SHR9352

SHR9352 is a drug which acts as a potent and selective biased agonist at the μ-opioid receptor, selective for activation of the G-protein signalling pathway over β-arrestin 2 recruitment. It was structurally derived from oliceridine by replacing the benzylic side chain with a cyclised group, although only some compounds in the series retained the desired biased agonist profile, with some derivatives such as compound 12 being potent, unbiased μ-opioid full agonists.[1]

Compound 12 from Li et al.
SHR9352
Identifiers
IUPAC name
  • (1'S)-N-[2-[(9R)-9-pyridin-2-yl-6-oxaspiro[4.5]decan-9-yl]ethyl]spiro[1,3-dithiolane-2,4'-2,3-dihydro-1H-naphthalene]-1'-amine
PubChem CID
Chemical and physical data
FormulaC28H36N2OS2
Molar mass480.73 g·mol−1
3D model (JSmol)
SMILES
  • C1CCC2(C1)C[C@](CCO2)(CCN[C@H]3CCC4(C5=CC=CC=C35)SCCS4)C6=CC=CC=N6
InChI
  • InChI=1S/C28H36N2OS2/c1-2-8-23-22(7-1)24(10-13-28(23)32-19-20-33-28)29-17-14-26(25-9-3-6-16-30-25)15-18-31-27(21-26)11-4-5-12-27/h1-3,6-9,16,24,29H,4-5,10-15,17-21H2/t24-,26+/m0/s1
  • Key:WRBLHOVSELHRMG-AZGAKELHSA-N

See also

References
  1. Li X, He W, Chen Y, Yang G, Wan H, Zhang L, et al. (December 2017). "Discovery of SHR9352: A Highly Potent G Protein-Biased μ-Opioid Receptor Agonist". ACS Omega. 2 (12): 9261–9267. doi:10.1021/acsomega.7b01452. PMC 6645658. PMID 31457439.
  • Media related to SHR9352 at Wikimedia Commons


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