Utopioid_(drug_class)

Utopioid (drug class)

Utopioid (drug class)

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Utopioids (U-type opioids) are a class of synthetic opioid analgesic drugs first developed in the 1970s by the pharmaceutical company Upjohn.[1] However, they were never marketed for medical use. Some compounds from this class have been used for scientific research as model kappa opioid receptor agonists. In the mid-2010s, one mu opioid receptor selective compound from this class, U-47700, re-emerged as a designer drug and became widely sold around the world for several years before being banned in various jurisdictions from 2016 onwards. Following the prohibition of U-47700, a number of related compounds have continued to appear on illicit drug markets. They are often marketed online or included as components in mixtures sold under the guise of "street heroin." U-47700 itself is the most potent mu opioid agonist from this class, around 7-10x the potency of morphine. Some other compounds such as 3,4-MDO-U-47700 and N-Ethyl-U-47700 retain similar mu selectivity but with lower potency similar to that of morphine, or have a mixture of mu and kappa mediated effects, such as U-48800. Most utopioid derivatives are however selective kappa agonists, which may have limited abuse potential as dissociative hallucinogens, but do not alleviate withdrawal distress in opioid dependent individuals or maintain addiction in a typical sense. Nevertheless, this has not stopped them from being sold as designer drugs, and a number of these compounds are now banned in many jurisdictions alongside U-47700 itself.[2][3][4][5][6][7][8][9]

Table of Utopioids

More information Chemical structure, Drug name ...

See also


References

  1. "Utopioids". Cayman Chemical News and Announcements. 12 July 2018.
  2. Armenian P, Vo KT, Barr-Walker J, Lynch KL (May 2018). "Fentanyl, fentanyl analogs and novel synthetic opioids: A comprehensive review". Neuropharmacology. 134 (Pt A): 121–132. doi:10.1016/j.neuropharm.2017.10.016. PMID 29042317. S2CID 21404877.
  3. Kyei-Baffour K, Lindsley CW (December 2020). "DARK Classics in Chemical Neuroscience: U-47700". ACS Chemical Neuroscience. 11 (23): 3928–3936. doi:10.1021/acschemneuro.0c00330. PMID 32639714. S2CID 220438986.
  4. Baumann MH, Tocco G, Papsun DM, Mohr AL, Fogarty MF, Krotulski AJ (November 2020). "U-47700 and Its Analogs: Non-Fentanyl Synthetic Opioids Impacting the Recreational Drug Market". Brain Sciences. 10 (11): 895. doi:10.3390/brainsci10110895. PMC 7700279. PMID 33238449.
  5. Vandeputte MM, Persson M, Walther D, Vikingsson S, Kronstrand R, Baumann MH, Gréen H, Stove CP (March 2022). "Characterization of recent non-fentanyl synthetic opioids via three different in vitro µ-opioid receptor activation assays". Archives of Toxicology. 96 (3): 877–897. doi:10.1007/s00204-021-03207-9. PMID 35072756. S2CID 246239574.
  6. Cheney BV. Structure-activity relationships for drugs binding to the agonist and antagonist states of the primary morphine receptor. J Med Chem. 1988 Mar;31(3):521-31. doi:10.1021/jm00398a007 PMID 2831361

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