Powder: -20°C for 3 years | In solvent: -80°C for 1 year
PZM21 is an effective and selective μ opioid receptor agonist (EC50: 1.8 nM).
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 44.00 | |
5 mg | In stock | $ 97.00 | |
10 mg | In stock | $ 168.00 | |
25 mg | In stock | $ 297.00 | |
50 mg | In stock | $ 513.00 | |
100 mg | In stock | $ 747.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 116.00 |
Description | PZM21 is an effective and selective μ opioid receptor agonist (EC50: 1.8 nM). |
Targets&IC50 | μ opioid receptor:1.8 nM (EC50) |
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 potent Gi activator with exceptional selectivity for μOR and minimal β-arrestin-2 recruitment. 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 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]. |
Molecular Weight | 361.5 |
Formula | C19H27N3O2S |
CAS No. | 1997387-43-5 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 27.5 mg/mL (76.07 mM)
You can also refer to dose conversion for different animals. More
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PZM21 1997387-43-5 Endocrinology/Hormones GPCR/G Protein Neuroscience Opioid Receptor Inhibitor PZM 21 inhibit PZM-21 inhibitor