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).
説明 | PZM21 is an effective and selective μ opioid receptor agonist (EC50: 1.8 nM). |
ターゲット&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 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]. |
分子量 | 361.5 |
分子式 | 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. 詳細
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PZM21 1997387-43-5 Endocrinology/Hormones GPCR/G Protein Neuroscience Opioid Receptor Inhibitor PZM 21 inhibit PZM-21 inhibitor