SR-14968 explained

SR-14968 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. It is closely related to other compounds such as brorphine and SR-17018. Similarly to brorphine, SR-14968 shows robust biased agonist activity in vitro, but in animal studies in vivo behaves more like a typical opioid agonist at higher dose ranges, though still with a superior safety profile compared to unbiased agonists such as fentanyl. Compounds of this class are under development as potential analgesic medications with lower risk of overdose and drug dependence compared to traditional opioid drugs.^{[1] [2] [3] [4] [5]}

See also

• SR-16435

Notes and References

1. Schmid CL, Kennedy NM, Ross NC, Lovell KM, Yue Z, Morgenweck J, Cameron MD, Bannister TD, Bohn LM . 6 . Bias Factor and Therapeutic Window Correlate to Predict Safer Opioid Analgesics . Cell . 171 . 5 . 1165–1175.e13 . November 2017 . 10.1016/j.cell.2017.10.035 . 29149605 . 5731250 .
2. Schwienteck KL, Faunce KE, Rice KC, Obeng S, Zhang Y, Blough BE, Grim TW, Negus SS, Banks ML . 6 . Effectiveness comparisons of G-protein biased and unbiased mu opioid receptor ligands in warm water tail-withdrawal and drug discrimination in male and female rats . Neuropharmacology . 150 . 200–209 . May 2019 . 10.1016/j.neuropharm.2019.01.020 . 30660628 . 6476319 .
3. Stahl EL, Schmid CL, Acevedo-Canabal A, Read C, Grim TW, Kennedy NM, Bannister TD, Bohn LM . 6 . G protein signaling-biased mu opioid receptor agonists that produce sustained G protein activation are noncompetitive agonists . Proceedings of the National Academy of Sciences of the United States of America . 118 . 48 . November 2021 . 10.1073/pnas.2102178118 . 34819362 . 8640941 . 2021PNAS..11802178S . free .
4. Kudla L, Bugno R, Podlewska S, Szumiec L, Wiktorowska L, Bojarski AJ, Przewlocki R . Comparison of an Addictive Potential of μ-Opioid Receptor Agonists with G Protein Bias: Behavioral and Molecular Modeling Studies . Pharmaceutics . 14 . 1 . December 2021 . 55 . 10.3390/pharmaceutics14010055 . 35056950 . 8779292 . free .
5. Noble F, Marie N . Biased Opioid Ligands: Revolution or Evolution? . Frontiers in Pain Research . Lausanne, Switzerland . 2 . 722820 . 2021 . 35295469 . 8915667 . 10.3389/fpain.2021.722820 . free .