Product Name:PL 017
Synonyms:PL 017
CAS No:83397-56-2
Purity:95%
Molar Mass:535.6
Chemical Formula:C29H37N5O5
Storage:Store at -20 degrees Celsius
Sequence:YPFP
Target:delta-opioid receptor (DOR)
Application:
PL 017 is a synthetic peptide that acts as a selective agonist for the delta-opioid receptor (DOR). This peptide is utilized in research to study the role of delta-opioid receptors in pain modulation, mood regulation, and neuroprotection. Delta-opioid receptors are one of the three main classes of opioid receptors, and their activation by agonists like PL 017 has been shown to produce analgesic effects without the addictive potential commonly associated with mu-opioid receptor agonists. PL 017 is particularly valuable in studies focused on developing new pain therapies, understanding opioid receptor signaling, and exploring the potential therapeutic applications of delta-opioid receptor activation in conditions such as chronic pain, anxiety, and neurodegenerative diseases.
Current Research:
PL-017, also known as [N-MePhe³,D-Pro⁴]-morphiceptin, is a synthetic analog of morphiceptin that functions as a potent and selective agonist for the μ-opioid receptor (MOR). It exhibits an inhibitory concentration (IC₅₀) of 5.5 nM for the displacement of [¹²⁵I]-FK 33,824 binding to μ-opioid sites, indicating high affinity for these receptors. In contrast, PL-017 shows significantly lower affinity for δ-opioid receptors, with an IC₅₀ exceeding 10,000 nM for [¹²⁵I]-DADLE binding, underscoring its selectivity for MOR.
Pharmacological Profile
In vivo studies have demonstrated that intracerebroventricular administration of PL-017 in male Sprague-Dawley rats induces dose-dependent analgesia, with the peak effect occurring approximately 15 to 30 minutes post-injection at lower doses. Higher doses result in analgesic effects lasting up to four hours. These analgesic effects are reversible by naloxone, confirming the involvement of μ-opioid receptors.
Clinical Implications
The high selectivity and potency of PL-017 for μ-opioid receptors make it a valuable tool in pain management research. Its ability to produce long-lasting analgesia with a reversible profile suggests potential therapeutic applications in conditions requiring effective pain control. However, further studies are necessary to fully elucidate its clinical utility and safety profile.
Conclusion
PL-017 is a potent and selective μ-opioid receptor agonist with significant analgesic properties. Its high affinity for MOR and minimal interaction with δ-opioid receptors highlight its potential as a therapeutic agent in pain management. Ongoing research is essential to explore its efficacy and safety in clinical settings.
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