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非尼拉敏

非尼拉敏用途

苯尼拉明是第一代组胺H1受体拮抗剂,作用于中枢神经系统(CNS),具有镇静和催眠作用。苯尼拉明具有抗肿瘤作用并诱导白血病细胞凋亡。苯尼拉明也是一种安全有效的局部麻醉药,具有止痒作用[1][2][3][4]。

非尼拉敏名称

[ CAS 号 ]:
86-21-5

[ 中文名 ]:
非尼拉敏

[ 英文名 ]:
Pheniramine

[中文别名 ]:

[英文别名 ]:

Histapyridamine
Avil
Propheniramine
Feniramine
pheniramine
EINECS 201-656-2
Trimeton
Prophenpyridamine
Pyriton
Tripoton

非尼拉敏生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 细胞凋亡 >> 细胞凋亡

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

[ 靶点 ]

H1 Receptor:1.01 mM (IC50)

[体外研究]

苯尼拉明抑制CYP2D6(特异性P450同工酶),以延迟代谢时间并延长抗组织胺作用[1]。苯尼拉明通过抑制IC50值为1.01 mM的组胺抑制Ca2+流入BC3H-1细胞,并调节细胞Ca2+跨膜作用[2]。苯尼拉明(0.5,1.0 mM；24小时)诱导人T细胞急性淋巴细胞白血病细胞株的细胞凋亡[3]。苯尼拉明(1μM-1 mM；12-48 h)以时间依赖性方式抑制细胞增殖,其抑制浓度IC50s分别为550μM(CCRF-CEM细胞)和420μM的(Jurkat细胞)[3]。细胞凋亡分析[3]细胞株：人T细胞急性淋巴细胞白血病细胞株：CCRF-CEM和Jurkat ALL浓度：0.5,1.0 mM培养时间：24小时结果：诱导细胞凋亡,染色质浓缩并边缘化,核碎片扩散到细胞质中。细胞活性测定[3]细胞株：人T细胞急性淋巴细胞白血病细胞株：CCRF-CEM和Jurkat ALL浓度：1μM-1 mM培养时间：12、24、48小时结果：以时间和剂量依赖性方式抑制细胞增殖和存活。

[体内研究]

芬尼拉明(1.75μM；i.t.)对大鼠产生局部麻醉作用并导致脊髓阻滞[4]。动物模型：Sprague–Dawley大鼠(300-350 g；雄性)[4]剂量：0.30、0.60、0.90、1.50、1.75μM给药：鞘内注射；一次性结果：造成脊髓阻滞,并显示剂量依赖性效应。在1.75μM时,运动功能、本体感觉和伤害感受被100%阻断,动作完全恢复时间分别为41、56和88分钟。

[参考文献]

[1]. Sharma A, et al. Classic histamine H1 receptor antagonists: a critical review of their metabolic and pharmacokinetic fate from a bird's eye view. Curr Drug Metab. 2003 Apr;4(2):105-29.

[2]. Brown RD, et al. Alpha 1-adrenergic and H1-histamine receptor control of intracellular Ca2+ in a muscle cell line: the influence of prior agonist exposure on receptor responsiveness. Mol Pharmacol. 1986 Jun;29(6):531-9.

[3]. Jangi SM, et al. Apoptosis of human T-cell acute lymphoblastic leukemia cells by diphenhydramine, an H1 histamine receptor antagonist. Oncol Res. 2004;14(7-8):363-72.

[4]. Hung CH, et al. Spinal anesthesia with diphenhydramine and pheniramine in rats. Eur J Pharmacol. 2011 Dec 30;673(1-3):20-4.

非尼拉敏物理化学性质

[ 密度 ]:
1.018 g/cm3

[ 沸点 ]:
84 °C20 mm Hg(lit.)

[ 熔点 ]:
30-34 °C(lit.)

[ 分子式 ]:
C₁₆H₂₀N₂

[ 分子量 ]:
240.34300

[ 闪点 ]:
179 °F

[ 精确质量 ]:
240.16300

[ PSA ]:
16.13000

[ LogP ]:
3.16520

[ 折射率 ]:
1.556

[ 储存条件 ]:
?20°C

非尼拉敏MSDS

详细MSDS(安全技术说明书)

非尼拉敏毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: US9625000

CHEMICAL NAME :: Pyridine, 2-(alpha-(2-(dimethylamino)ethyl)benzyl)-

CAS REGISTRY NUMBER :: 86-21-5

BEILSTEIN REFERENCE NO. :: 0192445

LAST UPDATED :: 199612

DATA ITEMS CITED :: 4

MOLECULAR FORMULA :: C16-H20-N2

MOLECULAR WEIGHT :: 240.38

WISWESSER LINE NOTATION :: T6NJ BYR&2N1&1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 14 mg/kg

TOXIC EFFECTS :: Behavioral - hallucinations, distorted perceptions Behavioral - muscle contraction or spasticity

REFERENCE :: MJAUAJ Medical Journal of Australia. (Australasian Medical Pub. Co. Ltd., 71-79 Arundel St., Glebe, N.S.W., Australia) V.1- 1914- Volume(issue)/page/year: 2,110,1976

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 48 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: AEPPAE Naunyn-Schmiedeberg's Archiv fuer Experimentelle Pathologie und Pharmakologie. (Berlin, Ger.) V.110-253, 1925-66. For publisher information, see NSAPCC. Volume(issue)/page/year: 211,328,1950

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 30 mg/kg

TOXIC EFFECTS :: Lungs, Thorax, or Respiration - other changes Endocrine - hyperglycemia Nutritional and Gross Metabolic - body temperature decrease

REFERENCE :: AEPPAE Naunyn-Schmiedeberg's Archiv fuer Experimentelle Pathologie und Pharmakologie. (Berlin, Ger.) V.110-253, 1925-66. For publisher information, see NSAPCC. Volume(issue)/page/year: 211,328,1950 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOHS - National Occupational Hazard Survey (1974) NOHS Hazard Code - 81485 No. of Facilities: 805 (estimated) No. of Industries: 1 No. of Occupations: 1 No. of Employees: 805 (estimated)

非尼拉敏安全信息

[ 符号 ]:

GHS02, GHS06, GHS08

[ 信号词 ]:
Danger

[ 危害声明 ]:
H225-H301 + H311 + H331-H370

[ 警示性声明 ]:
P210-P260-P280-P301 + P310-P311

[ 危害码 (欧洲) ]:
Xi

[ 风险声明 (欧洲) ]:
R36/37/38:Irritating to eyes, respiratory system and skin .

[ 安全声明 (欧洲) ]:
S26-S36/37/39

[ 危险品运输编码 ]:
1759

[ WGK德国 ]:
3

[ 包装等级 ]:
III

[ 危险类别 ]:
8

[ 海关编码 ]:
2933399090

非尼拉敏合成路线

详细合成路线

非尼拉敏上下游产品

非尼拉敏上游产品

非尼拉敏下游产品

非尼拉敏海关

[ 海关编码 ]: 2933399090

[ 中文概述 ]:
2933399090. 其他结构含非稠合吡啶环的化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期

[ Summary ]:
2933399090. other compounds containing an unfused pyridine ring (whether or not hydrogenated) in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

非尼拉敏文献

Assessment of protective effects of methylprednisolone and pheniramine maleate on reperfusion injury in kidney after distant organ ischemia: a rat model.

Ann. Vasc. Surg. 26(4) , 559-65, (2012)

Ischemia/reperfusion (I/R) injury of tissues is a common problem that cardiovascular surgeons are faced with. Suppression of inflammation, which plays an important role in the pathogenesis of I/R inju...

Artificial neural network combined with principal component analysis for resolution of complex pharmaceutical formulations.

Chem. Pharm. Bull. 59(1) , 35-40, (2011)

A chemometric approach based on the combined use of the principal component analysis (PCA) and artificial neural network (ANN) was developed for the multicomponent determination of caffeine (CAF), mep...

C7a, a biphosphinic cyclopalladated compound, efficiently controls the development of a patient-derived xenograft model of adult T cell leukemia/lymphoma.

Viruses 3(7) , 1041-58, (2011)

Adult T-cell leukemia/lymphoma (ATLL) is a highly aggressive disease that occurs in individuals infected with the human T lymphotropic virus type 1 (HTLV-1). Patients with aggressive ATLL have a poor ...

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