1. GPCR/G Protein
    Neuronal Signaling
  2. Opioid Receptor

PZM21 

Cat. No.: HY-101386 Purity: 98.54%
Data Sheet SDS Handling Instructions

PZM21 is a potent and selective μ opioid receptor agonist with an EC50 of 1.8 nM.

For research use only. We do not sell to patients.
PZM21 Chemical Structure

PZM21 Chemical Structure

CAS No. : 1997387-43-5

Size Price Stock Quantity
10 mM * 1 mL in DMSO $358 In-stock
1 mg $150 In-stock
5 mg $450 In-stock
10 mg $650 In-stock
50 mg $1950 In-stock
100 mg $2650 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

PZM21 is a potent and selective μ opioid receptor agonist with an EC50 of 1.8 nM.

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 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. PZM21 does not exhibit the type of biomarker responses, such as hyperlocomotion or conditioned place preference response, that are observed when morphine and other opioids are used and are associated with reinforcement and addiction[2].

References
Preparing Stock Solutions
Concentration Volume 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
Please refer to the solubility information to select the appropriate solvent.
Animal Administration
[1]

Mouse: PZM21 is dissolved in 0.9% sodium chloride. Mice are injected with either vehicle, morphine (5 mg/kg, or 10 mg/kg), TRV130 (1.2 mg/kg) or PZM21 (10 mg/kg; 20 mg/kg; or 40 mg/kg). After injection of drug, the analgesic effect expressed as percentage maximum possible effect (%MPE) is measured at 15, 30, 60, 90 and 120 min after drug treatment[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

361.5

Formula

C₁₉H₂₇N₃O₂S

CAS No.

1997387-43-5

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
PZM21
Cat. No.:
HY-101386
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