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Synthesis and biological evaluation of tripeptide derivatives of Cbz-Gly-Leu-Trp-OBzl(CF3)2 as NK1/NK2 ligands |
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| Authors: | Millet Régis Goossens Jean-François Bertrand-Caumont Karine Houssin Raymond Hénichart Jean-Pierre |
| Affiliation: | (1) Institut de Chimie Pharmaceutique, Université de Lille 2-Droit et Santé, 3 rue du Professeur Laguesse, B.P. 83, F-59006 Lille Cedex, France;(2) Laboratoire de Chimie Analytique, Faculté de Pharmacie, Université de Lille 2-Droit et Santé, 3 rue du Professeur Laguesse, B.P. 83, F-59006 Lille Cedex, France;(3) Chemin du Foriest, UCB S.A. Pharma Sector, B-1420 Braine l'Alleu, Belgium |
| Abstract: | Summary Chemical modifications were obtained on the dual NK1/NK2 ligand Cbz-Gly-Leu-Trp-OBzl(CF3)2 with a view to optimizing affinities for both NK1 and NK2 receptors. Replacement of the Gly residue by other amino acids increased affinities for NK1/NK2 receptors or induced selectivity for the NK1 receptor. |
| Keywords: | neurokinin A substance P tachykinins |
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