PZM21

SKU: orb1302899

Description

PZM21 is a potent and selective agonist of the μ-opioid receptor, exhibiting an EC50 of 1.8 nM. This research compound is utilized in vitro and in vivo to study analgesia, opioid signaling pathways, and the development of therapeutics with potentially reduced side effects.

Research Area

Metabolism Research, Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 1997387-43-5
• MW: 361.5
• Purity: >99.99% (May vary between batches)
• Formula: C₁₉H₂₇N₃O₂S
• SMILES: C[C@@H](Cc1ccsc1)NC(=O)NC[C@H](Cc1ccc(O)cc1)N(C)C
• Target: Opioid Receptor
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (5.53 mM);DMSO:27.5 mg/mL (76.07 mM)

Bioactivity

• Target IC50:
  μ opioid receptor:1.8 nM (EC50)
• 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 . 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 .
• 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 .

Storage & Handling

• Storage: store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Inhibitor, inhibit, OpioidReceptor, Opioid Receptor, μ-opioid receptor, PZM 21, PZM21, PZM-21

Compound Identifiers

PubChem CID

121596705