[CAS NO. 1997387-43-5] PZM21
PRODUCTS SPECIFICATIONS [1997387-43-5]
DESCRIPTION [1997387-43-5]
Overview
| MDL | MFCD30802176 |
|---|---|
| Molecular Weight | 361.50 |
| Molecular Formula | C19H27N3O2S |
| SMILES | O=C(N[C@@H](C)CC1=CSC=C1)NC[C@@H](N(C)C)CC2=CC=C(O)C=C2 |
4 Publications Citing Use of MCE
Summary
PZM21 is a potent and selective μ opioid receptor agonist with an EC 50 of 1.8 nM [1] [2] [3] .
IC50 & Target
EC50: 1.8 nM (μ opioid receptor) [1]
In Vitro
PZM21 has no detectable κOR or nociceptin receptor agonist activity-it is actually an 18 nM κOR antagonist-while it is a 500-fold weaker δOR agonist, making it a selective μOR agonist. At hERG, PZM21 has an IC 50 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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
PZM21 is a potent Gi activator with exceptional selectivity for μOR and minimal β-arrestin-2 recruitment. PZM21 is efficacious for the affective component of analgesia versus the reflexive component and is devoid of respiratory depression in mice at equi-analgesic doses. PZM21 displays dose-dependent analgesia in a mouse hotplate assay, with a per cent maximal possible effect (% MPE) of 87% reached 15 min after administration of the highest dose of drug tested [1] .PZM21 has a long-lasting analgesic effect on CNS mediated-pain responses, but does not cause respiratory depression and constipation, two key side effects of opioid agonists [2] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 100 mg/mL ( 276.63 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.7663 mL | 13.8313 mL | 27.6625 mL |
| 5 mM | 0.5533 mL | 2.7663 mL | 5.5325 mL |
| 10 mM | 0.2766 mL | 1.3831 mL | 2.7663 mL |
References
- [1] Manglik A, et al. Structure-based discovery of opioid analgesics with reduced side effects. Nature. 2016 Sep 8;537(7619):185-190.
- [2] Kostic M, et al. Biasing Opioid Receptors and Cholesterol as a Player in Developmental Biology.
- [3] Araldi D, et al. Mu-opioid Receptor (MOR) Biased Agonists Induce Biphasic Dose-dependent Hyperalgesia and Analgesia, and Hyperalgesic Priming in the Rat. Neuroscience. 2018 Oct 17;394:60-71.
Synonyms