Pizotifen hydrochloride
Based on 2 publication(s) in Google Scholar
Pizotifen hydrochloride (Pizotyline hydrochloride) is a 5-HT2 receptor antagonist. Pizotifen hydrochloride inhibits the Wnt/β-catenin-EMT signaling pathway and induces mitochondria-mediated Apoptosis. Pizotifen hydrochloride causes transient ERK1/2 phosphorylation and restores ATP. Pizotifen hydrochloride blocks Serotonin (HY-B1473A)-mediated platelet activation, inhibits Serotonin-enhanced ADP-induced platelet aggregation, and prolongs carotid artery occlusion and tail bleeding time. Pizotifen hydrochloride exhibits anticancer activity against gastric cancer and colon cancer. Pizotifen hydrochloride exerts neuroprotective effects in the striatum of R6/2 mice. Pizotifen hydrochloride can be used for research on Huntington's disease, metastasis, and thromboembolic diseases.
For research use only. We do not sell to patients.
- CAS No.: 73391-87-4
- Formula: C19H22ClNS
- Molecular Weight:331.90
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Publications Citing Use of MedChemExpress (MCE) Pizotifen hydrochloride
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Biological Activity
Description
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ERK1 |
ERK2 |
5-HT2 Receptor |
In Vitro
Pizotifen (10-20 µM; 24 h) hydrochloride inhibits the migration and invasion of MNK45 and AGS cells in Transwell assays[1].
Pizotifen (20 µM; 24 h) hydrochloride induces apoptosis in MNK45 and AGS cells[1].
Pizotifen (20 µM; 48 h) hydrochloride decreases Bcl-2 and increases Bax and active caspase-3 in MNK45 and AGS cells[1].
Pizotifen (5-25 μM; 48 h) hydrochloride inhibits HCT116 cell proliferation in a dose-dependent manner, with significant effects at 15-25 μM after 48 h and at 20 μM at 48 and 72 h[2].
Pizotifen (20 μM; 24 h) hydrochloride inhibits HCT116 cell migration and invasion, reducing migrated cells to 45 and invaded cells to 21[2].
Pizotifen (20 μM; 24 h) hydrochloride promotes apoptosis in HCT116 cells, increasing the apoptosis rate to 18.01%[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MNK45 and AGS cell lines
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Concentration:10, 20, 40 µM
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Incubation Time:24, 48, 72 h (viability measurement); 3 days (culture)
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Result:Inhibited viability of MNK45 cells in a dose-dependent manner at 48 h or 72 h.
Inhibited viability of AGS cells.
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Cell Line:MNK45 and AGS cell lines
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Concentration:10, 20 µM
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Incubation Time:24 h
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Result:Decreased migratory abilities of MNK45 cells in a dose-dependent manner at 10 and 20 µM.
Decreased migratory abilities of AGS cells at 10 and 20 µM.
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Cell Line:MNK45 and AGS cell lines
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Concentration:20 µM
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Incubation Time:48 h
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Result:Reduced Bcl-2 expression in MNK45 and AGS cells at 20 µM for 48 h.
Increased Bax and active caspase-3 expression in MNK45 and AGS cells at 20 µM for 48 h.
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Cell Line:HCT116 cells
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Concentration:5, 10, 15, 20, 25 μM (48 h); 20 μM (time-course)
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Incubation Time:48 h (dose-response); 0, 24, 48, 72 h (time-course)
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Result:Inhibited HCT116 cell proliferation dose-dependently.
Reduced proliferation significantly at 15, 20, and 25 μM after 48 h.
Decreased OD values significantly at 20 μM after 48 h and 72 h compared with negative control.
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Cell Line:HCT116 cells
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Concentration:20 μM
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Incubation Time:24 h (serum-free)
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Result:Increased apoptosis rate to 18.01% compared with 7.8% in negative control.
In Vivo
Pizotifen (10 mg/kg; i.p.; once daily; starting on day 2 after inoculation) hydrochloride inhibits metastatic progression without affecting primary tumor growth in the 4T1 mouse breast cancer model[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c (female)[4]
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Dosage:10 mg/kg
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Administration:i.p.; once daily; starting on day 2 post inoculation
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Result:Showed primary tumors equal in size to vehicle group at day 10.
Showed Ki67-positive cells in resected primary tumors same as vehicle group.
Showed less than 1% cleaved caspase 3-positive cells.
Showed no anti-tumor effect on primary tumor.
Detected no light emission in lungs, livers, or lymph nodes by bioluminescence imaging at 70 days.
Formed 0-5 metastatic nodules per lung in all 10 mice.
Detected lung metastatic lesions in only 2 of 10 mice; remaining mice showed metastatic colony formations around the bronchiole.
Showed no liver metastases in 10 mice; half showed metastatic colony formation around the portal tract.
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Animal Model:C57BL/6 (8-10 weeks old)[5]
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Dosage:3 mg/kg
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Administration:i.p.; once daily; 5 days
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Result:Prolonged time to vessel occlusion to 1199 sec.
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Animal Model:C57BL/6[5]
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Dosage:3 mg/kg
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Administration:i.p.; once daily; 5 days
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Result:Increased tail bleeding time to 714.4 sec.
Chemical Information
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CAS No. 73391-87-4
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Molecular Weight 331.90
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Formula C19H22ClNS
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SMILES
CN(CC/1)CCC1=C2C3=C(C=CC=C3)CCC4=C\2C=CS4.Cl
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Synonyms
Pizotyline hydrochloride; BC-105 hydrochloride
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (2)
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Journal Impact Factor
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Most Recent
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PLoS Negl Trop Dis
Identification of anti-flaviviral drugs with mosquitocidal and anti-Zika virus activity in Aedes aegypti. [Abstract]2019 Aug 20;13(8):e0007681. PMID: 31430351 -
Exp Ther Med
2020 Feb;19(2):817-824. PMID: 32010241
Purity & Documentation
References
[1]. Jiang Y, et al. Pizotifen inhibits the proliferation and invasion of gastric cancer cells. Experimental and therapeutic medicine. 2020 Feb;19(2):817-824. [Content Brief]
[5]. Lin OA, et al. The antidepressant 5-HT2A receptor antagonists pizotifen and cyproheptadine inhibit serotonin-enhanced platelet function. PloS one. 2014;9(1):e87026. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pizotifen hydrochloride Related Classifications
HY-B0115B Related Classifications
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Keywords
- Pizotifen
- 73391-87-4
- Pizotyline
- BC-105
- BC105
- BC 105
- 5-HT Receptor
- Wnt
- β-catenin
- Apoptosis
- ERK
- ATP Synthase
- Mitochondrial Metabolism
- ERK1/2 phosphorylation
- Huntington's disease
- Wnt/β-catenin-EMT signaling
- colon cancer
- gastric cancer
- metastasis
- mitochondrial-mediated apoptosis
- platelet activation
- serotonin 5-HT2A/HTR2C receptor
- thromboembolic disorders
- Inhibitor
- inhibitor
- inhibit