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.

Cappelli, A., Giuliani, G., Pericot Mhor, G., Galleli, A., Anzini, M., Vomero, S., et al. (2004). A Non-peptide NK1 receptor agonist showing subpicomolar affinità. JOURNAL OF MEDICINAL CHEMISTRY, 47(6), 1315-1318 [10.1021/jm034219a].

A Non-peptide NK1 receptor agonist showing subpicomolar affinità

MORESCO, ROSA MARIA;FAZIO, FERRUCCIO;
2004

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.
Articolo in rivista - Articolo scientifico
NK1 receptor, agonist, affinity,
English
2004
47
6
1315
1318
none
Cappelli, A., Giuliani, G., Pericot Mhor, G., Galleli, A., Anzini, M., Vomero, S., et al. (2004). A Non-peptide NK1 receptor agonist showing subpicomolar affinità. JOURNAL OF MEDICINAL CHEMISTRY, 47(6), 1315-1318 [10.1021/jm034219a].
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/10281/1860
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