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Biological Activity for PZM21
PZM21 is a selective μ receptor agonist (EC50 = 4.6 nM). PZM21 has been reported to exhibit bias for the Gi signaling pathway over arrestin-3. The compound exhibits 500-fold selectivity for μ over δ receptors and no detectable activity at κ or nociceptin receptors and a panel of 316 other GPCRs. PZM21 induces analgesia in a mouse hot plate assay, but not a tail-flick assay and exhibits no significant conditioned place preference response in in vivo assays. CNS penetrant.
Compound Libraries for PZM21
Technical Data for PZM21
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for PZM21
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions for PZM21
The following data is based on the product molecular weight 361.5. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||2.77 mL||13.83 mL||27.66 mL|
|5 mM||0.55 mL||2.77 mL||5.53 mL|
|10 mM||0.28 mL||1.38 mL||2.77 mL|
|50 mM||0.06 mL||0.28 mL||0.55 mL|
References for PZM21
References are publications that support the biological activity of the product.
Manglik et al (2016) Structure-based discovery of opioid analgesics with reduced side effects. Nature 537 185 PMID: 27533032
Hill et al (2018) The novel μ-opioid receptor agonist PZM21 depresses respiration and induces tolerance to antinociception. Br.J.Pharmacol. 175 2653 PMID: 29582414
If you know of a relevant reference for PZM21, please let us know.
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Keywords: PZM21, PZM21 supplier, selective, mu, opioid, receptor, agonist, μ, analgesic, brain, penetrant, Mu, Opioid, Receptors, 7218, Tocris Bioscience
Citations for PZM21
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
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Peptides Involved in Appetite Modulation Scientific Review
Written by Sonia Tucci, Lynsay Kobelis and Tim Kirkham, this review provides a synopsis of the increasing number of peptides that have been implicated in appetite regulation and energy homeostasis; putative roles of the major peptides are outlined and compounds available from Tocris are listed.
The key feature of drug addiction is the inability to stop using a drug despite clear evidence of harm. This poster describes the brain circuits associated with addiction, and provides an overview of the main classes of addictive drugs and the neurotransmitter systems that they target.
Peripheral sensitization is the reduction in the threshold of excitability of sensory neurons that results in an augmented response to a given external stimulus. This poster outlines the excitatory and inhibitory signaling pathways involved in modulation of peripheral sensitization. The role of ion channels, GPCRs, neurotrophins, and cytokines in sensory neurons are also described.