< 生产厂家价格 >

苯噻啶

苯噻啶用途

Pizotifen 是 5-HT2 受体的有效拮抗剂,并对 5-HT1C 有高亲和力。

点击显示

苯噻啶名称

[ CAS 号 ]:
15574-96-6

[ 中文名 ]:
苯噻啶

[ 英文名 ]:
Pizotifen

[中文别名 ]:

新度美安

[英文别名 ]:

UNII:0BY8440V3N
Pizotyline
EINECS 239-632-9
Pizotifen
Sandomigran
MFCD00864192

苯噻啶生物活性

[ 描述 ]:

Pizotifen 是 5-HT2 受体的有效拮抗剂,并对 5-HT1C 有高亲和力。

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 5-HT受体

信号通路 >> 神经信号通路 >> 5-HT受体

研究领域 >> 神经疾病

[ 靶点 ]

5-HT2A Receptor

5-HT1C Receptor

[体外研究]

Pizotifen是一种有效的5-HT2受体拮抗剂,对5-HT1C结合位点具有高亲和力[1]。 Pizotifen是一种抗过敏的5-HT2A受体拮抗剂,具有抑制5-羟色胺增强的ADP诱导的血小板聚集的能力[2]。

[体内研究]

所有给药剂量的Pipethiadene和Pizotifen都显着降低了胎儿的体重;在0.6和1.2 mg/kg Pipethiadene之后,并且仅在中等剂量的Pizotifen之后,胎盘的重量显着减少。植入,活体,死胎,再吸收以及外部,骨骼和内脏异常的发生方式与对照组没有差异。处理小鼠的骨髓细胞中的染色体畸变数与阴性对照组没有显着差异。与对照组相比,微核试验显示微核的频率没有升高。在两种较高剂量的Pipethiadene和Pizotifen马来酸盐后,有丝分裂指数低于对照组[3]。

[参考文献]

[1]. Mylecharane EJ, et al. 5-HT2 receptor antagonists and migraine therapy. J Neurol. 1991;238 Suppl 1:S45-52.

[2]. Lin OA, et al. The antidepressant 5-HT2A receptor antagonists pizotifen and cyproheptadine inhibit serotonin-enhanced platelet function. PLoS One. 2014 Jan 23;9(1):e87026.

[3]. Ujházy E, et al. Teratological and cytogenetical evaluation of two antihistamines (pipethiadene and pizotifen maleate) in mice. Agents Actions. 1988 Apr;23(3-4):376-8.

[相关活性小分子]

苯噻啶物理化学性质

[ 密度 ]:
1.2±0.1 g/cm3

[ 沸点 ]:
436.7±45.0 °C at 760 mmHg

[ 熔点 ]:
140-142°C

[ 分子式 ]:
C₁₉H₂₁NS

[ 分子量 ]:
295.442

[ 闪点 ]:
217.9±28.7 °C

[ 精确质量 ]:
295.139465

[ PSA ]:
31.48000

[ LogP ]:
6.13

[ 外观性状 ]:
固体;White to Almost white powder to crystal

[ 蒸汽压 ]:
0.0±1.0 mmHg at 25°C

[ 折射率 ]:
1.631

[ 储存条件 ]:
Refrigerator

苯噻啶MSDS

详细MSDS(安全技术说明书)

苯噻啶毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: TM7165000

CHEMICAL NAME :: Piperidine, 4-(9,10-dihydro-4H-benzo(4,5)cyclohepta(1,2-b)thien-4 -ylidene)-1-methyl-

CAS REGISTRY NUMBER :: 15574-96-6

LAST UPDATED :: 199612

DATA ITEMS CITED :: 2

MOLECULAR FORMULA :: C19-H21-N-S

MOLECULAR WEIGHT :: 295.47

WISWESSER LINE NOTATION :: T C576 BY FS&T&J BU- DT6N DYTJ A1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 12857 ug/kg/12D-I

TOXIC EFFECTS :: Liver - jaundice, other or unclassified

REFERENCE :: AIMDAP Archives of Internal Medicine. (AMA, 535 N. Dearborn St., Chicago, IL 60610) V.1- 1908- Volume(issue)/page/year: 144,815,1984

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 410 mg/kg

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

REFERENCE :: PHMCAA Pharmacologist. (American Soc. for Pharmacology and Experimental Therapeutics, 9650 Rockville Pike, Bethesda, MD 20014) V.1- 1959- Volume(issue)/page/year: 12,297,1970

点击显示

苯噻啶安全信息

[ 符号 ]:

GHS07, GHS08

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302-H361

[ 警示性声明 ]:
P281

[ 危害码 (欧洲) ]:
Xi

[ 风险声明 (欧洲) ]:
36/37/38

[ 安全声明 (欧洲) ]:
26-37/39

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

[ RTECS号 ]:
TM7165000

苯噻啶文献

Method development for impurity profiling in SFC: The selection of a dissimilar set of stationary phases.

J. Pharm. Biomed. Anal. 111 , 333-43, (2015)

Supercritical fluid chromatography (SFC) is drawing considerable interest as separation technique in the pharmaceutical industry. The technique is already well established in chiral separations both a...

Efficacy of amitriptyline, pizotifen and propranolol in the prevention of migraine.

Mymensingh Med. J. 22(1) , 93-100, (2013)

This intervention study conducted in the Neurology outpatient Department of Mymensingh Medical College Hospital (MMCH) from January 2006 to December 2007 to compare efficacy of amitriptyline, pizotife...

Potential vascular alpha1-adrenoceptor blocking properties of an array of 5-HT receptor ligands in the rat.

Eur. J. Pharmacol. 535(1-3) , 234-42, (2006)

This study set out to analyse the potential ability of some 5-hydroxytryptamine (5-HT) receptor ligands widely used in cardiovascular experimental models to interact with vascular alpha1-adrenoceptors...

更多文献

苯噻啶