SAR development of a selective 5-HT1D antagonist/serotonin reuptake inhibitor lead using rapid parallel synthesis.

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 α 1 and dopamine D 2 cross-reactivities.