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]
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Formula | C28H36N2OS2 |
Molar mass | 480.73 g·mol−1 |
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References
- 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. PMID 31457439.
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