Dermorphin

Modify Date: 2024-01-09 22:29:40

Dermorphin Structure
Dermorphin structure
Common Name Dermorphin
CAS Number 77614-16-5 Molecular Weight 802.87300
Density N/A Boiling Point N/A
Molecular Formula C40H50N8O10 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Dermorphin


Dermorphin is a natural heptapeptide μ-opioid receptor (MOR) agonist found in amphibian skin.

 Names

Name (2S)-N-[(2S)-1-amino-3-hydroxy-1-oxopropan-2-yl]-1-[(2S)-2-[[2-[[(2S)-2-[[(2R)-2-[[(2S)-2-amino-3-(4-hydroxyphenyl)propanoyl]amino]propanoyl]amino]-3-phenylpropanoyl]amino]acetyl]amino]-3-(4-hydroxyphenyl)propanoyl]pyrrolidine-2-carboxamide
Synonym More Synonyms

 Dermorphin Biological Activity

Description Dermorphin is a natural heptapeptide μ-opioid receptor (MOR) agonist found in amphibian skin.
Related Catalog
Target

μ-opioid receptor (MOR)[1]

In Vitro Dermorphin, a peptide isolated from the skin of Phyllomedusa frogs and the peptide receptor (NOP) component by the endogenous agonist nociceptin/orphanin FQ (N/OFQ). In displacement binding studies at CHOhMu, Dermorphin and DeNo displac the binding of [3H]-DPN in a concentration dependent and saturable manner. Dermorphin displays an affinity of 7.17, while N/OFQ fails to displace [3H]-DPN at the Delta receptor. Dermorphin and DeNo stimulate the binding of GTPγ[35S] in a concentration dependent and saturable manner at the Mu receptor[2].
Kinase Assay Membrane protein (40 μg) is incubated in 0.5 mL volume of 50 mM Tris, 0.2 mM EGTA, 1 mM MgCl2, 100 mM NaCl, 0.1% BSA, 0.15 mM bacitracin; pH 7.4, GDP (33 μM), and ∼150 pM GTPγ[35S]. Varying concentrations of reference ligands (Dermorphin, N/OFQ, Dynorphin-A and Leu-enkephalin) or DeNo (1 pM-10 μM) is added prior to incubation. Non-specific binding is determined in the presence of unlabeled GTPγS (10 μM). Samples are incubated at 30°C for 1 h with gentle agitation. Reactions are terminated by vacuum filtration through dry Whatman GF/B filters, using a Brandel harvester[2].
References

[1]. Tiwari V, et al. Activation of Peripheral μ-opioid Receptors by Dermorphin [D-Arg2, Lys4] (1-4) Amide Leads to Modality-preferred Inhibition of Neuropathic Pain. Anesthesiology. 2016 Mar;124(3):706-20.

[2]. Bird MF, et al. Characterisation of the Novel Mixed Mu-NOP Peptide Ligand Dermorphin-N/OFQ (DeNo). PLoS One. 2016 Jun 7;11(6):e0156897.

 Chemical & Physical Properties

Molecular Formula C40H50N8O10
Molecular Weight 802.87300
Exact Mass 802.36500
PSA 314.05000
LogP 3.98630
Storage condition 2-8℃

 Synonyms

Tyrosyl-alanyl-phenylalanyl-glycyl-tyrosyl-prolyl-serinamide
Dermorphin
H-Tyr-D-ala-phe-gly-tyr-pro-ser-NH2
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