| Name | PZM21 |
| Description | PZM21 is an effective and selective μ opioid receptor agonist (EC50: 1.8 nM). |
| In vitro | At hERG, PZM21 has an IC50 of between 2 and 4 μM, 500- to 1,000-fold weaker than its potency as a μOR agonist. Signalling by PZM21 and other μOR agonists appears to be mediated primarily by the heterotrimeric G protein Gi/o, as its effect on cAMP levels is eliminated by pertussis toxin and no activity is observed in a calcium release assay [1]. |
| In vivo | PZM21 is a highly selective μOR activator with significant Gi activation and minimal activation of β-arrestin-2, differentiating it from morphine by demonstrating greater efficacy in the affective aspect of pain relief compared to the reflexive aspect, without causing respiratory depression or exhibiting morphine-like addictive qualities in mice at equivalent analgesic doses. In a mouse hotplate assay, PZM21 achieved a maximal effect of 87% for pain relief 15 minutes post-administration of the highest dose [1]. Furthermore, PZM21 exerts a durable analgesic effect on central nervous system (CNS)-mediated pain without the typical opioid-induced side effects of respiratory depression and constipation [2]. |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | DMSO : 27.5 mg/mL (76.07 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (5.53 mM), Sonication is recommended.
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| Keywords | μ-opioid receptor | PZM-21 | PZM21 | PZM 21 | OpioidReceptor | Opioid Receptor | Inhibitor | inhibit |
| Inhibitors Related | Docusate sodium | Bevenopran | Mirtazapine | Matrine | (-)-Menthol | Cuminaldehyde | Progesterone | Naltrexone hydrochloride | Cebranopadol | BTRX-335140 | Bisacodyl | Mianserin hydrochloride |
| Related Compound Libraries | Target-Focused Phenotypic Screening Library | Pain-Related Compound Library | Anti-Neurodegenerative Disease Compound Library | Bioactive Compound Library | Neuronal Signaling Compound Library | Membrane Protein-targeted Compound Library | ReFRAME Related Library | Anti-Parkinson's Disease Compound Library | Neurotransmitter Receptor Compound Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-COVID-19 Compound Library |
United States
