| Identification | Back Directory | [Name]
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 | [CAS]
161611-99-0 | [Synonyms]
DU125530
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 | [Molecular Formula]
C23H26ClN3O5S | [MOL File]
161611-99-0.mol | [Molecular Weight]
491.99 |
| Hazard Information | Back Directory | [Uses]
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]. | [in vivo]
DU125530 (3 mg/kg; s.c.) reduces the reduction of 5-HT release induced by 8-OH-DPAT.html" class="link-product" target="_blank">8-OH-DPAT (HY-112061) in wild-type mice[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). |
| [IC 50]
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) | [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. DOI:10.1016/s0014-2999(97)00131-3
[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. DOI:10.1111/j.1476-5381.2011.01770.x |
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