Phenylalkyl 1,2-diamines as sigma-receptor ligands: the discovery of novel antidepressant agents.
This article focuses on the study of phenylalkyl 1,2-diamines as sigma-receptor ligands for the discovery of antidepressant agents. We synthesized N-chain substituted phenylalkyl 1,2-diamine derivatives. Phenylalkyl 1,2-diamines are one of the most important class of therapeutical medicines useful in managing central nervous system diseases and have been used mainly to treat obesity, narcolepsy, minimal brain dysfunction, and mild depression. In the present study, we found that phenylalkyl 1,2-diamine and amide compounds were strongly bound to the sigma-receptors and showed a potent activity of mice forced swimming test. Our article, after briefly outlining the background and nature of sigma-receptor ligands, explores the antidepressant activity of phenylalkyl 1,2-diamines.
SK Corporation, Bio-Pharmaceutical Business, Daejeon, Korea. ykk@skcorp.com
Y-G
YG
Kim
S-Y
SY
Seo
J
J
Heo
C-E
CE
Park
E-H
EH
Lee
Y-M
YM
Choi
D000818:Animals; D000928:Antidepressive Agents / Q000138:chemical synthesis / Q000494:pharmacology*; D001665:Binding Sites; D001921:Brain / Q000187:drug effects* / Q000378:metabolism; D006168:Guinea Pigs; D008024:Ligands; D008297:Male; D051379:Mice; D008813:Mice, Inbred ICR; D015394:Molecular Structure; D009043:Motor Activity / Q000187:drug effects; D010880:Piperidines / Q000138:chemical synthesis / Q000494:pharmacology*; D011437:Propylamines / Q000138:chemical synthesis / Q000494:pharmacology*; D017480:Receptors, sigma / Q000187:drug effects* / Q000378:metabolism; D013329:Structure-Activity Relationship; D013550:Swimming
D000928:Antidepressive Agents; D008024:Ligands; D010880:Piperidines; D011437:Propylamines; D017480:Receptors, sigma