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首页-小分子抑制剂&激动剂-GPCR-5-HT Receptor-DSP-6745
DSP-6745

Chemical Structure : DSP-6745

CAS No.: 1355354-70-9

DSP-6745 (DSP6745)

货号: PC-22510Not For Human Use, Lab Use Only.

DSP-6745 is a potent inhibitor of 5-HT transporter (human SERT, Ki=0.653 nM), and 5-HT2A, 5-HT2C, and 5-HT7 receptors with Ki of 0.331, 1.34, and 31.7 nM, respectively.

规格 价格 库存 数量
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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

DSP-6745 is a potent inhibitor of 5-HT transporter (human SERT, Ki=0.653 nM), and 5-HT2A, 5-HT2C, and 5-HT7 receptors with Ki of 0.331, 1.34, and 31.7 nM, respectively.
DSP-6745 shows potent binding affinity for human 5-HT2B receptor and moderate binding affinity for human adrenergic α1A, 5-HT6, and sigma-1 receptors, low affinity for human dopamine D2L, histamine H1, and muscarinic M1 receptors.
DSP-6745 inhibits the calcium response mediated by human 5-HT2A, 5-HT2C, and 5-HT7 receptors in CHO-K1 cells with Kb values of 0.566, 1.37, and 2.12  nM, respectively.
DSP-6745 inhibits [3H]5-HT uptake in CHO cells expressing human SERT with an IC50 value of 0.753 nM.
DSP-6745 (6.4 and 19.1 mg/kg, p.o.) shows rapid antidepressant-like efficacy in the rat forced swim test, even at 24 h post-dosing, and anxiolytic activity in the rat social interaction test.
DSP-6745 (12.7 mg/kg, p.o.) led to an improvement in the apomorphine-induced prepulse inhibition deficit in rats.

物理化学性质&存储条件

分子量 337.41
分子式 C18H25F2N3O
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

1-{5-[(2,5-difluorobenzyl)oxy]-1-(3,3-dimethylbutyl)-1H-pyrazol-3-yl}-N-methylmethanamine

参考文献

1. Maiko Kitaichi, et al. Psychopharmacology (Berl). 2024 Jun 10. doi: 10.1007/s00213-024-06629-2.

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