Abstract
Incorporation of an SRI (serotonin reuptake inhibitor) pharmacophore into a selective 5-HT(1D) agonist has led to the discovery of a molecule having both 5-HT(1D) antagonist and SRI activity. RPS methodology was used to develop the SAR and identify potential approaches to reduce unwanted adrenergic alpha 1 and dopamine D(2) cross-reactivities.
MeSH terms
-
Cell Line
-
Cross Reactions
-
Guanosine 5'-O-(3-Thiotriphosphate) / metabolism
-
Heterocyclic Compounds, 4 or More Rings / chemical synthesis
-
Heterocyclic Compounds, 4 or More Rings / pharmacology
-
Humans
-
Receptor, Serotonin, 5-HT1D / metabolism
-
Selective Serotonin Reuptake Inhibitors / chemical synthesis*
-
Serotonin 5-HT1 Receptor Antagonists*
-
Serotonin Antagonists / chemical synthesis*
-
Structure-Activity Relationship
Substances
-
Heterocyclic Compounds, 4 or More Rings
-
Receptor, Serotonin, 5-HT1D
-
Serotonin 5-HT1 Receptor Antagonists
-
Serotonin Antagonists
-
Serotonin Uptake Inhibitors
-
Guanosine 5'-O-(3-Thiotriphosphate)