马来酸吡拉明

马来酸吡拉明用途

Mepyramine maleate 是第一代抗组胺剂,为 histamine H1 受体拮抗剂,对 H1,H2 和 H3 受体的 Kd 值分别为 0.8 nM,5200 nM 和 >3000 nM,对 H1 受体的 pKd 值为 9.4。

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马来酸吡拉明名称

[ CAS 号 ]:
59-33-6

[ 中文名 ]:
吡拉明马来酸盐

[ 英文名 ]:
Pyrilamine Maleate Salt

[中文别名 ]:

[英文别名 ]:

EINECS 200-422-7
pyrilamine maleate
MFCD00069333
Mepyramine maleate

马来酸吡拉明生物活性

[ 描述 ]:

Mepyramine maleate 是第一代抗组胺剂,为 histamine H1 受体拮抗剂,对 H1,H2 和 H3 受体的 Kd 值分别为 0.8 nM,5200 nM 和 >3000 nM,对 H1 受体的 pKd 值为 9.4。

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 组胺受体

信号通路 >> 免疫及炎症 >> 组胺受体

研究领域 >> 神经疾病

[ 靶点 ]

Kd: 0.8 nM (Histamine H1 receptor), 5200 nM (Histamine H2 receptor), >3000 nM (Histamine H3 receptor)[1] pKd: 9.4 (Histamine H1 receptor)[2]

[体外研究]

马来酸美吡拉敏是组胺H1受体的拮抗剂,H1,H2和H3受体的Kds分别为0.8 nM,5200 nM和> 3000 nM [1],H1受体的pKd为9.4 [2]。美吡拉敏与豚鼠脑(0.8 nM),大鼠脑(9.1 nM)和DDT1-MF-2和BC3H1细胞(276 nM)中不同Kds的H1受体结合[1]。美吡拉敏降低CHO-gpH1细胞中的InsP水平,log EC50为-7.94±0.11,并降低CHO-gpH1细胞对ATP的最大反应[3]。

[体内研究]

美吡拉敏通过腹腔注射10和20 mg/kg明显降低伤害性反应的第二阶段,但对大鼠5 mg/kg无显着影响[4]。

[细胞实验]

简而言之，将细胞接种在24孔簇培养皿中并在DMEM中培养24小时（70-80％汇合）。然后洗涤细胞，并将培养基更换为不含小牛血清的DMEM加上myo- [3H]肌醇（2μCi/ mL）并培养24小时。此后，吸出培养基并用不含有10mM LiCl的小牛血清的DMEM替换，并孵育20分钟。然后在存在或不存在[3H]肌醇的情况下，在每个特定实验中指示的浓度下，用浓度范围为1nM至100μM的最终体积300μL的组胺刺激细胞20分钟。通过加入900μL冷氯仿，甲醇，0.12M HCl（1：2：1v / v，新制备）来终止温育，并通过添加300μL水和300μL氯仿来分离各相。。然后将混合物以1500×g离心10分钟，并通过阴离子交换色谱法纯化总的水溶性肌醇磷酸酯级分。使用液体闪烁计数器测量洗脱级分的放射性。结果表示为当总[3H]肌醇磷酸盐放射性标准化为从柱的初始水洗中回收的总[3H]肌醇放射性时获得的比例[3]。

[动物实验]

大鼠[4]将体重为200-220g的健康成年雄性白化Wistar大鼠保持在聚丙烯笼中，每个笼中有6只大鼠，随意提供食物和水。美吡拉敏溶于正常的saine。剂量为5,10和20mg / kg的美吡拉敏，并在诱导伤害感受前30分钟腹膜内注射。在诱导福尔马林诱导的疼痛之前20和40分钟分别皮下施用剂量为0.05,0.1和0.2mg / kg的毒扁豆碱和剂量为2mg / kg的阿托品。在皮下注射毒扁豆碱（0.1mg / kg）之前20分钟注射阿托品（2mg / kg，sc）。在联合治疗中，在毒扁豆碱（0.1mg / kg，sc）给药前10分钟和阿托品（0.2mg / kg，sc）给药后10分钟腹膜内注射美吡拉敏（10mg / kg）和法莫替丁（20mg / kg）。。使用25号注射针以1mL / kg的体积腹膜内注射药物溶液。使用27号注射针在颈部区域以每只大鼠0.2mL的体积注射药物溶液进行皮下注射[4]。

[参考文献]

[1]. Hill SJ. Distribution, properties, and functional characteristics of three classes of histamine receptor. Pharmacol Rev. 1990 Mar;42(1):45-83.

[2]. van der Goot H1, et al. Selective ligands as tools to study histamine receptors. Eur J Med Chem. 2000 Jan;35(1):5-20.

[3]. Fitzsimons CP, et al. Mepyramine, a histamine H1 receptor inverse agonist, binds preferentially to a G protein-coupled form of the receptor and sequesters G protein. J Biol Chem. 2004 Aug 13;279(33):34431-9.

[4]. Mojtahedin A, et al. Effects of mepyramine and famotidine on the physostigmine-induced antinociception in the formalin test in rats. Pak J Biol Sci. 2008 Nov 15;11(22):2573-8.

[相关活性小分子]

马来酸吡拉明物理化学性质

[ 沸点 ]:
423.8ºC at 760 mmHg

[ 熔点 ]:
100-101ºC

[ 分子式 ]:
C₂₁H₂₇N₃O₅

[ 分子量 ]:
401.45600

[ 闪点 ]:
210.1ºC

[ 精确质量 ]:
401.19500

[ PSA ]:
103.20000

[ LogP ]:
2.37020

[ 外观性状 ]:
白色结晶粉末

[ 储存条件 ]:
2-8°C

[ 稳定性 ]:
Stability Combustible. Incompatible with strong oxidizing agents.

[ 水溶解性 ]:
水溶性：可溶

马来酸吡拉明MSDS

详细MSDS(安全技术说明书)

马来酸吡拉明毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: UT1225000

CAS REGISTRY NUMBER :: 59-33-6

LAST UPDATED :: 199701

DATA ITEMS CITED :: 24

MOLECULAR FORMULA :: C17-H23-N3-O.C4-H4-O4

MOLECULAR WEIGHT :: 401.51

WISWESSER LINE NOTATION :: T6NJ BN1R DO1&2N1&1 &OV1U1VO

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - child

DOSE/DURATION :: 42 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - acute pulmonary edema Gastrointestinal - nausea or vomiting

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 200 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Cardiac - other changes Vascular - BP elevation not characterized in autonomic section

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 513 mg/kg

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

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 150 mg/kg

TOXIC EFFECTS :: Behavioral - tremor

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 220 mg/kg

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

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 100 mg/kg

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

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 141 mg/kg

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

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 23 mg/kg

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

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - guinea pig

DOSE/DURATION :: 44 mg/kg

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

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - guinea pig

DOSE/DURATION :: 24400 ug/kg

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

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 8766 gm/kg/90D-C

TOXIC EFFECTS :: Liver - changes in liver weight Nutritional and Gross Metabolic - weight loss or decreased weight gain Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - transaminases

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 7378 mg/kg/14D-C

TOXIC EFFECTS :: Gastrointestinal - changes in structure or function of salivary glands

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 91 gm/kg/90D-C

TOXIC EFFECTS :: Cardiac - changes in heart weight Kidney, Ureter, Bladder - changes in bladder weight Nutritional and Gross Metabolic - weight loss or decreased weight gain

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 77 gm/kg/2Y-C

TOXIC EFFECTS :: Tumorigenic - equivocal tumorigenic agent by RTECS criteria Liver - tumors

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 100 mg/kg

SEX/DURATION :: female 1 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intramuscular

DOSE :: 50 mg/kg

SEX/DURATION :: female 1 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 4200 mg/kg

SEX/DURATION :: female 1-21 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Newborn - stillbirth Reproductive - Effects on Newborn - viability index (e.g., # alive at day 4 per # born alive)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 420 mg/kg

SEX/DURATION :: female 1-21 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Newborn - weaning or lactation index (e.g., # alive at weaning per # alive at day 4)

MUTATION DATA

TYPE OF TEST :: Mutation in microorganisms

TEST SYSTEM :: Rodent - mouse Lymphocyte

DOSE/DURATION :: 400 mg/L

REFERENCE :: MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1964- Volume(issue)/page/year: 189,285,1987 *** REVIEWS *** TOXICOLOGY REVIEW JRPMAP Journal of Reproductive Medicine. (2 Jacklynn Ct., St. Louis, MO 63132) V.3- 1969- Volume(issue)/page/year: 12,27,1974 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOHS - National Occupational Hazard Survey (1974) NOHS Hazard Code - 80498 No. of Facilities: 1580 (estimated) No. of Industries: 3 No. of Occupations: 9 No. of Employees: 6126 (estimated) NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - 80498 No. of Facilities: 342 (estimated) No. of Industries: 3 No. of Occupations: 13 No. of Employees: 3505 (estimated) No. of Female Employees: 1579 (estimated)

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马来酸吡拉明安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302-H315-H319-H335

[ 警示性声明 ]:
P261-P305 + P351 + P338

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Gloves

[ 危害码 (欧洲) ]:
Xn: Harmful;

[ 风险声明 (欧洲) ]:
R22;R36/37/38

[ 安全声明 (欧洲) ]:
S26-S36/37

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
3

[ RTECS号 ]:
UT1225000

[ 海关编码 ]:
2933399090

马来酸吡拉明海关

[ 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%

马来酸吡拉明文献

Salt effects in electromembrane extraction.

J. Chromatogr. A. 1347 , 1-7, (2014)

Electromembrane extraction (EME) was performed on samples containing substantial amounts of NaCl to investigate how the presence of salts affected the recovery, repeatability, and membrane current in ...

Olodaterol attenuates citric acid-induced cough in naïve and ovalbumin-sensitized and challenged guinea pigs.

PLoS ONE 10(3) , e0119953, (2015)

Excessive coughing is a common feature of airway diseases. Different G-protein coupled receptors, including β2-adrenergic receptors (β2-AR), have been implicated in the molecular mechanisms underlying...

Involvement of H1 and H2 receptors and soluble guanylate cyclase in histamine-induced relaxation of rat mesenteric collecting lymphatics.

Microcirculation 21(7) , 593-605, (2014)

This study investigated the roles of the H1 and H2 histamine receptors, NO synthase, and sGC cyclase in histamine-induced modulation of rat mesenteric collecting lymphatic pumping.Isolated rat mesente...

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