Novel serotonergic agents.
The preliminary structure-activity relationships are described for a series of substituted phenethylamines that induce the release of neuronal serotonin. Structures that also have the ability to release neuronal catecholamines are toxic to serotonin neurons, leading to long-term reductions in serotonin markers in rat brain. Conversely, compounds that are selective for the serotonin uptake carrier, and do not affect catecholamines, are not neurotoxic. It is suggested that these novel, selective serotonin releasing agents may find therapeutic utility in disorders where serotonin uptake inhibitors are currently employed.
Nichols
D E
DE
Department of Medicinal Chemistry, School of Pharmacy and Pharmacal Sciences, Purdue University, West Lafayette, Indiana 47907.
Marona-Lewicka
D
D
Huang
X
X
Johnson
M P
MP
D009474:Neurons / Q000187:drug effects* / Q000378:metabolism*; D010627:Phenethylamines / Q000737:chemistry / Q000494:pharmacology*; D012701:Serotonin / Q000378:metabolism*; D012702:Serotonin Antagonists / Q000737:chemistry / Q000494:pharmacology; D017366:Serotonin Receptor Agonists / Q000737:chemistry / Q000494:pharmacology; D017367:Selective Serotonin Reuptake Inhibitors / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
D010627:Phenethylamines; D012701:Serotonin; D012702:Serotonin Antagonists; D017366:Serotonin Receptor Agonists; D017367:Selective Serotonin Reuptake Inhibitors