Abstract
The biogenic monoamine transporters are integral membrane proteins that perform active transport of extracellular dopamine, serotonin and norepinephrine into cells. These transporters are targets for therapeutic agents such as antidepressants, as well as addictive substances such as cocaine and amphetamine. Seminal advances in the understanding of the structure and function of this transporter family have recently been accomplished by structural studies of a bacterial transporter, as well as medicinal chemistry and pharmacological studies of mammalian transporters. This feature article focuses on antidepressant drugs that act on the serotonin and/or the norepinephrine transporters. Specifically, we focus on structure-activity relationships of these drugs with emphasis on relationships between their molecular properties and the current knowledge of transporter structure.
Publication types
-
Research Support, Non-U.S. Gov't
-
Review
MeSH terms
-
Animals
-
Antidepressive Agents / chemistry
-
Antidepressive Agents / metabolism*
-
Antidepressive Agents / pharmacology
-
Humans
-
Models, Molecular
-
Norepinephrine Plasma Membrane Transport Proteins / antagonists & inhibitors
-
Norepinephrine Plasma Membrane Transport Proteins / chemistry
-
Norepinephrine Plasma Membrane Transport Proteins / metabolism*
-
Selective Serotonin Reuptake Inhibitors / chemistry
-
Selective Serotonin Reuptake Inhibitors / metabolism
-
Selective Serotonin Reuptake Inhibitors / pharmacology
-
Serotonin Plasma Membrane Transport Proteins / chemistry
-
Serotonin Plasma Membrane Transport Proteins / metabolism*
-
Structure-Activity Relationship
Substances
-
Antidepressive Agents
-
Norepinephrine Plasma Membrane Transport Proteins
-
Serotonin Plasma Membrane Transport Proteins
-
Serotonin Uptake Inhibitors