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. 2004 Mar 11;47(6):1315-8.
doi: 10.1021/jm034219a.

A non-peptide NK1 receptor agonist showing subpicomolar affinity

Andrea Cappelli  1 , Germano Giuliani, Gal la Pericot Mohr Gl, Andrea Gallelli, Maurizio Anzini, Salvatore Vomero, Aroldo Cupello, Simona Scarrone, Mario Matarrese, Rosa Maria Moresco, Ferruccio Fazio, Federica Finetti, Lucia Morbidelli, Marina Ziche
Affiliations

A non-peptide NK1 receptor agonist showing subpicomolar affinity

Andrea Cappelli et al. J Med Chem. .

Abstract

3-Quinolinecarboxamides have been synthesized and evaluated for their binding to the human NK(1) receptor. Several secondary amide derivatives show NK(1) receptor affinity in the picomolar range. The most active compound, hydroxymethylcarboxamide 3h showing an IC(50) value in the subpicomolar range, behaved as an agonist of NK(1) receptor in endothelial cell proliferation, inositol phosphate turnover, and NO-mediated cyclic GMP accumulation, thus proving it to be the first non-peptide NK(1) receptor agonist showing very high potency.

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