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盐酸布克立嗪 /Buclizine 2HCl {[allProObj[0].p_purity_real_show]}

货号:A137542 同义名: 盐酸安其敏 / Buclizine (hydrochloride);UCB-4445

Buclizine 2HCl, the derivative of piperazine, is an antihistamine and anticholinergic agent.

Buclizine 2HCl 化学结构 CAS号:129-74-8
Buclizine 2HCl 化学结构
CAS号:129-74-8
Buclizine 2HCl 3D分子结构
CAS号:129-74-8
Buclizine 2HCl 化学结构 CAS号:129-74-8
Buclizine 2HCl 3D分子结构 CAS号:129-74-8
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Buclizine 2HCl 纯度/质量文件 产品仅供科研

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更多 >
产品名称 H1 receptor H2 receptor H3 receptor H4 receptor Histamine receptor 其他靶点 纯度
Hydroxyzine 2HCl 99+%
Cyclizine 97%
Loratadine +

B(0)AT2, IC50: 4 μM

98%
Desloratadine ++

Histamine H1 receptor, IC50: 51 nM

98%
Doxylamine succinate 99%
Ebastine 98%
Tripelennamine HCl +

H1 receptor, IC50: 30 μM

98%
Meclizine dihydrochloride 98%
Chlorpheniramine maleate +++

Histamine H1 receptor, IC50: 12 nM

99%
Diphenhydramine HCl 99%
Alcaftadine ++++

H1 receptor, pKi: 8.5

++

H2 receptor, pKi: 7.2

99%+
Fexofenadine HCl ++

Histamine H1 receptor, IC50: 246 nM

99%+
Bilastine +++

H1 receptor, Ki: 44.15 nM

98%
Pemirolast potassium 98%
Bepotastine besilate +

Histamine H1 receptor, pIC50: 5.7

98%
Mizolastine +++

Histamine H1 receptor, IC50: 47 nM

98%
Brompheniramine maleate 98%
Carbinoxamine maleate salt 99+%
Clemastine fumarate ++++

Histamine H1 receptor, IC50: 3 nM

98%
Ketotifen fumarate salt 95%
Rupatadine Fumarate ++

Histamine H1 receptor, Ki: 102 nM

PAFR 98%
Famotidine 97%
Roxatidine Acetate HCl +

Histamine H2 receptor, IC50: 3.2 μM

98%
Lafutidine 99%
Cimetidine 98%
Nizatidine ++++

Histamine H2 receptor, IC50: 0.9 nM

AChE 98%
Ranitidine 98%
Betahistine +

Histamine H3 receptor, IC50: 1.9 μM

98%
Ciproxifan maleate +++

Histamine H3 receptor, IC50: 9.2 nM

99%+
S 38093 ++

human H3 receptor, Ki: 1.2 μM

rat H3 receptor, Ki: 1.44 μM

98%
JNJ-7777120 ++++

Histamine H4 receptor, Ki: 4.5 nM

98%
Azelastine HCl 98%
Epinastine HCl 98%
Levodropropizine 97%
Cyproheptadine hydrochloride 98%
Hesperetin 97%
Olopatadine HCl 98%
Mianserin hydrochloride 99+%
Buclizine 2HCl 97%
Latrepirdine 2HCl GluR 98%
Cetirizine 2HCl 98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Buclizine 2HCl 生物活性

靶点
  • Histamine receptor

描述 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. It also possesses anticholinergic, antihistaminic, central nervous system depressant, and local anesthetic effects[3]. Moreover, levomepromazine and buclizine inhibited cancer cell growth by binding to TCTP (Translationally controlled tumor protein) and induction of cell differentiation. Buclizine (0 - 100 μM, 72 h) inhibits cancer cell growth by binding to TCTP and induction of cell differentiation[4]. Buclizine dihydrochloride is a potent teratogen in the rat. Buclizine dihydrochloride (≥40 mg/kg) exhibits teratogenic effect[5]. Buclizine dihydrochloride exhibits the t1/2 of ~10h via oral administration[6].

Buclizine 2HCl 参考文献

[1]Mostafa GA, Al-Badr AA. Buclizine. Profiles Drug Subst Excip Relat Methodol. 2011;36:1-33. doi: 10.1016/B978-0-12-387667-6.00001-4.

[2]Burgess HA, Merrington DM, et al. The relative bioavailability of paracetamol after rectal administration of suppositories containing a mixture of paracetamol, codeine phosphate and buclizine hydrochloride in healthy volunteers. Curr Med Res Opin. 1985;9(9):634-41.

[3]Mostafa GA, Al-Badr AA. Buclizine. Profiles Drug Subst Excip Relat Methodol. 2011;36:1-33

[4]Seo EJ, Efferth T. 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

[5]King CT, Howell J. 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

[6]Simultaneous determination of antihistamine anti-allergic drugs, cetirizine, domperidone, chlorphenamine maleate, loratadine, meclizine and buclizine in pharmaceutical formulations, human serum and pharmacokinetics application

Buclizine 2HCl 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.98mL

0.40mL

0.20mL

9.88mL

1.98mL

0.99mL

19.76mL

3.95mL

1.98mL

Buclizine 2HCl 技术信息

CAS号129-74-8
分子式C28H35Cl3N2
分子量 505.95
别名 盐酸安其敏 ;Buclizine (hydrochloride);UCB-4445;NSC 25141;Buclizine HCl;Buclizine dihydrochloride
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,Room Temperature

溶解度

DMSO: 2 mg/mL(3.95 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
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