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盐酸安其敏

盐酸安其敏用途

Buclizine dihydrochloride 是具有口服活性的抗组胺、抗过敏化合物。Buclizine dihydrochloride 对大鼠是一种强效的致畸剂。

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盐酸安其敏名称

[ CAS 号 ]:
129-74-8

[ 中文名 ]:
盐酸安其敏

[ 英文名 ]:
Buclizine dihydrochloride

[中文别名 ]:

盐酸布可立嗪

[英文别名 ]:

Posdel
MFCD00242700
Buclina
Postafen
BUCLIZINE, DIHYDROCHLORIDE
buclizine hydrochloride
buclizine dihydrochloride
Longifene

盐酸安其敏生物活性

[ 描述 ]:

Buclizine dihydrochloride 是具有口服活性的抗组胺、抗过敏化合物。Buclizine dihydrochloride 对大鼠是一种强效的致畸剂。

[ 相关类别 ]:

研究领域 >> 癌症

信号通路 >> 免疫及炎症 >> 组胺受体

研究领域 >> 炎症/免疫

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 组胺受体

[体外研究]

布加勒辛(0-100μM,72h)通过与TCTP结合和诱导细胞分化抑制癌细胞生长[3]。细胞增殖试验[3]。细胞系：MCF-7细胞[3]。孵育时间：18.0±50.0μM。

[体内研究]

盐酸布利嗪(≥40mg/kg)具有致畸作用[1]。盐酸布利嗪经口给药表现出~10小时的t1/2[2]。动物模型：成年雌性大鼠87只,体重240±20克[1]。剂量：30-200mg/kg。给药：从第10天到第15天。结果：当≥40mg/kg时,其致畸作用呈剂量依赖性。

[参考文献]

[1]. 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.

[2]. Nawab Sher, et al. Simultaneous determination of antihistamine anti-allergic drugs, cetirizine, domperidone, chlorphenamine maleate, loratadine, meclizine and buclizine in pharmaceutical formulations, human serum and pharmacokinetics application. Analytical methods • March 2014.

[3]. 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.

盐酸安其敏物理化学性质

[ 沸点 ]:
520.1ºC at 760 mmHg

[ 熔点 ]:
230-240ºC

[ 分子式 ]:
C₂₈H₃₅Cl₃N₂

[ 分子量 ]:
505.950

[ 闪点 ]:
268.3ºC

[ 精确质量 ]:
504.186584

[ PSA ]:
6.48000

[ LogP ]:
8.02450

[ 外观性状 ]:
灰白色粉末

[ 蒸汽压 ]:
6.44E-11mmHg at 25°C

[ 储存条件 ]:
库房通风低温干燥

盐酸安其敏毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: TL0280000

CHEMICAL NAME :: Piperazine, 1-(p-tert-butylbenzyl)-4-(p-chloro-alpha-phenylbenzyl )-, dihydrochloride

CAS REGISTRY NUMBER :: 129-74-8

LAST UPDATED :: 199701

DATA ITEMS CITED :: 4

MOLECULAR FORMULA :: C28-H33-Cl-N2.2Cl-H

MOLECULAR WEIGHT :: 506.00

WISWESSER LINE NOTATION :: T6N DNTJ AYR&R DG& D1R DX1&1&1 &GH 2

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 2100 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Behavioral - excitement Lungs, Thorax, or Respiration - other changes

REFERENCE :: JAPMA8 Journal of the American Pharmaceutical Association, Scientific Edition. (Washington, DC) V.29-49, 1940-60. For publisher information, see JPMSAE. Volume(issue)/page/year: 43,653,1954

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 430 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Behavioral - excitement Lungs, Thorax, or Respiration - other changes

REFERENCE :: JAPMA8 Journal of the American Pharmaceutical Association, Scientific Edition. (Washington, DC) V.29-49, 1940-60. For publisher information, see JPMSAE. Volume(issue)/page/year: 43,653,1954 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 360 mg/kg

SEX/DURATION :: female 10-15 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - craniofacial (including nose and tongue) Reproductive - Specific Developmental Abnormalities - musculoskeletal system

REFERENCE :: AJOGAH American Journal of Obstetrics and Gynecology. (C.V. Mosby Co., 11830 Westline Industrial Dr., St. Louis, MO 63146) V.1- 1920- Volume(issue)/page/year: 95,109,1966