PZM21
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| Formula | C19H27N3O2S |
| Molar mass | 361.50 g·mol−1 |
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PZM21 is an experimental opioid analgesic drug that is being researched for the treatment of pain.[1] It is claimed to be a functionally selective μ-opioid receptor agonist which produces μ-opioid receptor mediated G protein signaling, with potency and efficacy similar to morphine, but with less β-arrestin 2 recruitment. In tests on mice, PZM21 was slightly less potent than morphine or TRV130 as an analgesic, but also had significantly reduced adverse effects, with less constipation than morphine, and very little respiratory depression, even at high doses.[2] This research was described as a compelling example of how modern high-throughput screening techniques can be used to discover new chemotypes with specific activity profiles, even at targets such as the μ-opioid receptor which have already been thoroughly investigated.[3]
See also
References
- ^ Kostic, Milka (September 2016). "Biasing Opioid Receptors and Cholesterol as a Player in Developmental Biology". Cell Chemical Biology. 23 (9): 1039–1040. doi:10.1016/j.chembiol.2016.09.007.
- ^ Manglik, Aashish; Lin, Henry; Aryal, Dipendra K.; McCorvy, John D.; Dengler, Daniela; Corder, Gregory; Levit, Anat; Kling, Ralf C.; Bernat, Viachaslau; Hübner, Harald; Huang, Xi-Ping; Sassano, Maria F.; Giguère, Patrick M.; Löber, Stefan; Da Duan; Scherrer, Grégory; Kobilka, Brian K.; Gmeiner, Peter; Roth, Bryan L.; Shoichet, Brian K. (2016). "Structure-based discovery of opioid analgesics with reduced side effects". Nature. doi:10.1038/nature19112. ISSN 1476-4687. PMID 27533032.
- ^ Kieffer BL. Drug discovery: Designing the ideal opioid. Nature 537, 170–171 (08 September 2016) doi:10.1038/nature19424
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