SR-17018

{{Short description|Chemical compound}}

{{Drugbox

| IUPAC_name = 5,6-dichloro-3-[1-[(4-chlorophenyl)methyl]piperidin-4-yl]-1H-benzimidazol-2-one

| image = SR-17018.svg

| image_class = skin-invert-image

| tradename =

| legal_US =

| legal_status =

| bioavailability =

| metabolism =

| elimination_half-life =

| excretion =

| CAS_number_Ref = {{cascite|correct|CAS}}

| CAS_number = 2134602-45-0

| UNII_Ref = {{fdacite|correct|FDA}}

| ChEMBL = 4452384

| PDB_ligand = WH9

| UNII = 2M8P7UAW4W

| PubChem = 130431397

| ChemSpiderID = 67886365

| C = 19

| H = 18

| Cl = 3

| N = 3

| O = 1

| SMILES = C1CN(CCC1N2C3=CC(=C(C=C3NC2=O)Cl)Cl)CC4=CC=C(C=C4)Cl

| StdInChI = 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)

| StdInChIKey = LAGUDYUGRSQDKS-UHFFFAOYSA-N

}}

SR-17018 is a drug which acts as a biased agonist at the μ-opioid receptor, selective for activation of the G-protein signalling pathway over β-arrestin 2 recruitment.{{cite journal |vauthors=Schmid CL, Kennedy NM, Ross NC, Lovell KM, Yue Z, Morgenweck J, Cameron MD, Bannister TD, Bohn LM |title=Bias Factor and Therapeutic Window Correlate to Predict Safer Opioid Analgesics |journal=Cell |volume=171 |issue=5 |pages=1165–75.e13 |date=November 2017 |pmid=29149605 |pmc=5731250 |doi=10.1016/j.cell.2017.10.035 }} In animal studies it produces analgesic effects but with less respiratory depression and development of tolerance than conventional opioids.{{cite journal | vauthors = Grim TW, Schmid CL, Stahl EL, Pantouli F, Ho JH, Acevedo-Canabal A, Kennedy NM, Cameron MD, Bannister TD, Bohn LM | display-authors = 6 | title = A G protein signaling-biased agonist at the μ-opioid receptor reverses morphine tolerance while preventing morphine withdrawal | journal = Neuropsychopharmacology | volume = 45 | issue = 2 | pages = 416–425 | date = January 2020 | pmid = 31443104 | doi = 10.1038/s41386-019-0491-8 | pmc = 6901606 }}{{cite journal |vauthors=Grim TW, Acevedo-Canabal A, Bohn LM |title=Toward Directing Opioid Receptor Signaling to Refine Opioid Therapeutics |journal=Biol Psychiatry |volume=87 |issue=1 |pages=15–21 |date=January 2020 |pmid=31806082 |pmc=6919561 |doi=10.1016/j.biopsych.2019.10.020 }}{{cite journal | vauthors = Podlewska S, Bugno R, Kudla L, Bojarski AJ, Przewlocki R | title = Molecular Modeling of µ Opioid Receptor Ligands with Various Functional Properties: PZM21, SR-17018, Morphine, and Fentanyl-Simulated Interaction Patterns Confronted with Experimental Data | journal = Molecules | volume = 25 | issue = 20 | date = October 2020 | page = 4636 | pmid = 33053718 | doi = 10.3390/molecules25204636 | pmc = 7594085 | doi-access = free }}{{cite journal | vauthors = Pantouli F, Grim TW, Schmid CL, Acevedo-Canabal A, Kennedy NM, Cameron MD, Bannister TD, Bohn LM | display-authors = 6 | title = Comparison of morphine, oxycodone and the biased MOR agonist SR-17018 for tolerance and efficacy in mouse models of pain | journal = Neuropharmacology | pages = 108439 | date = December 2020 | volume = 185 | pmid = 33345829 | doi = 10.1016/j.neuropharm.2020.108439 | pmc = 7887086 | s2cid = 229306872 }}