Dermorphin
Names
[ CAS No. ]:
77614-16-5
[ Name ]:
Dermorphin
[Synonym ]:
Tyrosyl-alanyl-phenylalanyl-glycyl-tyrosyl-prolyl-serinamide
Dermorphin
H-Tyr-D-ala-phe-gly-tyr-pro-ser-NH2
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]
[Related Small Molecules]
Chemical & Physical Properties
[ Molecular Formula ]:
C40H50N8O10
[ Molecular Weight ]:
802.87300
[ Exact Mass ]:
802.36500
[ PSA ]:
314.05000
[ LogP ]:
3.98630
[ Storage condition ]:
2-8℃