DU-125530

DU‑125530 is a potent and selective small molecule antagonist of the serotonin 5‑HT₁A receptor. It exhibits high affinity for both pre-synaptic (autoreceptor) and post-synaptic 5‑HT₁A receptors in rat and human brain tissue (Ki ≈ 0.7 nM), with much lower affinity for other serotonin receptor subtypes[3][4][5]. Preclinical studies demonstrated that DU‑125530 can block the negative feedback mechanism mediated by pre-synaptic autoreceptors that limits the efficacy of selective serotonin reuptake inhibitors (SSRIs). In clinical trials (notably NCT01119430), it was investigated as an adjunct to fluoxetine in major depressive disorder but did not show significant benefit over fluoxetine alone[1][3][7]. The compound has also been considered for anxiety and other psychiatric disorders[8].

Other names

UNII-ZB05V621UDUNII-ZB-05V621UDUNII-ZB 05V621UD1,2-Benzisothiazol-3(2H)-one, 2-(4-(4-(7-chloro-2,3-dihydro-1,4-benzodioxin-5-yl)-1-piperazinyl)butyl)-, 1,1-dioxideCHEMBL79261CHEMBL-79261CHEMBL 79261DTXSID00167208DTXSID-00167208DTXSID 00167208DTXCID5089699DTXCID-5089699DTXCID 5089699CAS 161611–99–0