匹美噻吨马来酸盐

匹美噻吨马来酸盐用途

Pimethixene maleate 是抗组胺和抗血清素剂,用作抗偏头疼剂。Pimethixene maleate 为高效的多靶点拮抗剂,对 5-HT1A,5-HT2A,5-HT2B,5-HT2C,组胺 H1,多巴胺 D2 和 D4.4 以及毒蕈碱 M1 和 M2 的 pKi 值分别为 7.63,10.22,10.44,8.42,10.14,8.19,7.54,8.61 和 9.38。

匹美噻吨马来酸盐名称

[ CAS 号 ]:
13187-06-9

[ 中文名 ]:
匹美噻吨马来酸盐

[ 英文名 ]:
Pimethixene maleate

[中文别名 ]:

马来酸甲哌硫蒽

[英文别名 ]:

1-Methyl-4-(thioxanthen-9-ylidene)piperidine
PIMETHIXEN MALEATE SALT
9-(1-methyl-4-piperidylene)thioxanthenemaleate
9-(1-methyl-4-piperidylene)-thioxanthenmaleate
PIMETHIXENE MALEATE SALT
bp-400
9-(n-methyl-piperidyliden-4)thioxanemaleate
Pimethixene maleic salt
PIMETHIXENE MALEATE

匹美噻吨马来酸盐生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 神经信号通路 >> mAChR

信号通路 >> 免疫及炎症 >> 组胺受体

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 由mAChR

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 多巴胺受体

信号通路 >> 神经信号通路 >> 多巴胺受体

研究领域 >> 神经疾病

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 5-HT受体

信号通路 >> 神经信号通路 >> 5-HT受体

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 组胺受体

[ 靶点 ]

pKi: 7.63 (5-HT1A receptor), 10.22 (5-HT2A receptor), 10.44 (5-HT2B receptor), 8.42 (5-HT2C receptor), 10.14 (histamine H1 receptor), 8.19 (D2 receptor), 7.54 (DD4.4 receptor), 8.61 (M1 receptor), 9.38 (M2 receptor)[1]

[参考文献]

[1]. Schmitz B, et al. BF-1--a novel selective 5-HT2B receptor antagonist blocking neurogenic dural plasma protein extravasation in guinea pigs. Eur J Pharmacol. 2015 Mar 15;751:73-80.

匹美噻吨马来酸盐物理化学性质

[ 密度 ]:
1.192g/cm3

[ 沸点 ]:
439.7ºC at 760mmHg

[ 分子式 ]:
C₂₃H₂₃NO₄S

[ 分子量 ]:
409.50

[ 闪点 ]:
219.7ºC

[ 精确质量 ]:
409.13500

[ PSA ]:
103.14000

[ LogP ]:
4.32840

[ 蒸汽压 ]:
5.08E-17mmHg at 25°C

[ 储存条件 ]:
-20°C，密闭，干燥

匹美噻吨马来酸盐MSDS

详细MSDS(安全技术说明书)

匹美噻吨马来酸盐毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: XO0782000

CHEMICAL NAME :: Thioxanthene, 9-(1-methyl-4-piperidylene)-, maleate

CAS REGISTRY NUMBER :: 13187-06-9

LAST UPDATED :: 199709

DATA ITEMS CITED :: 6

MOLECULAR FORMULA :: C19-H19-N-S.C4-H4-O4

MOLECULAR WEIGHT :: 409.53

WISWESSER LINE NOTATION :: T C666 BS IYJ IU- DT6N DYTJ A1 &QV1U1VQ -C

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 :: 1186 mg/kg

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

REFERENCE :: ANAEA3 Annals of Allergy. (American College of Allergists, POB 20671, Bloomington, MN 55420) V.1- 1943- Volume(issue)/page/year: 21,233,1963

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 18 mg/kg

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

REFERENCE :: ANAEA3 Annals of Allergy. (American College of Allergists, POB 20671, Bloomington, MN 55420) V.1- 1943- Volume(issue)/page/year: 21,233,1963

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 433 mg/kg

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

REFERENCE :: ANAEA3 Annals of Allergy. (American College of Allergists, POB 20671, Bloomington, MN 55420) V.1- 1943- Volume(issue)/page/year: 21,233,1963

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 31400 ug/kg

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

REFERENCE :: ANAEA3 Annals of Allergy. (American College of Allergists, POB 20671, Bloomington, MN 55420) V.1- 1943- Volume(issue)/page/year: 21,233,1963

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 25 mg/kg

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

REFERENCE :: ANAEA3 Annals of Allergy. (American College of Allergists, POB 20671, Bloomington, MN 55420) V.1- 1943- Volume(issue)/page/year: 21,233,1963 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Unreported

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 9100 mg/kg/13W-I

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Related to Chronic Data - death

REFERENCE :: ANAEA3 Annals of Allergy. (American College of Allergists, POB 20671, Bloomington, MN 55420) V.1- 1943- Volume(issue)/page/year: 21,233,1963

匹美噻吨马来酸盐安全信息

[ 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) ]:
22-36/37/38

[ 安全声明 (欧洲) ]:
26-36

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

[ WGK德国 ]:
3

[ RTECS号 ]:
XO0782000

[ 海关编码 ]:
2934999090

匹美噻吨马来酸盐海关

[ 海关编码 ]: 2934999090

[ 中文概述 ]:
2934999090. 其他杂环化合物. 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

[ Summary ]:
2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%