Studies toward the discovery of the next generation of antidepressants. Part 2: incorporating a 5-HT(1A) antagonist component into a class of serotonin reuptake inhibitors.
The design and synthesis of a novel series of indole derivatives (9) having dual 5-HT transporter reuptake and 5-HT(1A) antagonist activity are described.
Mewshaw
Richard E
RE
Global Chemical Sciences and Neuroscience Departments, Wyeth-Ayerst Research Laboratories, PO Box 42528, Philadelphia, PA 19101-2528, USA. mewshar@war.wyeth.com
Meagher
Kristin L
KL
Zhou
Ping
P
Zhou
Dahui
D
Shi
Xiaojie
X
Scerni
Rosemary
R
Smith
Deborah
D
Schechter
Lee E
LE
Andree
Terrance H
TH
D018687:Antidepressive Agents, Second-Generation / Q000138:chemical synthesis* / Q000494:pharmacology; D002352:Carrier Proteins / Q000187:drug effects / Q000378:metabolism; D015195:Drug Design; D006801:Humans; D007202:Indicators and Reagents; D019169:Jurkat Cells; D007700:Kinetics; D008562:Membrane Glycoproteins / Q000187:drug effects / Q000378:metabolism; D026901:Membrane Transport Proteins; D009419:Nerve Tissue Proteins; D010880:Piperidines / Q000737:chemistry / Q000494:pharmacology; D011985:Receptors, Serotonin / Q000187:drug effects*; D044263:Receptors, Serotonin, 5-HT1; D012702:Serotonin Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology; D050486:Serotonin Plasma Membrane Transport Proteins; D017367:Selective Serotonin Reuptake Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship
D018687:Antidepressive Agents, Second-Generation; D002352:Carrier Proteins; D007202:Indicators and Reagents; D008562:Membrane Glycoproteins; D026901:Membrane Transport Proteins; D009419:Nerve Tissue Proteins; D010880:Piperidines; D011985:Receptors, Serotonin; D044263:Receptors, Serotonin, 5-HT1; D012702:Serotonin Antagonists; D050486:Serotonin Plasma Membrane Transport Proteins; D017367:Selective Serotonin Reuptake Inhibitors; C493230:SLC6A4 protein, human; C018181:indalpine