<生产厂家 价格>

美索哒嗪

美索哒嗪用途

中噻嗪(TPS-23)是噻嗪的代谢物(HY-B0965A),作为口服活性吩噻嗪类抗精神病药物。中瑞他嗪是人类乙醚-a-go-go相关基因(hERG)通道的有效且快速的开放通道阻断剂,在人类胚胎肾293细胞中以550nM(0 mV)的IC50阻断hERG电流[1]。美索里达嗪可用于精神分裂症以及某些其他精神疾病的研究[1][2]。

美索哒嗪名称

[ CAS 号 ]:
5588-33-0

[ 中文名 ]:
美索哒嗪

[ 英文名 ]:
Mesoridazine

[中文别名 ]:

[英文别名 ]:

美索哒嗪生物活性

[ 描述 ]:

中噻嗪(TPS-23)是噻嗪的代谢物(HY-B0965A),作为口服活性吩噻嗪类抗精神病药物。中瑞他嗪是人类乙醚-a-go-go相关基因(hERG)通道的有效且快速的开放通道阻断剂,在人类胚胎肾293细胞中以550nM(0 mV)的IC50阻断hERG电流[1]。美索里达嗪可用于精神分裂症以及某些其他精神疾病的研究[1][2]。

[ 相关类别 ]:

研究领域 >> 神经疾病
信号通路 >> 跨膜转运 >> 钾通道

[ 靶点 ]

IC50: hERG currents[1]


[体外研究]

中瑞他嗪以浓度依赖性的方式阻断人乙醚-a-go-go相关基因(HERG)电流(0 mV时IC50=550 nM),在HERG激活和饱和的电压范围内,阻断作用显著增加,导致最大HERG通道激活[1]。中硝嗪(15mM;24h)在裸鼠和猪皮中的总吸收率分别为15.94±4.04%和39.24±5.11%[3]。

[体内研究]

美索里达嗪(15mM;局部给药;一次或每天一次,连续7天)在阻断皮肤疼痛方面显示出有效的活性和长时间的镇痛[3]。在裸鼠背部局部施用6小时后,中硝嗪(15mM)显示皮内浓度为0.34 0.74 nmol/mg[3]。动物模型:8周龄雌性裸鼠[3]剂量:15mM给药:局部给药,一次(镇痛试验)或每天给药,连续7天(刺激试验)。结果:显示镇痛效果。观察到轻微的经表皮水分损失(TEWL)从7.8 g/m2/h增加到9.9 g/m2/h。

[参考文献]

[1]. Zhi Su, et al. Mesoridazine: an open-channel blocker of human ether-a-go-go-related gene K+ channel. J Mol Cell Cardiol. 2004 Jan;36(1):151-60.

[2]. I S M Salih, et al. Comparison of the effects of thioridazine and mesoridazine on the QT interval in healthy adults after single oral doses. Clin Pharmacol Ther. 2007 Nov;82(5):548-54.

[3]. Liu KS, et al. Topically applied mesoridazine exhibits the strongest cutaneous analgesia and minimized skin disruption among tricyclic antidepressants: The skin absorption assessment. Eur J Pharm Biopharm. 2016 Aug;105:59-68.

美索哒嗪物理化学性质

[ 密度 ]:
1.3g/cm3

[ 沸点 ]:
570.5ºC at 760mmHg

[ 分子式 ]:
C21H26N2OS2

[ 分子量 ]:
386.57400

[ 闪点 ]:
298.9ºC

[ 精确质量 ]:
386.14900

[ PSA ]:
68.06000

[ LogP ]:
5.76970

[ 折射率 ]:
1.694

美索哒嗪毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :
SP1880000
CHEMICAL NAME :
Phenothiazine, 10-(2-(1-methyl-2-piperidyl)ethyl)-2-(methylsulfinyl) -
CAS REGISTRY NUMBER :
5588-33-0
LAST UPDATED :
199512
DATA ITEMS CITED :
10
MOLECULAR FORMULA :
C21-H26-N2-O-S2
MOLECULAR WEIGHT :
386.61
WISWESSER LINE NOTATION :
T C666 BN ISJ ESO&1 B2- BT6NTJ A

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human - man
DOSE/DURATION :
86 mg/kg
TOXIC EFFECTS :
Cardiac - arrhythmias (including changes in conduction)
REFERENCE :
JCPYDR Journal of Clinical Pyschopharmacology. (Williams & Wilkins Co., 428 E. Preston St., Baltimore, MD 21202) V.1- 1981- Volume(issue)/page/year: 2,222,1982
TYPE OF TEST :
LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human
DOSE/DURATION :
42 mg/kg
TOXIC EFFECTS :
Vascular - regional or general arteriolar or venous dilation Lungs, Thorax, or Respiration - chronic pulmonary edema Blood - hemorrhage
REFERENCE :
ARGPAQ Archives of General Psychiatry. (AMA, 535 N. Dearborn St., Chicago,IL 60610) V.3- 1960- Volume(issue)/page/year: 34,955,1977
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
644 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 19,363,1971
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intramuscular
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
509 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 19,363,1971
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
560 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
27ZQAG "Psychotropic Drugs and Related Compounds," 2nd ed., Usdin, E., and D.H. Efron, Washington, DC, 1972 Volume(issue)/page/year: -,29,1972
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
26 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
27ZQAG "Psychotropic Drugs and Related Compounds," 2nd ed., Usdin, E., and D.H. Efron, Washington, DC, 1972 Volume(issue)/page/year: -,29,1972
TYPE OF TEST :
LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rabbit
DOSE/DURATION :
800 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 19,363,1971
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intramuscular
SPECIES OBSERVED :
Rodent - rabbit
DOSE/DURATION :
405 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 19,363,1971 ** OTHER MULTIPLE DOSE TOXICITY DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
60480 mg/kg/72W-I
TOXIC EFFECTS :
Brain and Coverings - recordings from specific areas of CNS Skin and Appendages - dermatitis, other (after systemic exposure) Related to Chronic Data - death
REFERENCE :
TXAPA9 Toxicology and Applied Pharmacology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1959- Volume(issue)/page/year: 19,363,1971 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X4738 No. of Facilities: 7 (estimated) No. of Industries: 1 No. of Occupations: 1 No. of Employees: 103 (estimated) No. of Female Employees: 52 (estimated)

美索哒嗪合成路线

美索哒嗪上下游产品

美索哒嗪上游产品

美索哒嗪下游产品

推荐生产厂家/供应商:

公司名:上海脉铂医药科技有限公司

区域:上海市嘉定区

价格:
¥2989.0/50mg ¥489.0/1g ¥789.0/10mg ¥需询单/1g

联系人:李先生

产品详情:Mesoridazine


公司名:上海创赛科技有限公司

区域:上海市嘉定区

价格:
¥2940.0/50mg ¥需询单/1ml ¥784.0/10mg

联系人:夏言

产品详情:Mesoridazine


公司名:上海陌孚医药科技有限公司

区域:上海市嘉定区

价格:
¥需询单/1mg ¥705.6/10mg ¥2646.0/50mg

联系人:朱经理

产品详情:Mesoridazine


查看所有供应商请点击:

美索哒嗪供应商


相关化合物

【美索哒嗪】化源网提供美索哒嗪CAS号5588-33-0,美索哒嗪MSDS及其说明、性质、英文名、生产厂家、作用/用途、分子量、密度、沸点、熔点、结构式等。CAS号查询美索哒嗪上化源网,专业又轻松。>>电脑版:美索哒嗪

标题:美索哒嗪_用途_密度_沸点_美索哒嗪CAS号【5588-33-0】_化源网 地址:https://www.chemsrc.com/amp/cas/5588-33-0_127860.html