129-74-8

• 常用中文名：盐酸安其敏
• 常用英文名：Buclizine dihydrochloride
• CAS号：129-74-8
• 分子式：C₂₈H₃₅Cl₃N₂
• 分子量：505.950
• 相关类别： 生物化工 抑制剂 神经信号通路(Neuronal Signaling) Histamine Receptor 抑制剂
• 发布时间：2018-07-16 18:22:13
• 更新时间：2024-01-08 10:31:13
• 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。

名称

• 中文名: 盐酸安其敏
• 英文名: anileridine dihydrochloride
• 中文别名: 盐酸布可立嗪; 布克立嗪/1-(对-叔丁苄基)-4-(对-氯代二苯甲基)哌嗪
• 英文别名: 1-(p-Chlorobenzhydryl)-4-(p-tert-butylbenzyl)piperazine dihydrochloride; Posdel; 1-(p-Chlorobenzhydryl)-4-(p-tert-butylbenzyl)diethylenediamine dihydrochloride; 1-(4-tert-Butylbenzyl)-4-[(4-chlorophenyl)(phenyl)methyl]piperazine dihydrochloride; MFCD00242700; Buclina; 1-(4-(tert-Butyl)benzyl)-4-((4-chlorophenyl)(phenyl)methyl)piperazine dihydrochloride; 1-(p-tert-Butylbenzyl)-4-(p-chloro-a-phenylbenzyl)piperazine Dihydrochloride; 1-[(4-Chlorophenyl)(phenyl)methyl]-4-[4-(2-methyl-2-propanyl)benzyl]piperazine dihydrochloride; Postafen; BUCLIZINE, DIHYDROCHLORIDE; buclizine hydrochloride; Piperazine, 1- (p-tert-butylbenzyl)-4-(p-chloro-α-phenylbenzyl)-, dihydrochloride; buclizine dihydrochloride; Longifene; Piperazine, 1-[(4-chlorophenyl)phenylmethyl]-4-[[4-(1,1-dimethylethyl)phenyl]methyl]-, hydrochloride (1:2); 1-(p-tert-Butylbenzyl)-4-(p-chloro-α-phenylbenzyl)piperazine dihydrochloride; Piperazine, 1-(p-tert-butylbenzyl)-4-(p-chloro-α-phenylbenzyl)-, dihydrochloride

物化性质

• 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
• 更多:

  1.熔点（℃）：230-240。

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.

毒性和生态

毒理学数据: 口服-小鼠 LD50: 2100 毫克/公斤; 腹腔-小鼠 LD50: 430 毫克/公斤。 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

安全

• 危害码 (欧洲): Xi