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盐酸曲普利啶

盐酸曲普利啶用途

盐酸曲普利啶是一种口服活性、细胞渗透性和第一代组胺H1拮抗剂[1]。盐酸曲普利啶是一种抗组胺药,可用于过敏性鼻炎、哮喘和荨麻疹[2]。

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盐酸曲普利啶名称

[ CAS 号 ]:
6138-79-0

[ 中文名 ]:
盐酸曲普利啶

[ 英文名 ]:
Triprolidine hydrochloride

[英文别名 ]:

MFCD00150574
Triprolidine hydrochloride

盐酸曲普利啶生物活性

[ 描述 ]:

盐酸曲普利啶是一种口服活性、细胞渗透性和第一代组胺H1拮抗剂[1]。盐酸曲普利啶是一种抗组胺药,可用于过敏性鼻炎、哮喘和荨麻疹[2]。

[ 相关类别 ]:

信号通路 >> 免疫及炎症 >> 组胺受体

研究领域 >> 神经疾病

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 组胺受体

[ 靶点 ]

H1 Receptor

[体内研究]

曲普利啶(间隔内注射；0.5μl中0.5μM；破伤风后30、60和180 min)对基线fEPSPs没有显著影响,但是,与盐水注射(60 min时为208%)相比,步行时诱导的长时程增强(LTP)较小(60 min时为基线值的173%)[2]。动物模型：成年雄性Long-Evans TMN(tuberomamillary nucleus,TMN)损伤大鼠[2]剂量：0.5μl给药0.5μm：间隔内灌注；破伤风后30、60、180min结果：LTP的步行相关增强减弱。

[参考文献]

[1]. Tao Luo, et al. Endogenous Histamine Facilitates Long-Term Potentiation in the Hippocampus During WalkingJ Neurosci. 2010 Jun 9;30(23):7845-52.

[2]. Sang-Chul Shin, et al. Controlled Release of Triprolidine Using Ethylene-Vinyl Acetate Membrane and Matrix Systems. Eur J Pharm Biopharm

盐酸曲普利啶物理化学性质

[ 沸点 ]:
462ºC at 760 mmHg

[ 熔点 ]:
115-120ºC

[ 分子式 ]:
C₁₉H₂₅ClN₂O

[ 分子量 ]:
314.85200

[ 闪点 ]:
233.2ºC

[ 精确质量 ]:
314.15500

[ PSA ]:
16.13000

[ LogP ]:
4.65740

[ 外观性状 ]:
白色结晶粉末

[ 储存条件 ]:
2-8°C

[ 稳定性 ]:
Stable, but discolours in light. Incompatible with strong oxidizing agents.

[ 水溶解性 ]:
>=10 g/100 mL at 20 ºC

盐酸曲普利啶MSDS

详细MSDS(安全技术说明书)

盐酸曲普利啶毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: UT7658000

CHEMICAL NAME :: Pyridine, 2-(3-(1-pyrrolidinyl)-1-p-tolylpropenyl)-, monohydrochloride, monohydrate, stereoisomer

CAS REGISTRY NUMBER :: 6138-79-0

LAST UPDATED :: 199803

DATA ITEMS CITED :: 6

MOLECULAR FORMULA :: C19-H22-N2.Cl-H.H2-O

MOLECULAR WEIGHT :: 332.91

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 840 mg/kg

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

REFERENCE :: NCTR** National Center for Toxicology Research Technical Report. Office of Associate Director for Scientific Coordination, Jefferson, Arkansas 72079 Volume(issue)/page/year: #414/415,1991

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 163 mg/kg

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

REFERENCE :: NCTR** National Center for Toxicology Research Technical Report. Office of Associate Director for Scientific Coordination, Jefferson, Arkansas 72079 Volume(issue)/page/year: #414/415,1991 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 10760 mg/kg/90D-I

TOXIC EFFECTS :: Cardiac - changes in heart weight Gastrointestinal - changes in structure or function of salivary glands Blood - changes in leukocyte (WBC) count

REFERENCE :: JACTDZ Journal of the American College of Toxicology. (Mary Ann Liebert, Inc., 1651 Third Ave., New York, NY 10128) V.1-12, 1982-1993. Discontinued. Volume(issue)/page/year: 12,359,1993

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 103 gm/kg/2Y-C

TOXIC EFFECTS :: Liver - changes in liver weight Endocrine - changes in spleen weight Nutritional and Gross Metabolic - weight loss or decreased weight gain

REFERENCE :: FAATDF Fundamental and Applied Toxicology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1981- Volume(issue)/page/year: 27,223,1995

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 175 gm/kg/2Y-C

TOXIC EFFECTS :: Liver - other changes Liver - changes in liver weight Nutritional and Gross Metabolic - weight loss or decreased weight gain

REFERENCE :: NCTR** National Center for Toxicology Research Technical Report. Office of Associate Director for Scientific Coordination, Jefferson, Arkansas 72079 Volume(issue)/page/year: #414/415,1991 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X2762 No. of Facilities: 269 (estimated) No. of Industries: 1 No. of Occupations: 4 No. of Employees: 4419 (estimated) No. of Female Employees: 2546 (estimated)

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盐酸曲普利啶安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302-H315-H319-H335

[ 警示性声明 ]:
P301 + P312 + P330-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

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

[ WGK德国 ]:
3

[ RTECS号 ]:
UT7658000

盐酸曲普利啶文献

Involvement of histaminergic inputs in the jaw-closing reflex arc.

J. Neurophysiol. 113 , 3720-35, (2015)

Histamine receptors are densely expressed in the mesencephalic trigeminal nucleus (MesV) and trigeminal motor nucleus. However, little is known about the functional roles of neuronal histamine in cont...

Development and validation of an ultra-performance liquid chromatography method for simultaneous analysis of 20 antihistaminics in dietary supplements.

Biomed. Chromatogr. 29(3) , 465-74, (2015)

The purpose of this study was to develop and validate an ultra-performance liquid chromatography method for simultaneous analysis of 20 antihistamines (illegal additives) in dietary supplements. The l...

Quantification of antihistamine acrivastine in plasma by solid-phase extraction and high-performance liquid chromatography.

J. Pharm. Biomed. Anal. 43(1) , 293-7, (2007)

An automated solid-phase extraction method was developed for the determination of the H1-antihistamine acrivastine in plasma samples. Acrivastine was analyzed at the wavelength of 254 nm using a rever...

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