| ID | 1314 | |
| PMID | 2845208 | |
| Year | 1988 | |
| Sequence | SYS-Nle-EHfRWGKPV | |
| Name | [Nle4, D-Phe7]-alpha-MSH | |
| Length | 13 | |
| N-Terminal Modification | Acetylation | |
| C-Terminal Modification | Amidation | |
| Linear/ Cyclic | Linear | |
| Chirality | Mix | |
| Chemical Modification | Nle=Norleucine | |
| Origin of Peptide | Derived from α-MSH | |
| Nature of Peptide/Cargo | A superpotent(10-1000 times) analogue of alpha-melanocyte stimulating hormone, it causes a very long lasting stimulation of melanocytes in vitro and in vivo, its nonbiodegradeable and it is resistant to enzymatic inactivation by sera, brain enzymes or purified proteolytic enzymes. | |
| Mechanism | Topically applied melanotropin could activate cellular processes within follicular melanocytes leading to new eumelanin formation | |
| Cargo Sequence/Structure | None | |
| Name of cargo | Not applicable | |
| Assay | Radioimmunoassay | |
| Enhancer | Each skin sample was sectioned, stained with hematoxylin and eosin and examined by light microscopy | |
| Properties of enhancer | Not mentioned | |
| Concentration | First dissolved at 10-3M in distilled water and then diluted in a polyethylene glycol vehicle (26% PEG 400 and 74% PEG 3350, by weight) to 10-4M | |
| Incubation time | 24 hours | |
| Tissue permeability (value with units) | Percent positive samples of transdermal delivery :11.8% (2/17) | |
| Tissue Sample | Full thickness skin samples (approximately 1 and a half" in diameter) were removed from the trunk area of mature Sprague Dawley rats. | |
| Ex vivo/In vivo/In vitro | in vivo | |
| STRUCTURE |
| |
| SMILES | CC(=O)N[C@@H](CO)C(=O)N[C@@H](Cc1ccc(O)cc1)C(=O)N[C@@H](CO) C(=O)N[C@@H](CCCC)C(=O)N[C@H](CCC(=O)O)C(=O)N[C@H](Cc1nc[nH]c1)C (=O)N[C@@H](Cc1ccccc1)C(=O)N[C@@H](CCCNC(=[NH2])N)C(=O) N[C@@H](Cc1c[nH]c2ccccc12)C(=O)NCC(=O)N[C@@H](CCCC[NH3]) C(=O)N1CCC[C@H]1C(=O)N[C@@H](C(C)C)C(=O)N | |