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尼扎替丁

尼扎替丁用途

Nizatidine是组胺H2受体拮抗剂,毒性低,可抑制胃酸分泌。

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尼扎替丁名称

[ CAS 号 ]:
76963-41-2

[ 中文名 ]:
尼扎替丁

[ 英文名 ]:
Nizatidine

[中文别名 ]:

盐酸阿那格雷

[英文别名 ]:

Tazac
Acinon
Nizax
Cronizat
Axid
MFCD00865660
Galitidin
Distaxid
Nizatidine
Zanizal

尼扎替丁生物活性

[ 描述 ]:

Nizatidine是组胺H2受体拮抗剂,毒性低,可抑制胃酸分泌。

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 组胺受体

信号通路 >> 免疫及炎症 >> 组胺受体

研究领域 >> 炎症/免疫

[参考文献]

[1]. Lin, T.M., et al., Actions of nizatidine, a selective histamine H2-receptor antagonist, on gastric acid secretion in dogs, rats and frogs. J Pharmacol Exp Ther, 1986. 239(2): p. 406-10.

[2]. Ueki, S., et al., Gastroprokinetic activity of nizatidine, a new H2-receptor antagonist, and its possible mechanism of action in dogs and rats. J Pharmacol Exp Ther, 1993. 264(1): p. 152-7.

[相关活性小分子]

尼扎替丁物理化学性质

[ 密度 ]:
1.2±0.1 g/cm3

[ 沸点 ]:
478.2±45.0 °C at 760 mmHg

[ 熔点 ]:
130-132ºC

[ 分子式 ]:
C₁₂H₂₁N₅O₂S₂

[ 分子量 ]:
331.457

[ 闪点 ]:
243.0±28.7 °C

[ 精确质量 ]:
331.113678

[ PSA ]:
139.55000

[ LogP ]:
1.18

[ 外观性状 ]:
白色至灰白色结晶粉末

[ 蒸汽压 ]:
0.0±1.2 mmHg at 25°C

[ 折射率 ]:
1.592

[ 储存条件 ]:
-20?C Freezer

尼扎替丁MSDS

尼扎替丁毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: KM6565000

CHEMICAL NAME :: 1,1-Ethenediamine, N-(2-(((2-((dimethylamino)methyl)-4-thiazolyl)methyl) thio)ethyl)-N'- methyl-2-nitro-

CAS REGISTRY NUMBER :: 76963-41-2

LAST UPDATED :: 199806

DATA ITEMS CITED :: 18

MOLECULAR FORMULA :: C12-H21-N5-O2-S2

MOLECULAR WEIGHT :: 331.50

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 :: 1653 mg/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,920,1995

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >2 gm/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Behavioral - coma Gastrointestinal - hypermotility, diarrhea

REFERENCE :: FAATDF Fundamental and Applied Toxicology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1981- Volume(issue)/page/year: 13,778,1989

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 301 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Behavioral - coma Gastrointestinal - hypermotility, diarrhea

REFERENCE :: FAATDF Fundamental and Applied Toxicology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1981- Volume(issue)/page/year: 13,778,1989

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1630 mg/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,920,1995

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1082 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Behavioral - coma Gastrointestinal - hypermotility, diarrhea

REFERENCE :: FAATDF Fundamental and Applied Toxicology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1981- Volume(issue)/page/year: 13,778,1989

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 232 mg/kg

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

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,920,1995

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: >800 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - lacrimation Behavioral - changes in motor activity (specific assay) Gastrointestinal - nausea or vomiting

REFERENCE :: FAATDF Fundamental and Applied Toxicology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1981- Volume(issue)/page/year: 13,778,1989

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: >75 mg/kg

TOXIC EFFECTS :: Behavioral - tremor Lungs, Thorax, or Respiration - dyspnea Gastrointestinal - nausea or vomiting

REFERENCE :: FAATDF Fundamental and Applied Toxicology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1981- Volume(issue)/page/year: 13,778,1989

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

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: >225 mg/kg

TOXIC EFFECTS :: Behavioral - tremor Behavioral - tetany Gastrointestinal - nausea or vomiting

REFERENCE :: FAATDF Fundamental and Applied Toxicology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1981- Volume(issue)/page/year: 13,778,1989

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Primate - monkey

DOSE/DURATION :: >1200 mg/kg

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

REFERENCE :: FAATDF Fundamental and Applied Toxicology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1981- Volume(issue)/page/year: 13,778,1989

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Primate - monkey

DOSE/DURATION :: >200 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - ptosis Behavioral - tremor Gastrointestinal - nausea or vomiting

REFERENCE :: FAATDF Fundamental and Applied Toxicology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1981- Volume(issue)/page/year: 13,778,1989 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 51415 mg/kg/13W-I

TOXIC EFFECTS :: Endocrine - changes in thymus weight Blood - change in clotting factors Blood - pigmented or nucleated red blood cells

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 17,525,1989

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 91 gm/kg/26W-C

TOXIC EFFECTS :: Liver - changes in liver weight Kidney, Ureter, Bladder - changes in bladder weight Nutritional and Gross Metabolic - weight loss or decreased weight gain

REFERENCE :: FAATDF Fundamental and Applied Toxicology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1981- Volume(issue)/page/year: 13,778,1989

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 146 gm/kg/1Y-C

TOXIC EFFECTS :: Liver - changes in liver weight Kidney, Ureter, Bladder - changes in bladder weight Nutritional and Gross Metabolic - weight loss or decreased weight gain

REFERENCE :: FAATDF Fundamental and Applied Toxicology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1981- Volume(issue)/page/year: 13,778,1989

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 164 gm/kg/91D-C

TOXIC EFFECTS :: Liver - changes in liver weight Nutritional and Gross Metabolic - weight loss or decreased weight gain

REFERENCE :: FAATDF Fundamental and Applied Toxicology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1981- Volume(issue)/page/year: 13,778,1989

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 73 gm/kg/91D-I

TOXIC EFFECTS :: Liver - other changes Nutritional and Gross Metabolic - weight loss or decreased weight gain Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - other Enzymes

REFERENCE :: FAATDF Fundamental and Applied Toxicology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1981- Volume(issue)/page/year: 13,778,1989

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 146 gm/kg/1Y-I

TOXIC EFFECTS :: Liver - other changes Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - other Enzymes

REFERENCE :: FAATDF Fundamental and Applied Toxicology. (Academic Press, Inc., 1 E. First St., Duluth, MN 55802) V.1- 1981- Volume(issue)/page/year: 13,778,1989 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 16500 mg/kg

SEX/DURATION :: female 7-17 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Effects on Newborn - sex ratio

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 17,547,1989

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尼扎替丁安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302

[ 警示性声明 ]:
P301 + P312 + P330

[ 危害码 (欧洲) ]:
Xn

[ 风险声明 (欧洲) ]:
R22

[ 安全声明 (欧洲) ]:
S36

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

[ WGK德国 ]:
3

[ RTECS号 ]:
KM6565000

[ 海关编码 ]:
2934999090

尼扎替丁合成路线

尼扎替丁上下游产品

尼扎替丁上游产品

尼扎替丁下游产品

尼扎替丁制备

【方法一】
硝基甲烷和二硫化碳在无水乙醇中，在33-35℃滴加氢氧化钾的乙醇溶液，反应结束后抽滤；得到的红色固体悬浮于甲醇中，在25℃滴加碘甲烷，并继续反应，得到的黄色粗品用环己酮重结晶，得金黄色针状结晶的1，1-二甲硫基-2-硝基乙烯，收率68%。然后和半胱胺盐酸盐及氢氧化钾在乙醇和水的混合液中，回流得橘红色的2-硝基亚甲基-1，3-噻唑烷结晶，收率65%。再和33%的甲胺乙醇溶液，于室温下反应，得N-(2-巯乙基)-N’-甲基-2-硝基-1，l-乙烯二胺，收率85%。
33%二甲胺水溶液和亚硫酸氢钠、36%甲醛及水一起搅拌。加入氰化钾，继续反应得二甲胺基乙腈，沸点34-38℃/2.7kPa，收率83.6%。再和无水吡啶、无水三乙胺和无水甲醇混合，通人硫化氢，在80℃加热后，再室温放置，可得二甲胺基硫代乙酰胺，收率35%。然后在-5℃，将其加入1，3-二氯丙酮的丙酮溶液，反应得2-二甲胺基甲基-4-氯甲基-4-羟基噻唑啉，收率72%。将其溶于1，2-二氯乙烷中，在室温下滴加氯化亚砜的二氯乙烷溶液，室温反应后，再在40℃反应，可得2-二甲胺基甲基-4-氯甲基噻唑盐酸盐，收率62%。最后和N-(2-巯乙基)-N’-甲基-2-硝基-1，1-乙烯二胺在氢氧化钠水溶液中反应，得尼扎替丁，用甲醇-醋酸乙酯重结晶，熔点129-132℃，收率52%。

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尼扎替丁海关

[ 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%

尼扎替丁文献

Impact of sleep disorders in Japanese patients with functional dyspepsia (FD): nizatidine improves clinical symptoms, gastric emptying and sleep disorders in FD patients.

J. Gastroenterol. Hepatol. 28(8) , 1314-20, (2013)

The association between functional dyspepsia (FD) and sleep disorders has yet to be studied in detail. The aim of this study is to evaluate the risk factors associated with sleep disorders and the cli...

[Nizatidine].

Medicina (Firenze.) 9(1) , 93-6, (1989)

Nizatidine is a new H2-receptor antagonist, as potent as ranitidine. It does not interfere with hepatic metabolism and it lacks anti-androgenic effects. An evening dose of 300 mg suppresses nocturnal ...

Nizatidine improves clinical symptoms and gastric emptying in patients with functional dyspepsia accompanied by impaired gastric emptying.

Digestion 86(2) , 114-21, (2012)

In this crossover study, we investigated whether nizatidine, a H(2)-receptor antagonist, can alleviate clinical symptoms and gastric emptying in patients with Rome III-based functional dyspepsia (FD) ...

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尼扎替丁

尼扎替丁用途

尼扎替丁名称

尼扎替丁生物活性

尼扎替丁物理化学性质

尼扎替丁MSDS

详细MSDS(安全技术说明书)

尼扎替丁毒性和生态

CHEMICAL IDENTIFICATION

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

尼扎替丁安全信息

尼扎替丁合成路线

详细合成路线

尼扎替丁上下游产品

尼扎替丁上游产品

尼扎替丁下游产品

尼扎替丁制备

尼扎替丁海关

尼扎替丁文献

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