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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 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.
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. 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.
| Cell Experiment | |
|---|---|
| Cell lines | HEK-293T cells |
| Preparation method | Determination of functional activity of PZM21-29 for SAR studies was performed using a BRET-based cAMP accumulation assay50. |
| Concentrations | 10 μM |
| Incubation time | 24 h |
| Animal Experiment | |
|---|---|
| Animal models | Adult male C57BL/6J |
| Formulation | 0.9% sodium chloride |
| Dosages | |
| Administration | i.v. |
| Molecular Weight | 361.5 |
| Formula | C19H27N3O2S |
| CAS Number | 1997387-43-5 |
| Solubility (25°C) | DMSO 50 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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