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DSP-1053

Chemical Structure : DSP-1053

CAS No.: 1176326-78-5

DSP-1053 (DSP1053)

Catalog No.: PC-63256Not For Human Use, Lab Use Only.

DSP-1053 is a novel potent serotonin reuptake (SERT) inhibitor with 5-HT1A partial agonistic activity that binds to human serotonin transporter and 5-HT1A receptor with Ki of 1.02 and 5.05 nM, respectively.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

DSP-1053 is a novel potent serotonin reuptake (SERT) inhibitor with 5-HT1A partial agonistic activity that binds to human serotonin transporter and 5-HT1A receptor with Ki of 1.02 and 5.05 nM, respectively; inhibits serotonin transporter with IC50 of 2.74 nM and shows an intrinsic activity for 5-HT1A receptors of 70.0%; dose-dependently increases extracellular 5-HT levels in rat microdialysis at 3-10 mg/kg, demonstrates antidepressant-like effect in vivo.

Depression

Phase 1 Discontinued

Physicochemical Properties

M.Wt 660.62
Formula C32H38BrNO7S
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

6-(2-{4-[4-Bromo-3-(2-methoxyethoxy)benzyl]piperidin-1-yl}ethyl)-2,3-dihydro-4H-chromen-4-one benzenesulfonate

References

1. Yoshinaga H, et al. Bioorg Med Chem. 2018 May 1;26(8):1614-1627.

2. Kato T, et al. Pharmacol Res Perspect. 2015 Jun;3(3):e00142.

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