For research use only. Not for therapeutic Use.
PZM21 is a potent Gi activator with exceptional selectivity for μOR and minimal β-arrestin-2 recruitment. PZM21 is an experimental opioid analgesic drug that is being researched for the treatment of pain. It is 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.
| Catalog Number | I008934 |
| CAS Number | 1997387-43-5 |
| Synonyms | PZM21; PZM-21; PZM 21.;1-[(2S)-2-(Dimethylamino)-3-(4-hydroxyphenyl)propyl]-3-[(2S)-1-(thiophen-3-yl)propan-2-yl]urea |
| Molecular Formula | C19H27N3O2S |
| Purity | ≥95% |
| Solubility | Soluble in DMSO |
| Storage | 0 - 4 °C for short term, or -20 °C for long term |
| InChI | InChI=1S/C19H27N3O2S/c1-14(10-16-8-9-25-13-16)21-19(24)20-12-17(22(2)3)11-15-4-6-18(23)7-5-15/h4-9,13-14,17,23H,10-12H2,1-3H3,(H2,20,21,24)/t14-,17-/m0/s1 |
| InChIKey | MEDBIJOVZJEMBI-YOEHRIQHSA-N |
| SMILES | O=C(N[C@@H](C)CC1=CSC=C1)NC[C@@H](N(C)C)CC2=CC=C(O)C=C2 |
| Reference | </br>1: Manglik A, Lin H, Aryal DK, McCorvy JD, Dengler D, Corder G, Levit A, Kling RC, Bernat V, Hübner H, Huang XP, Sassano MF, Giguère PM, Löber S, Da Duan, Scherrer G, Kobilka BK, Gmeiner P, Roth BL, Shoichet BK. Structure-based discovery of opioid analgesics with reduced side effects. Nature. 2016 Sep 8;537(7619):185-190. doi: 10.1038/nature19112. PubMed PMID: 27533032; PubMed Central PMCID: PMC5161585.</br>2:Link A, Müller CE. G-Protein-Coupled Receptors: Sustained Signaling via Intracellular Megaplexes and Pathway-Specific Drugs. Angew Chem Int Ed Engl. 2016 Dec 23;55(52):15962-15964. doi: 10.1002/anie.201609015. PubMed PMID: 27775210.</br>3:Kostic M. Biasing Opioid Receptors and Cholesterol as a Player in Developmental Biology. Cell Chem Biol. 2016 Sep 22;23(9):1039-40. doi: 10.1016/j.chembiol.2016.09.007. PubMed PMID: 27662248. |
