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Chemical Structure : PZM21
CAS No.: 1997387-43-5
Catalog No.: PC-42356Not For Human Use, Lab Use Only.
PZM21 is a potent, selective Gi-biased μ-opioid-receptor (μOR, MOR) agonist with Ki/EC50 of 1.1/4.6 nM, has little to no detectable κOR/δOR agonist or nociceptin receptor agonist activity.
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PZM21 is a potent, selective Gi-biased μ-opioid-receptor (μOR, MOR) agonist with Ki/EC50 of 1.1/4.6 nM, has little to no detectable κOR/δOR agonist or nociceptin receptor agonist activity.
PZM21 is actually an κOR antagonist (Ki=18 nM), 500- to 1,000-fold weaker activity for hERG and neurotransmitter transporters; also has no detectable β-arrestin-2 recruitment in the PathHunter assay.
Unlike morphine, PZM21 is more efficacious for the affective component of analgesia versus the reflexive component and is devoid of both respiratory depression and morphine-like reinforcing activity in mice.
| M.Wt | 361.50158 | |
| Formula | C19H27N3O2S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
Urea, N-[(2S)-2-(dimethylamino)-3-(4-hydroxyphenyl)propyl]-N'-[(1S)-1-methyl-2-(3-thienyl)ethyl]- |
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1. Manglik A, et al. Nature. 2016 Sep 8;537(7619):185-190.
2. Kostic M. Cell Chem Biol. 2016 Sep 22;23(9):1039-1040.
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