Pizotifen | Pizotyline | 5-HT Receptor Antagonist | AmBeed-信号通路专用抑制剂

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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 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]} 产品说明书

批次查询：批次纯度: COA SDS NMR HPLC CNMR LC-MS

全球学术期刊中引用的产品: • Nat. Biomed. Eng., 2024, 8, 1412-1424. Ambeed. [ A538667 , A631746 ]; • JMC, 2024. Ambeed. [ A833302 , A475501 , A341986 , A356070 ]; • BMC Cancer, 2024, 24(1): 1415. Ambeed. [ A809692 , A209020 ]; • J. Am. Soc. Mass Spectrom., 2024, 35(12): 3192-3202. Ambeed. [ A166127 , A902473 , A753371 , A961334 , A292945 , A230770 , A300620 , A1114580 , A1159765 , A206238 ]; • PloS One, 2024, 19(11): e0308060. Ambeed. [ A302917 ]; 更多 >

5-羟色胺受体亚型比较

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 (human), Ki: 6.8 nM 5-HT2 (bovine), Ki: 6.6 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, pKi: 9.5 5-HT2B, pIC50: 10.4						99%+
Sarpogrelate HCl			++++ 5-HT2C, Kd: 1.1 nM 5-HT2A, Kd: 2.1 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-HT1A, pKi: 8.6 5-HT1B, pKi: 8.4	++++ 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-HT2A, Ki: 61.9 nM 5-HT2C, Ki: 12 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

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

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Pizotifen 纯度/质量文件 产品仅供科研

全球学术期刊中引用的产品

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Pizotifen 参考文献

Pizotifen 实验方案

Pizotifen 技术信息

最近浏览的产品

大规格询价

摩尔计算器

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总药量计算器

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细胞研究

临床研究

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