PZM-21 free base · Synonyms: PZM 21 · PZM21
PZM21 is a potent and selective μ opioid receptor agonist.
For research use only. Not for human or veterinary use.
PZM-21 structure
CAS No.: 1997387-43-5
Pack sizes & pricing
| Size | Price | SKU | Stock | |
|---|---|---|---|---|
| 100 mg | USD 420.00 | BP-01957-100mg | In stock | Get quote |
| 250 mg | USD 720.00 | BP-01957-250mg | In stock | Get quote |
| 500 mg | USD 1,120.00 | BP-01957-500mg | In stock | Get quote |
| 1 g | USD 1,620.00 | BP-01957-1g | In stock | Get quote |
| 5 g | Inquire | BP-01957-5g | Inquire | Inquire |
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Description
PZM21 is a potent and selective μ opioid receptor agonist with an EC50 of 1.8 nM.
Biological activity
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. PZM21 is efficacious for the affective component of analgesia versus the reflexive component and is devoid of respiratory depression 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.
Identifiers
- SMILES
-
C[C@@H](CC1=CSC=C1)NC(=O)NC[C@H](CC1=CC=C(O)C=C1)N(C)C - InChIKey
-
MEDBIJOVZJEMBI-YOEHRIQHSA-N
Specifications
- MW (average)
- 361.5020
- Formula
- C19H27N3O2S
- CAS No.
- 1997387-43-5
- Physical state
- Solid
- Color
- white to off-white
- Shipping
- Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
- Storage
- Powder -20℃ 2 years; In solvent -20℃ 1 month;
Solubility
Soluble in DMSO