产品说明书

Buclizine 2HCl

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Chemical Structure| 129-74-8 同义名 : 盐酸安其敏 ;Buclizine (hydrochloride);UCB-4445;NSC 25141;Buclizine HCl;Buclizine dihydrochloride
CAS号 : 129-74-8
货号 : A137542
分子式 : C28H35Cl3N2
纯度 : 97%
分子量 : 505.95
MDL号 : MFCD00242700
存储条件：

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
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：
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].
实验方案
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
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