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塞庚啶

塞庚啶用途

赛庚啶是一种口服有效的5-HT2A受体拮抗剂,具有抗抑郁和抗腐烂作用。赛庚啶具有抗血小板和血栓保护活性。赛庚啶可用于研究血栓栓塞性疾病[1][2]。
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塞庚啶名称

[ CAS 号 ]:
129-03-3

[ 中文名 ]:
塞庚啶

[ 英文名 ]:
Cyproheptadine

[中文别名 ]:

[英文别名 ]:

塞庚啶生物活性

[ 描述 ]:

赛庚啶是一种口服有效的5-HT2A受体拮抗剂,具有抗抑郁和抗腐烂作用。赛庚啶具有抗血小板和血栓保护活性。赛庚啶可用于研究血栓栓塞性疾病[1][2]。

[ 相关类别 ]:

信号通路 >> 细胞凋亡 >> 细胞凋亡
研究领域 >> 心血管疾病
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

[体外研究]

赛庚啶(0.01-100 nM；1分钟)在体外剂量依赖性地抑制5-羟色胺增强的ADP诱导的小鼠血小板聚集[2]。赛庚啶(10 nM)能够在体外抑制血小板中15µM血清素增强的ADP诱导的(1µM)酪氨酸磷酸化[2]。赛庚啶在体外抑制人血小板PS暴露(膜联蛋白V)、P-选择素和GPIIb-IIIa(PAC-1结合)激活[2]。

[体内研究]

赛庚啶(1 mg/kg；静脉注射；每天,持续5天；C57BL/6小鼠)在体内发挥血栓保护作用[2]。动物模型：C57BL/6小鼠(8-10周龄)[2]剂量：1mg/kg给药：腹腔注射；每天一次,连续5天。结果：小鼠阻塞时间和尾部出血时间延长。

[参考文献]

[1]. Calka O, et, al. Effect of cyproheptadine on serum leptin levels. Adv Ther, 2005. 22(5): p. 424-8.

[2]. Olivia A Lin, et al. The Antidepressant 5-HT2A Receptor Antagonists Pizotifen and Cyproheptadine Inhibit Serotonin-Enhanced Platelet Function. PLoS One. 2014; 9(1): e87026.

塞庚啶物理化学性质

[ 密度 ]:
1.115g/cm3

[ 沸点 ]:
440.1ºC at 760mmHg

[ 熔点 ]:
298 °C (dec.)(lit.)

[ 分子式 ]:
C21H22ClN

[ 分子量 ]:
323.85900

[ 闪点 ]:
194.5ºC

[ 精确质量 ]:
323.14400

[ PSA ]:
3.24000

[ LogP ]:
5.43780

[ 外观性状 ]:
无色液体,甜的,杏仁气味

[ 蒸汽压 ]:
6.03E-08mmHg at 25°C

[ 折射率 ]:
1.5339 (20ºC)

塞庚啶毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :
TM7000000
CHEMICAL NAME :
Piperidine, 4-(5H-dibenzo(a,d)cyclohepten-5-ylidene)-1-methyl-
CAS REGISTRY NUMBER :
129-03-3
BEILSTEIN REFERENCE NO. :
1685976
LAST UPDATED :
199706
DATA ITEMS CITED :
12
MOLECULAR FORMULA :
C21-H21-N
MOLECULAR WEIGHT :
287.43
WISWESSER LINE NOTATION :
L C676 BYJ BU- DT6N DYTJ A1

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 :
295 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: -,69,1972
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
52 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: -,69,1972
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
106 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold
REFERENCE :
ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 25,1723,1975
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intraperitoneal
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
43300 ug/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold
REFERENCE :
ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 25,1723,1975
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Subcutaneous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
107 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: -,69,1972
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
15 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold
REFERENCE :
ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 25,1723,1975
TYPE OF TEST :
LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
50 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
27ZIAQ "Drug Dosages in Laboratory Animals - A Handbook," Rev. ed., Barnes, C.D., and L.G. Eltherington, Berkeley, Univ. of California Press, 1973 Volume(issue)/page/year: -,82,1973
TYPE OF TEST :
LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rabbit
DOSE/DURATION :
3500 ug/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: -,69,1972 ** REPRODUCTIVE DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intraperitoneal
DOSE :
10 mg/kg
SEX/DURATION :
female 10 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Embryo or Fetus - fetal death Reproductive - Specific Developmental Abnormalities - musculoskeletal system Reproductive - Effects on Newborn - weaning or lactation index (e.g., # alive at weaning per # alive at day 4)
REFERENCE :
AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 257,168,1982
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intraperitoneal
DOSE :
20 mg/kg
SEX/DURATION :
female 13 day(s) after conception
TOXIC EFFECTS :
Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants)
REFERENCE :
AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 257,168,1982
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intraperitoneal
DOSE :
20 mg/kg
SEX/DURATION :
female 10 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Newborn - viability index (e.g., # alive at day 4 per # born alive)
REFERENCE :
AIPTAK Archives Internationales de Pharmacodynamie et de Therapie. (Heymans Institute of Pharmacology, De Pintelaan 185, B-9000 Ghent, Belgium) V.4- 1898- Volume(issue)/page/year: 257,168,1982
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塞庚啶安全信息

[ 包装等级 ]:
I; II; III

[ 海关编码 ]:
29143900

塞庚啶合成路线

详细合成路线

塞庚啶上下游产品

塞庚啶上游产品

塞庚啶下游产品

塞庚啶海关

[ 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%

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公司名：上海化源世纪贸易有限公司

区域：上海市普陀区

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联系人：徐经理

产品详情：Cyproheptadine

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