Synthesis of the first paramagnetic and active analogue (epm-2) of the melanocyte stimulating hormone containing stable free radical in amino acid form

摘要

B "SUMMARY OF THE FIRST ANALOGUE (EPM-2) PARAMAGNETIC AND ACTIVE HONEY STIMULATOR OF MELANOCYTE CONTAINING STABLE FREE RADICAL IN THE FORM OF AMINO ACID" D. The present invention concerns the chemical synthesis, and the application in numerous biochemical assays, of a new analogue of the melanocyte stimulating hormone (244 -MSH), marked with a derivative of paramagnetic amino acid (Toac, or acid 1, 2,6,6-piperidine-N-oxide-4-amino-4-carboxylic). The analogue to which the invention refers, Acetyl-Toac ^ 0 ^ - 244 -MSH or abbreviated EPM-2 is the first reported in the scientific literature and, even containing in its structure an unnatural compound (the Toac spin marker ), fully maintained the native activity of that hormone. The activity equivalent to that of the native hormone, for allowing its study (due to the paramagnetic compound) by the spectroscopic method of electronic paramagnetic resonance (RPE) and also fluorescence (due to the presence of a natural fluorescent tryptophan residue in its structure), which this hormonal analogue presents, enables the study of the countless and relevant physiological functions already known to this neuroimmunomodulator.