Morphiceptin

Product Name:Morphiceptin

CAS No:87777-29-5

Purity:95%

Molar Mass:521.64

Chemical Formula:C28H35N5O5

Storage:Store at -20 degrees Celsius

Sequence:Tyr-Pro-Phe-Pro-NH2

Target:µ-opoid receptor

Application:

Morphiceptin is a tetrapeptide that exhibits high selectivity for the μ-opioid receptor, making it an important compound in pain research. Structurally related to β-casomorphins, it mimics the actions of endogenous opioid peptides, resulting in analgesic properties. Morphiceptin is often used in studies focused on opioid receptor binding, pain modulation, and understanding the mechanisms of opioid activity. Its potent affinity for the μ-opioid receptor also allows researchers to explore potential therapeutic applications, such as in the development of novel analgesics, while minimizing the risks of addiction and side effects associated with traditional opioids.

Current Research:

Morphiceptin is a tetrapeptide with the amino acid sequence Tyr-Pro-Phe-Pro-NH₂, identified as a fragment of β-casomorphin, a peptide derived from the digestion of the milk protein casein. It functions as a selective agonist for the μ-opioid receptor (MOR), exhibiting over 1,000 times greater selectivity for μ- over δ-opioid receptors.

Pharmacological Profile

When administered intracerebroventricularly in animal models, morphiceptin demonstrates potent analgesic effects, with an effective dose (ED₅₀) of approximately 1.7 nmol per animal. These analgesic effects are reversed by naloxone, indicating that morphiceptin's activity is mediated specifically through μ-opioid receptors.

Structural Characteristics

As a tetrapeptide, morphiceptin's compact structure contributes to its high affinity and selectivity for MORs. The presence of the Tyr-Pro-Phe sequence is critical for receptor binding, while the C-terminal Pro-NH₂ enhances its stability and receptor specificity.

Research Applications

Due to its high selectivity and potency, morphiceptin serves as a valuable tool in neuropharmacological research:

Receptor Characterization: It aids in studying the structural and functional properties of μ-opioid receptors, enhancing our understanding of opioid receptor pharmacology.

Drug Development: Insights into its interaction with MORs contribute to the design of novel analgesics with improved efficacy and reduced side effects.

Conclusion

Morphiceptin is a potent and selective μ-opioid receptor agonist, offering significant insights into opioid receptor function and potential therapeutic avenues for pain management. Its applications extend from fundamental research to the development of novel pharmacological agents targeting the opioid system.

Reference:

Keller, M., Boissard, C., Patiny, L., Chung, N. N., Lemieux, C., Mutter, M., & Schiller, P. W. (2001). Pseudoproline-containing analogues of morphiceptin and endomorphin-2: evidence for a Cis Tyr− Pro amide bond in the bioactive conformation. Journal of medicinal chemistry, 44(23), 3896-3903.