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. [1]

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


Allikas: https://en.wikipedia.org/wiki/SHR9352
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