5-8,11H2,(H,23,26). InChi Key: LAGUDYUGRSQDKS-UHFFFAOYSA-N.