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Buclizine dihydrochloride

Catalog No. T6426 CAS 129-74-8

Synonyms: Longifene, Buclina, Buclizine HCl, UCB-4445

Buclizine dihydrochloride (Buclina) is the hydrochloride salt form of buclizine, a piperazine histamine H1 receptor antagonist with primarily antiemetic and antivertigo activities. Buclizine dihydrochloride binds to and blocks the histamine H1 receptor, thereby preventing the symptoms that are caused by histamine activity. Buclizine dihydrochloride 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.

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Buclizine dihydrochloride Chemical Structure

Buclizine dihydrochloride, CAS 129-74-8

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50 mg	In stock	$ 30.00
100 mg	In stock	$ 42.00
200 mg	In stock	$ 55.00
1 mL * 10 mM (in DMSO)	In stock	$ 45.00

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Purity: 99.56%

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Description	Buclizine dihydrochloride (Buclina) is the hydrochloride salt form of buclizine, a piperazine histamine H1 receptor antagonist with primarily antiemetic and antivertigo activities. Buclizine dihydrochloride binds to and blocks the histamine H1 receptor, thereby preventing the symptoms that are caused by histamine activity. Buclizine dihydrochloride 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.
In vitro	Buclizine hydrochloride, a piperazine derivative, is a sedating antihistamine with antimuscarinic and moderate sedative action. Buclizine is used in the prevention and treatment of nausea, vomiting, and dizziness associated with motion sickness. Additionally, it has been used in the management of vertigo in diseases affecting the vestibular apparatus. Although the mechanism by which buclizine exerts its antiemetic and antivertigo effects has not been fully elucidated, its central anticholinergic properties are partially responsible. The drug depresses labyrinth excitability and vestibular stimulation, and it may affect the medullary chemoreceptor trigger zone. It also possesses anticholinergic, antihistaminic, central nervous system depressant, and local anesthetic effects. [1]
Kinase Assay	Topoisomerase I Catalytic Actioity Assay [1]: Topoisomerase I Catalytic Actioity Assay: The enzymatic activity is analyzed by the DNA unwinding assay. DNA topoisomerase I, from TopoGEN (1 unit, which is defined as the amount of enzyme that converts 0.5 μg of superhelical DNA to the relaxed state in 30 minutes at 37 °C), is incubated with 0.5 μg of 6x174 RF DNA, in the presence or absence of Beta-Lapachone, in 20 μL of relaxation buffer (50 mM Tris (pH 7.5). 50 mM KCI, 10 mM MgCl2, 0.5 mM dithiothreitol, 0.5 mM EDTA, 30 μg/mL bovine serum albumin) for 30 minutes at 37 °C. Reactions are stopped by adding 1% SDS and proteinase K (50 μg/mL). After an additional 1-hour incubation at 37 °C, the products are separated by electrophoresis in 1% agarose gel in TAE buffer (0.04 M tris acetate, 0.001 M EDTA). The gel is stained with ethidium bromide after electrophoresis. The photographic negative is scanned with an NIH image analysis system.

Synonyms	Longifene, Buclina, Buclizine HCl, UCB-4445
Molecular Weight	505.95
Formula	C28H33ClN2·2HCl
CAS No.	129-74-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 11 mg/mL (21.74 mM), Sonification is recommended

References and Literature

1. Mostafa GA, et al. Profiles Drug Subst Excip Relat Methodol, 2011, 36:1-33.

Related compound libraries

This product is contained In the following compound libraries：

Inhibitor Library Drug Repurposing Compound Library Anti-Cancer Approved Drug Library Anti-Cancer Drug Library GPCR Compound Library Anti-Neurodegenerative Disease Compound Library Anti-Cancer Compound Library FDA-Approved & Pharmacopeia Drug Library Anti-Parkinson's Disease Compound Library Neurotransmitter Receptor Compound Library

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Keywords

Buclizine dihydrochloride 129-74-8 GPCR/G Protein Immunology/Inflammation Neuroscience 5-HT Receptor AChR Histamine Receptor teratogen Inhibitor MCF-7 anti-tumor activity antiallergic Longifene antihistamine inhibit Buclizine Dihydrochloride UCB 4445 Buclina Buclizine HCl UCB4445 UCB-4445 Buclizine inhibitor

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