Studies towards the next generation of antidepressants. Part 1 : Indolylcyclohexylamines as potent serotonin reuptake inhibitors

A series of indolylcyclohexylamines possessing potent and selective serotonin reuptake inhibition is reported. The most interesting compounds proved to have subnanomolar 5-HT transporter activity, and exhibited moderate 5-HT(1A) affinity.

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2001-07, Vol.11 (14), p.1885-1888
Main Authors: MEAGHER, Kristin L, MEWSHAW, Richard E, ANDREE, Terrance H, EVRARD, Deborah A, PING ZHOU, SMITH, Deborah L, SCERNI, Rosemary, SPANGLER, Taylor, ABULHAWA, Susan, XIAOJIE SHI, SCHECHTER, Lee E
Format: Article
Language:English
Subjects:
Animals
Antidepressive Agents - chemical synthesis
Antidepressive Agents - pharmacology
Biological and medical sciences
Carrier Proteins - drug effects
Carrier Proteins - metabolism
CHO Cells
Cricetinae
Cyclohexylamines - chemical synthesis
Cyclohexylamines - pharmacology
Humans
Indoles - chemistry
Inhibitory Concentration 50
Medical sciences
Membrane Glycoproteins - drug effects
Membrane Glycoproteins - metabolism
Membrane Transport Proteins
Nerve Tissue Proteins
Neuropharmacology
Neurotransmitters. Neurotransmission. Receptors
Pharmacology. Drug treatments
Rats
Receptors, Adrenergic, alpha - drug effects
Receptors, Adrenergic, alpha - metabolism
Receptors, Serotonin - drug effects
Receptors, Serotonin - metabolism
Receptors, Serotonin, 5-HT1
Serotonin Plasma Membrane Transport Proteins
Serotonin Uptake Inhibitors - metabolism
Serotonin Uptake Inhibitors - pharmacology
Serotoninergic system
Structure-Activity Relationship
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Description
Summary:A series of indolylcyclohexylamines possessing potent and selective serotonin reuptake inhibition is reported. The most interesting compounds proved to have subnanomolar 5-HT transporter activity, and exhibited moderate 5-HT(1A) affinity.
ISSN:0960-894X
1464-3405
DOI:10.1016/S0960-894X(01)00334-1