Buclizine HCl

Research use only, not for human use.

Buclizine HCl is the hydrochloride salt form of buclizine, a piperazine histamine H1 receptor antagonist with primarily antiemetic and antivertigo activities.

Buclizine HCl is the hydrochloride salt form of buclizine, a piperazine histamine H1 receptor antagonist with primarily antiemetic and antivertigo activities. Buclizine binds to and blocks the histamine H1 receptor, thereby preventing the symptoms that are caused by histamine activity. Buclizine exerts its anti-emetic effect by binding to and blocking the muscarinic and histamine receptors in the vomiting center of the central nervous system (CNS). This may prevent activation of the chemoreceptor trigger zone (CTZ) and may reduce nausea and vomiting.

Buclizine (0.1-100 μM; 72 h) inhibits growth of MCF-7 cells.Buclizine (9.625-77 μM; 72 h) arrests the cell cycle in the G1 phase in a dose-dependent manner.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. Cell Proliferation Assay.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.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 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.

Buclizine dihydrochloride (30-200 mg/kg; tenth to fifteenth and twelfth to fifteenth days of gestation) shows potent teratogens in the rat. Animal Model:Eighty-seven mature female rats weighing 240±20 grams.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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Others

Other Targets

HT| Cholinergic

Others-Field

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129-74-8

505.95

C28H33ClN2·2HCl

>98% (HPLC)

In Vitro:?DMSO : 2.5 mg/mL (4.94 mM)

CC(C)(C)c1ccc(cc1)CN1CCN(CC1)C(c1ccccc1)c1ccc(cc1)Cl.Cl.Cl

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(-20℃)

With Ice Pack

≥ 2 years