3-Quinolinecarboxamides have been synthesized and evaluated for their binding to the human NK1 receptor. Several secondary amide derivatives show NK1 receptor affinity in the picomolar range. The most active compound, hydroxymethylcarboxamide 3h showing an IC50 value in the subpicomolar range, behaved as an agonist of NK1 receptor in endothelial cell proliferation, inositol phosphate turnover, and NO-mediated cyclic GMP accumulation, thus proving it to be the first non-peptide NK1 receptor agonist showing very high potency.
Cappelli, A., Giuliani, G., Pericot Mohr, G.L., Gallelli, A., Anzini, M., Vomero, S., et al. (2004). A Non-Peptide NK1 Receptor Agonist Showing Subpicomolar Affinity. JOURNAL OF MEDICINAL CHEMISTRY, 47(6), 1315-1318 [10.1021/jm034219a].
A Non-Peptide NK1 Receptor Agonist Showing Subpicomolar Affinity
Cappelli, Andrea;Giuliani, Germano;Anzini, Maurizio;Vomero, Salvatore;Finetti, Federica;Morbidelli, Lucia;Ziche, Marina
2004-01-01
Abstract
3-Quinolinecarboxamides have been synthesized and evaluated for their binding to the human NK1 receptor. Several secondary amide derivatives show NK1 receptor affinity in the picomolar range. The most active compound, hydroxymethylcarboxamide 3h showing an IC50 value in the subpicomolar range, behaved as an agonist of NK1 receptor in endothelial cell proliferation, inositol phosphate turnover, and NO-mediated cyclic GMP accumulation, thus proving it to be the first non-peptide NK1 receptor agonist showing very high potency.
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https://hdl.handle.net/11365/3841
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