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Pizotifen

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Chemical Structure| 15574-96-6 同义名 : Pizotyline;BC-105;Pizotifen, Pizotyline
CAS号 : 15574-96-6
货号 : A312001
分子式 : C19H21NS
纯度 : 98%
分子量 : 295.442
MDL号 : MFCD00864192
存储条件：

粉末 Keep in dark place,Inert atmosphere,Room temperature

液体 -20°C:3-6个月-80°C:12个月
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：
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].
实验方案
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
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