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苯噻啶 /Pizotifen {[allProObj[0].p_purity_real_show]}

货号:A312001 同义名: Pizotyline;BC-105

Pizotifen is a highly selective 5-HT receptor blocking agent, which is a benzocycloheptane based drug.

Pizotifen 化学结构 CAS号:15574-96-6
Pizotifen 化学结构
CAS号:15574-96-6
Pizotifen 3D分子结构
CAS号:15574-96-6
Pizotifen 化学结构 CAS号:15574-96-6
Pizotifen 3D分子结构 CAS号:15574-96-6
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Pizotifen 纯度/质量文件 产品仅供科研

货号:A312001 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 5-HT 5-HT1 5-HT2 5-HT3 5-HT5 5-HT6 5-HT7 其他靶点 纯度
Desvenlafaxine ++

5-HT, Ki: 40.2 nM

98%
Lamotrigine +

5-HT (human platelets), IC50: 240 μM

5-HT (rat brain synaptosomes), IC50: 474 μM

98%
Venlafaxine 98%
Fluvoxamine maleate 99%
Iloperidone 98%
Ziprasidone HCl 98+%
Atomoxetine HCI +

5-HT, Ki: 77 nM

98%
Dapoxetine HCl 97%
Trazodone 98+%
Clomipramine HCl 98%
Mirtazapine 99+%
Escitalopram oxalate +++

5-HT, Ki: 0.89 nM

97%
Duloxetine 98+%
Sertraline HCl ++

5-HT, Ki: 13 nM

98%
Citalopram HBr +++

serotonin reuptake, IC50: 1.8 nM

98%
Latrepirdine 2HCl GluR 98%
Fluoxetine HCl 99.5%
Paroxetine hydrochloride AChR 97%
BMY 7378 ++

5-HT1A, pIC50: 6.4

5-HT1D, pIC50: 5.9

+

5-HT2, pIC50: 5.5

97%
Flibanserin +++

5-HT1A, Ki: 1 nM

+

5-HT2A, Ki: 49 nM

98%
LY310762 +

5-HT1D, Ki: 249 nM

99%+
Cyclobenzaprine HCI 99%
Blonanserin +++

5-HT2, Ki: 3.98 nM

98% HPLC
Cyproheptadine HCl ++++

5-HT2, IC50: 0.6 nM

99+%
Olanzapine 99+%
Pimavanserin hemitartrate +++

5-HT2A, pIC50: 8.7

99%
Ketanserin +++

5-HT2C (Human), Ki: 2.5 nM

5-HT2C (Rat), Ki: 50 nM

99%+
Loxapine succinate ++

5-HT2 (bovine), Ki: 6.6 nM

5-HT2 (human), Ki: 6.8 nM

99%
Agomelatine 98%
Clozapine 98%
Amitriptyline +

5-HT2, Ki: 235 nM

SERT 98%
PRX-08066 maleate +++

5-HT2B, IC50: 3.4 nM

98+%
RS-127445 ++++

5-HT2B, pIC50: 10.4

5-HT2B, pKi: 9.5

99%+
Sarpogrelate HCl ++++

5-HT2A, Kd: 2.1 nM

5-HT2C, Kd: 1.1 nM

98%
Tropisetron 99%
Palonosetron 98+%
Ramosetron HCl ++++

5-HT3 receptor, Ki: 0.091 nM

98%
Ondansetron 99%
Granisetron 98%
Alosetron HCl 98%
Ondansetron hydrochloride dihydrate 98%
VUF10166 ++++

5-HT3A, Ki: 0.04 nM

5-HT3AB, Ki: 22 nM

99%+
Azasetron hydrochloride ++++

5-HT3, IC50: 0.33 nM

98%
Asenapine maleate +++

5-HT1B, pKi: 8.4

5-HT1A, pKi: 8.6

++++

5-HT2A, pKi: 9.75

5-HT2C, pKi: 10.46

+++

5-HT5A, pKi: 8.84

++++

5-HT6, pKi: 9.6

++++

5-HT7, pKi: 9.94

97%
Risperidone ++

5-HT1B, Ki: 14.9 nM

5-HT1D, Ki: 84.6 nM

++++

5-HT2C, Ki: 12 nM

5-HT2A, Ki: 61.9 nM

+

5-HT5A, Ki: 206 nM

++

5-HT7, Ki: 6.6 nM

98%
SB 271046 HCl +++

5-HT6, pKi: 8.92

99%+
Intepirdine ++++

5-HT6, pKi: 9.63

99%+
SB-269970 HCl ++

5-HT7, pKi: 8.3

98+%
BRL 15572 ++

5-HT1D, pKi: 6

5-HT1B, pKi: 6.1

++

5-HT2A, pKi: 6.6

5-HT2B, pKi: 6.2

+

5-HT6, pKi: 5.9

+

5-HT7, pKi: 6.3

98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Pizotifen 生物活性

描述 Pizotifen is a potent 5-HT2 receptor antagonist, with a high affinity for 5-HT1C binding site[3]. Pizotifen could significantly inhibit HCT116 cells proliferation, migration, and invasion. Pizotifen could promote the apoptosis of HCT116 cells. The expression of Wnt3a and β-Catenin protein were significantly inhibited, while the expression of E-cadherin was significantly up-regulated in Pizotifen treated HCT116 cells[4]. Pizotifen also has the capacity to inhibit serotonin-enhanced ADP-induced platelet aggregation[5]. Pizotifen could inhibit the viability of gastric cancer cell lines MNK45 and AGS cells in a dose-dependent manner. Pizotifen treatment suppressed cell migration and invasion in MNK45 and AGS cells, whilst also inducing apoptosis[6]. Both in SNL (spinal nerve ligation) and CFA (complete Freund's adjuvant) mice, spinally administered pizotifen reduced mechanical and thermal hyperalgesia dose-dependently. Furthermore, high dose of pizotifen (5 μg) weakly affected motor performance and did not influence the locomotor activity in normal animals[7].

Pizotifen 参考文献

[1]Gross ML. Hemifacial spasm: treatment with pizotifen. J Neurol Neurosurg Psychiatry. 1996 Jul;61(1):118.

[2]Muller-Schweinitzer E. Pizotifen, an antimigraine drug with venoconstrictor activity in vivo. J Cardiovasc Pharmacol. 1986 Jul-Aug;8(4):805-10.

[3]Mylecharane EJ. 5-HT2 receptor antagonists and migraine therapy. J Neurol. 1991;238 Suppl 1:S45-52

[4]Piao SS, Shang B. Pizotifen Inhibits the Proliferation and Migration of Colon Cancer HCT116 Cells by Down-regulating Wnt Signaling Pathway. Ann Clin Lab Sci. 2019 Mar;49(2):183-188

[5]Lin OA, Karim ZA, Vemana HP, Espinosa EV, Khasawneh FT. The antidepressant 5-HT2A receptor antagonists pizotifen and cyproheptadine inhibit serotonin-enhanced platelet function. PLoS One. 2014 Jan 23;9(1):e87026

[6]Jiang Y, Wang W, Wu X, Shi J. Pizotifen inhibits the proliferation and invasion of gastric cancer cells. Exp Ther Med. 2020 Feb;19(2):817-824

[7]Li J, Zhang X, Xu C, Liu YX, Ge C, Zhao Z, Zhu YB, Bao HG. Intrathecally administered pizotifen alleviates neuropathic and inflammatory pain in mice by enhancing GABAergic inhibition. Neurosci Lett. 2022 Apr 1;775:136545

Pizotifen 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.38mL

0.68mL

0.34mL

16.92mL

3.38mL

1.69mL

33.85mL

6.77mL

3.38mL

Pizotifen 技术信息

CAS号15574-96-6
分子式C19H21NS
分子量 295.442
别名 Pizotyline;BC-105;Pizotifen, Pizotyline
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,Room temperature

溶解度

DMSO: 18 mg/mL(60.93 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方
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