Add time:08/10/2019         Source:sciencedirect.com

A structure-activity study on neurokinin A and its C-terminal fragment NKA (4–10) has been performed in order to find selective agonists for the NK-2 receptor and identify chemical modifications suitable for protecting the peptides from degradation, while maintaining activity. Five series of compounds have been prepared and tested: 1. the complete series of the L-Ala monosubstituted analogues of NKA; 2. a series of NKA fragments from the C- or N-terminal; 3. the complete series of NKA (4–10) analogues monosubstituted with β-Ala; 4. a series of NKA (4–10) analogues with monosubstitutions in pos. 4, 8, 10 or multisubstitutions in two or more of the same position; and 5. a series of 6 NKA (4–10) analogues monosubstituted with 1-amino,1-cyclohexane carboxylic acid residue.It has been found that the most selective agonists for the NK-2 receptor system are [βAla8]NKA (4–10) and [Nle10]NKA (4–10). Protection from aminopeptidase may be obtained by acetylation of the N-terminal amide of NKA (4–10), while partial protection from endopeptidases should be expected from the presence of β-Ala in position 8. Conformational constraints induced with 1,amino,1-cyclohexane carboxylic acid residue gave weakly active compounds. Multiple substitutions reduce rather than potentiating the favorable effects of the corresponding monosubstituted compounds.

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