DU125530

Names

[ Name ]:
DU125530

[Synonym ]:
1,2-Benzisothiazol-3(2H)-one,2-(4-(4-(7-chloro-2,3-dihydro-1,4-benzodioxin-5-yl)-1-piperazinyl)butyl)-,1,1-dioxide
UNII-ZB05V621UD

Biological Activity

[Description]:

DU125530 is a potent and selective5-HT1A receptor antagonist with Ki values of 0.7, 890, 1200, 240, 750, 1100 nM for 5-HT1A, 5-HT1B, 5-HT1D, 5-HT2A, 5-HT2C, 5-HT3, respectively. DU125530 shows antidepressant effects[1][2].

[Related Catalog]:

Research Areas >> Neurological Disease

Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor

Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor

[Target]

5-HT1A Receptor:0.7 nM (Ki)

5-HT1B Receptor:890 nM (Ki)

5-HT1C Receptor:1200 nM (Ki)

5-HT2A Receptor:240 nM (Ki)

5-HT2C Receptor:750 nM (Ki)

5-HT3 Receptor:1100 nM (Ki)

[In Vivo]

DU125530 (3 mg/kg; s.c.) 在野生型小鼠中的降低 8-OH-DPAT (HY-112061) 诱导的 5-HT 释放的减少[1]。 Animal Model: wild-type mice[2] Dosage: 3 mg/kg Administration: S.c. Result: Prevented the reduction of 5-HT release induced by 0.5 mg·kg−1 s.c. 8-OH-DPAT in WT mice, alone had no effect on the extracellular 5-HT concentration in mPFC of wild-type mice (WT) nor in 5-HT1A receptor knock-out mice (KO).

[References]

[1]. Mos J, et al. The putative 5-HT1A receptor antagonist DU125530 blocks the discriminative stimulus of the 5-HT1A receptor agonist flesinoxan in pigeons. Eur J Pharmacol. 1997 May 1;325(2-3):145-53.

[2]. Scorza MC, et al. Preclinical and clinical characterization of the selective 5-HT(1A) receptor antagonist DU-125530 for antidepressant treatment. Br J Pharmacol. 2012 Nov;167(5):1021-34.

Chemical & Physical Properties

[ Molecular Formula ]:
C₂₃H₂₆ClN₃O₅S

[ Molecular Weight ]:
491.98800

[ Exact Mass ]:
491.12800

[ PSA ]:
87.77000

[ LogP ]:
3.87970

Related Compounds

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