First dual NK(1) antagonists-serotonin reuptake inhibitors: synthesis and SAR of a new class of potential antidepressants.
Compounds combining NK(1) antagonism and serotonin reuptake inhibition are described, and potentially represent a new generation of antidepressants. Compound 24 displays good affinities for both the NK(1) receptor and the serotonin reuptake site (32 and 25 nM, respectively).
Ryckmans
Thomas
T
Chemical Research, R&D, UCB Pharma SA, Chemin du Foriest, B-1420 Braine-l'Alleud, Belgium. thomas.ryckmans@ucb-group.com
Balançon
Laurent
L
Berton
Olivier
O
Genicot
Christophe
C
Lamberty
Yves
Y
Lallemand
Benedicte
B
Pasau
Patrick
P
Pirlot
Nathalie
N
Quéré
Luc
L
Talaga
Patrice
P
D000928:Antidepressive Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D064729:Neurokinin-1 Receptor Antagonists; D017367:Selective Serotonin Reuptake Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
D000928:Antidepressive Agents; D064729:Neurokinin-1 Receptor Antagonists; D017367:Selective Serotonin Reuptake Inhibitors