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盐酸赛庚啶

盐酸赛庚啶用途

Cyproheptadine是5-HT2受体拮抗剂,IC50为0.6 nM。

盐酸赛庚啶作用

为H1受体拮抗剂，作用较氯苯那敏、异丙嗪强，并有中度抗5－羟色胺作用和抗胆碱作用。另外，临床发现，赛庚啶还有治疗流行性腮腺炎等多种新用途，研究表明盐酸赛庚啶的H1拮抗作用比扑尔敏强5倍以上。

盐酸赛庚啶名称

[ CAS 号 ]:
969-33-5

[ 中文名 ]:
盐酸赛庚啶

[ 英文名 ]:
cyproheptadine hydrochloride

[英文别名 ]:

periactinolhydrochloride
cyproheptadienehydrochloride
CYPROHEPTADINE HCL BP
peritol
ANAREXOL
Cyproheptadin
periactinhydrochloride
MFCD00012538
cyproheptadine hydrochloride
CYPROHEPTADINE HCL

盐酸赛庚啶生物活性

[ 描述 ]:

Cyproheptadine是5-HT2受体拮抗剂,IC50为0.6 nM。

[ 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

[参考文献]

[1]. Honda, M., T. Nishida, and H. Ono, Tricyclic analogs cyclobenzaprine, amitriptyline and cyproheptadine inhibit the spinal reflex transmission through 5-HT(2) receptors. Eur J Pharmacol, 2003. 458(1-2): p. 91-9.

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

[相关活性小分子]

盐酸赛庚啶物理化学性质

[ 沸点 ]:
440.1ºC at 760mmHg

[ 分子式 ]:
C₂₁H₂₂ClN

[ 分子量 ]:
323.859

[ 闪点 ]:
194.5ºC

[ 精确质量 ]:
323.144073

[ PSA ]:
3.24000

[ LogP ]:
5.43780

[ 外观性状 ]:
粉末

[ 储存条件 ]:
Store at RT

[ 水溶解性 ]:
ethanol: soluble

盐酸赛庚啶毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: TM7050000

CHEMICAL NAME :: Piperidine, 4-(5H-dibenzo(a,d)cyclohepten-5-ylidene)-1-methyl-, hydrochloride

CAS REGISTRY NUMBER :: 969-33-5

LAST UPDATED :: 199707

DATA ITEMS CITED :: 14

MOLECULAR FORMULA :: C21-H21-N.Cl-H

MOLECULAR WEIGHT :: 323.89

WISWESSER LINE NOTATION :: L C676 BYJ BU- DT6N DYTJ A1 &GH

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 7 mg/kg/4W-C

TOXIC EFFECTS :: Gastrointestinal - other changes Liver - jaundice, cholestatic Liver - liver function tests impaired

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

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 52400 ug/kg

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

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >1 gm/kg

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

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 69 mg/kg

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

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 55300 ug/kg

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

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

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 23 mg/kg

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

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - guinea pig

DOSE/DURATION :: 216 mg/kg

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

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 60 mg/kg

SEX/DURATION :: female 5-16 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 250 mg/kg

SEX/DURATION :: female 6-15 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Specific Developmental Abnormalities - homeostasis

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 40 mg/kg

SEX/DURATION :: female 13-20 day(s) after conception

TOXIC EFFECTS :: Reproductive - Specific Developmental Abnormalities - endocrine system

MUTATION DATA

TYPE OF TEST :: Cytogenetic analysis

TEST SYSTEM :: Human Lymphocyte

DOSE/DURATION :: 2200 umol/L/24H (Continuous)

REFERENCE :: ZEKIA5 Zeitschrift fuer Kinderheilkunde. (Berlin, Ger.) V.1-120, 1910-75. For publisher information, see EJPEDT. Volume(issue)/page/year: 118,219,1974 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X3187 No. of Facilities: 79 (estimated) No. of Industries: 1 No. of Occupations: 2 No. of Employees: 2047 (estimated) No. of Female Employees: 947 (estimated)

盐酸赛庚啶安全信息

[ 危害码 (欧洲) ]:
Xn: Harmful;

[ 风险声明 (欧洲) ]:
R22;R36/37/38

[ 安全声明 (欧洲) ]:
26-36

[ 危险品运输编码 ]:
UN 2811

[ WGK德国 ]:
3

[ RTECS号 ]:
TM7050000

[ 包装等级 ]:
III

[ 危险类别 ]:
6.1(b)

[ 海关编码 ]:
2933399090

盐酸赛庚啶海关

[ 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%