| Description |
Buclizine is an orally active antihistamine antiallergic compound. Buclizine is a potent teratogen in the rat and shows anti-tumor activity[1][2][3].
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| Related Catalog |
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| In Vitro |
Buclizine (0.1-100 μM; 72 h) inhibits growth of MCF-7 cells[2]. Buclizine (9.625-77 μM; 72 h) arrests the cell cycle in the G1 phase in a dose-dependent manner[2]. Buclizine (0-75 μM; 72 h) decreases TCTP (translationally controlled tumor protein) and cell cycle regulatory proteins expression in MCF-7 cells, increases pro-apoptotic MCL-1S expression[2]. Cell Proliferation Assay[2] Cell Line: MCF-7 cells Concentration: 0-100 μM Incubation Time: 72 hours Result: Showed considerable growth inhibition (IC50=19.18 μM). Cell Cycle Analysis[2] Cell Line: MCF-7 cells Concentration: 9.625, 19.25, 38.5, and 77 μM Incubation Time: 72 hours Result: Increased the percentages of cells in the G1 phase to 73% at 77 μM. Western Blot Analysis[2] Cell Line: MCF-7 cells Concentration: 0-75 μM Incubation Time: 72 hours Result: Decreased TCTP expression by 40% at 75 μM. Decreased cyclin D1, cyclin D3, CDK2 and CDK4 expression after 72 h.
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| In Vivo |
Buclizine dihydrochloride (30-200 mg/kg; tenth to fifteenth and twelfth to fifteenth days of gestation) shows potent teratogens in the rat[3]. Animal Model: Eighty-seven mature female rats weighing 240±20 grams[3] Dosage: 30, 40, 60, 100, and 200 mg/kg Administration: 30-200 mg/kg; tenth to fifteenth and twelfth to fifteenth days of gestation Result: Resulted in malformations in 100% of the young at a dose level of 60-100 mg/kg.
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| References |
[1]. Gamal A E Mostafa, et al. Buclizine. Profiles Drug Subst Excip Relat Methodol. 2011;36:1-33. [2]. Ean-Jeong Seo, et al. Interaction of antihistaminic drugs with human translationally controlled tumor protein (TCTP) as novel approach for differentiation therapy. Oncotarget. 2016 Mar 29;7(13):16818-39. [3]. C T King, et al. Teratogenic effect of buclizine and hydroxyzine in the rat and chlorcyclizine in the mouse. Am J Obstet Gynecol. 1966 May 1;95(1):109-11.
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