Abstract
Derivatives of the serotonin reuptake inhibitor 4-(5-fluoro-1H-indol-3-yl)cyclohexylamine, in which serotonin 1A (5-HT(1A)) receptor pharmacophoric elements are incorporated, are reported. Analogs exhibiting affinity for both the serotonin transporter and the 5-HT(1A) receptor are described. Compounds containing 1-(4-indolyl)piperazine and 2-(1H-indol-4-yloxy)ethylamine are promising leads for further SAR studies.
MeSH terms
-
Antidepressive Agents / chemical synthesis*
-
Antidepressive Agents / chemistry
-
Cyclohexylamines / chemical synthesis*
-
Cyclohexylamines / chemistry
-
Drug Design
-
Ethylamines
-
Humans
-
Membrane Glycoproteins / chemistry*
-
Membrane Transport Proteins / chemistry*
-
Nerve Tissue Proteins / chemistry*
-
Piperazines
-
Protein Binding
-
Receptor, Serotonin, 5-HT1A / chemistry*
-
Selective Serotonin Reuptake Inhibitors / chemical synthesis*
-
Selective Serotonin Reuptake Inhibitors / chemistry
-
Serotonin Plasma Membrane Transport Proteins
-
Structure-Activity Relationship
Substances
-
Antidepressive Agents
-
Cyclohexylamines
-
Ethylamines
-
Membrane Glycoproteins
-
Membrane Transport Proteins
-
Nerve Tissue Proteins
-
Piperazines
-
SLC6A4 protein, human
-
Serotonin Plasma Membrane Transport Proteins
-
Serotonin Uptake Inhibitors
-
Receptor, Serotonin, 5-HT1A