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盐酸替扎尼定

盐酸替扎尼定用途

Tizanidine盐酸盐是α2-肾上腺素受体激动剂,能抑制神经递质从CNS去甲肾上腺素激活的神经元中释放。

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盐酸替扎尼定名称

[ CAS 号 ]:
64461-82-1

[ 中文名 ]:
盐酸替扎尼定

[ 英文名 ]:
Tizanidine hydrochloride

[中文别名 ]:

[英文别名 ]:

MFCD00798231

盐酸替扎尼定生物活性

[ 描述 ]:

Tizanidine盐酸盐是α2-肾上腺素受体激动剂,能抑制神经递质从CNS去甲肾上腺素激活的神经元中释放。

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 肾上腺素能受体

研究领域 >> 神经疾病

[参考文献]

[1]. Kamen L, et al. A practical overview of tizanidine use for spasticity secondary to multiple sclerosis, stroke, and spinal cord injury. Curr Med Res Opin. 2008 Feb;24(2):425-39.

[相关活性小分子]

盐酸替扎尼定物理化学性质

[ 沸点 ]:
391.2ºC at 760 mmHg

[ 熔点 ]:
280 °C

[ 分子式 ]:
C₉H₉Cl₂N₅S

[ 分子量 ]:
290.17200

[ 闪点 ]:
190.4ºC

[ 精确质量 ]:
288.99600

[ PSA ]:
90.44000

[ LogP ]:
2.35520

[ 外观性状 ]:
白色固体

[ 储存条件 ]:
Desiccate at RT

[ 水溶解性 ]:
H2O: ~29 mg/mL

盐酸替扎尼定MSDS

详细MSDS(安全技术说明书)

盐酸替扎尼定毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: DK9910000

CHEMICAL NAME :: 2,1,3-Benzothiadiazol-4-amine, 5-chloro-N-(4,5-dihydro-1H-imidazol-2-yl)-, monohydrochloride

CAS REGISTRY NUMBER :: 64461-82-1

LAST UPDATED :: 199209

DATA ITEMS CITED :: 10

MOLECULAR FORMULA :: C9-H8-Cl-N5-S.Cl-H

MOLECULAR WEIGHT :: 290.19

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 :: 414 mg/kg

TOXIC EFFECTS :: Behavioral - tremor Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 19,5811,1985

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 282 mg/kg

TOXIC EFFECTS :: Behavioral - tremor Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 19,5811,1985

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 35 mg/kg

TOXIC EFFECTS :: Behavioral - tremor Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 19,5811,1985

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 235 mg/kg

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

REFERENCE :: JKXXAF Japanese Kokai Tokyo Koho Patents. (U.S. Patent and Trademark Office, Foreign Patents, Washington, DC 20231) Volume(issue)/page/year: #81-02912

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 48 mg/kg

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

REFERENCE :: IYKEDH Iyakuhin Kenkyu. Study of Medical Supplies. (Nippon Koteisho Kyokai, 12-15, 2-chome, Shibuya, Shibuya-ku, Tokyo 150, Japan) V.1- 1970- Volume(issue)/page/year: 19,544,1988

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 98 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: -,642,1990 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 2100 mg/kg/5W-C

TOXIC EFFECTS :: Liver - other changes Endocrine - other changes Blood - changes in spleen

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 19,5811,1985 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 110 mg/kg

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

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

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 19,5825,1985

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 33 mg/kg

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

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

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 19,5825,1985

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 11 mg/kg

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

TOXIC EFFECTS :: Reproductive - Effects on Newborn - physical

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 19,5825,1985

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盐酸替扎尼定安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302-H315-H319-H335

[ 警示性声明 ]:
P301 + P312 + P330-P305 + P351 + P338

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Faceshields;Gloves

[ 危害码 (欧洲) ]:
Xn: Harmful;

[ 风险声明 (欧洲) ]:
R22;R36/37/38

[ 安全声明 (欧洲) ]:
S26-S36

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

[ WGK德国 ]:
3

[ RTECS号 ]:
DK9910000

[ 海关编码 ]:
2934300000

盐酸替扎尼定制备

1. 4-氯-1,2-苯二胺的制备

在反应瓶中加入4-氯-2-硝基苯胺60.4g(0.35mol)、95%乙醇170ml和2%NaOH水溶液30ml,搅拌升温至回流,分批加入锌粉98g(1.5mol),加毕#继续搅拌回流2h.热过滤,滤饼用热乙醇(85ml×2)洗涤,滤液洗液合并,加入保险粉2g,减压浓缩至1/2体积,冰浴冷却后抽滤,滤饼用冰水洗涤,用水重结晶,得浅粉红色固体4-氯-1,2-苯二胺43.9g,收率88%,mp72~73 ºC.

2. 5-氯-2,1,3-苯并噻二唑的制备

在反应瓶中加入甲苯400ml、催化量的DMF和4-氯-1,2-苯二胺38.6g(0.27mol),搅拌溶解,冰浴冷却下慢慢滴加SOCl2 50ml(0.69mol),滴毕,搅拌回流5h. 将反应液冷至室温,抽滤,滤液减压蒸除溶剂,得棕色固体5-氯-2,1,3-苯并噻二唑44.5g,收率96.3%.直接用于下步反应.

3. 5-氯-4-硝基-2,1,3-苯并噻二唑的制备

在反应瓶中加入浓硝酸50ml(0.75mol)和浓硫酸150ml组成的混酸,搅拌下冷至10 ºC,20 ºC以下

分批加入5-氯-2,1,3-苯并噻二唑44.5g(0.26mol), 加毕于20ºC搅拌反应2.5h.反应液倒入碎冰中,抽滤,滤饼用冰水洗,抽干,干燥,得黄色固体5-氯-4-硝基-2,1,3-苯并噻二唑粗品53.9g,用乙醇重结晶#得浅黄色针状结晶5-氯-4-硝基-2,1,3-苯并噻二唑49.0g,收率87.2%,mp143~144ºC.

4. 4-氨基-5-氯-2,1,3-苯并噻二唑的制备

在反应瓶中加入36%乙酸水溶液300ml和铁粉40g(0.72mol),搅拌下分批加入5-氯-4-硝基-2,1,3-苯并噻二唑32.8g(0.15mol),升至90~95ºC搅拌反应30min. 趁热过滤,滤液减压蒸除溶剂,剩余液冷至室温,用氯仿150ml提取,有机相依次用水30ml和饱和食盐水30ml洗涤,无水Na2SO4干燥,过滤,滤液减压蒸除溶剂,剩余物用异丙醇重结晶,得淡黄色粉末4-氨基-5-氯-2,1,3-苯并噻二唑24.9g,收率88.1%,mp91~93ºC.

5. 5-氯-N-(1-乙酰基-4,5-二氢-1H-咪唑-2-基)-2,1,3-苯并噻唑-4-胺的制备

在反应瓶中加入4-氨基-5-氯-2,1,3-苯并噻二唑36g(0.2mol)、1-乙酰基咪唑啉-2-酮25.4g(0.2mol)和POCl3 120ml(1.29mol),于60~65 ºC搅拌反应36h,减压蒸除溶剂,剩余红棕色油状物加至冰水250ml中,用30%NaOH水溶液调至pH9~10,析出结晶,过滤,滤饼用少量冰水洗涤后干燥,再用甲醇重结晶,得黄色针状结晶5-氯-N-(1-乙酰基-4,5-二氢-1H-咪唑-2-基)-2,1,3-苯并噻唑-4-胺49g,收率85.4%,mp214~216 ºC,

6. 替扎尼定的制备

在反应瓶中加入5-氯-N-(1-乙酰基-4,5-二氢-1H-咪唑-2-基)-2,1,3-苯并噻唑-4-胺26.7g(0.09mol)、甲醇100ml,搅拌溶解,再加入1.5mol/LNaOH水溶液100ml(0.15mol),于60~65 ºC搅拌反应2h. 减压蒸除甲醇,冷至室温后过滤,滤饼用少量甲醇洗涤,干燥#得黄色粉状固体替扎尼定粗品22.0g,再用甲醇重结晶,得亮黄色针状结晶替扎尼定22.0g,收率88.4%,mp220~222 ºC.

7. 盐酸替扎尼定的合成

在反应瓶中加入替扎尼定19.5g(0.77mol)和饱和HCl气体乙醇溶液100ml,室温搅拌1h.抽滤,滤饼用无水乙醇洗涤后抽干,干燥,用乙醇重结晶,得淡黄色针状结晶盐酸替扎尼定20.9g,收率93.8%,mp288~290 ºC.纯度99.5%.

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盐酸替扎尼定海关

[ 海关编码 ]: 2934300000

[ 中文概述 ]:
2934300000. 含一个吩噻嗪环系的化合物(吩噻嗪环系不论是否氢化,化合物未经进一步稠合的 ). 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 ]:
2934300000. other compounds containing in the structure a phenothiazine ring-system (whether or not hydrogenated), not further fused. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

盐酸替扎尼定文献

Spectrophotometric determination of tizanidine and orphenadrine via ion pair complex formation using eosin Y.

Chem. Cent. J. 5 , 60, (2011)

A simple, sensitive and rapid spectrophotometric method was developed and validated for the determination of two skeletal muscle relaxants namely, tizanidine hydrochloride (I) and orphenadrine citrate...

Antihyperalgesic and side effects of intrathecal clonidine and tizanidine in a rat model of neuropathic pain.

Anesthesiology 98 , 1480-1483, (2003)

Although intrathecal clonidine produces pronounced analgesia, antinociceptive doses of intrathecal clonidine produce several side effects, including hypotension, bradycardia, and sedation. Intrathecal...

更多文献

盐酸替扎尼定

盐酸替扎尼定用途

盐酸替扎尼定名称

盐酸替扎尼定生物活性

盐酸替扎尼定物理化学性质

盐酸替扎尼定MSDS

详细MSDS(安全技术说明书)

盐酸替扎尼定毒性和生态

CHEMICAL IDENTIFICATION

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

盐酸替扎尼定安全信息

盐酸替扎尼定制备

盐酸替扎尼定海关

盐酸替扎尼定文献

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