Synthesis of partially modified retro-inverso substance P analogs and their biological activity

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Abstract
Partial retro-inverso modification of a single peptide bond was applied to pGlu-Phe-Phe-Gly-Leu-met-NH2 (I), a C-terminal hexapeptide analog of the neuropeptide substance P. Two analogs with reversed peptide bonds, between the pGlu-Phe and Phe-Gly residues, were prepared, purified and characterized. The analog gpGlu-(RS)-mPhe-Phe-Gly-Leu-Met-NH2 (II) was devoid of either agonistic or antagonistic activity. The 2nd pseudopeptide analog, i.e., pGlu-Phe-gPhe-mGly-Leu-Met-NH2 (III), was a full agonist with 22% of the potency of I in the guinea pig ileum assay.

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