Insertion of 2-carboxysuccinate and tricarballylic acid fragments into cyclic-pseudopeptides: new antagonists for the human tachykinin NK-2 receptor |
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| Authors: | Harmat Nicholas J S Giannotti Danilo Nannicini Rossano Perrotta Enzo Criscuoli Marco Patacchini Riccardo Renzetti Anna-Rita Giuliani Sandro Altamura Maria Maggi Carlo A |
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| Affiliation: | Menarini Ricerche S.p.A. Laboratori di Firenze, Via Rismondo 12/A, 50131 Firenze, Italy. chimfarm@menarini.ricerche.it |
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| Abstract: | A series of cyclic pseudopeptides were synthesized containing the sequence -Trp-Phe-(D)-PhePsiCH2NH-, the terminal ends of which were bound to 2-carboxy succinate or enantiomerically enriched tricarballylic acid to give the final cyclic structures. These two molecules and their subsequent derivatives were screened for h-NK2 receptor binding and functional antagonist activity on the rabbit urinary bladder. |
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