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盐酸噻氯匹定

盐酸噻氯匹定用途

Ticlopidine盐酸盐是ADP受体抑制剂,对血小板凝集的IC50为2 μM。

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盐酸噻氯匹定名称

[ CAS 号 ]:
53885-35-1

[ 中文名 ]:
盐酸噻氯匹定

[ 英文名 ]:
Ticlopidine Hydrochloride

[中文别名 ]:

[英文别名 ]:

MFCD00661081
Ticlopidine hydrochloride
EINECS 258-837-4
Ticlopidine HCl

盐酸噻氯匹定生物活性

[ 描述 ]:

Ticlopidine盐酸盐是ADP受体抑制剂,对血小板凝集的IC50为2 μM。

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 腺苷受体

研究领域 >> 心血管疾病

[参考文献]

[1]. Thebault JJ, et al. Effects of ticlopidine, a new platelet aggregation inhibitor in man. Clin Pharmacol Ther. 1975 Oct;18(4):485-90.

[2]. Ashida SI, et al. Mode of action of ticlopidine in inhibition of platelet aggregation in the rat. Thromb Haemost. 1979 Apr 23;41(2):436-49.

[相关活性小分子]

盐酸噻氯匹定物理化学性质

[ 沸点 ]:
367.3ºC at 760 mmHg

[ 熔点 ]:
205°C

[ 分子式 ]:
C₁₄H₁₅Cl₂NS

[ 分子量 ]:
300.247

[ 闪点 ]:
175.9ºC

[ 精确质量 ]:
299.030212

[ PSA ]:
31.48000

[ LogP ]:
4.69970

[ 外观性状 ]:
白色粉末

[ 储存条件 ]:
库房通风低温干燥

[ 水溶解性 ]:
水溶性：可溶；可溶于：甲醇；微溶：乙醇；不溶：乙醚

盐酸噻氯匹定MSDS

详细MSDS(安全技术说明书)

盐酸噻氯匹定毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: XJ9089100

CHEMICAL NAME :: Thieno(3,2-c)pyridine, 4,5,6,7-tetrahydro-5-(o-chlorobenzyl)-, hydrochloride

CAS REGISTRY NUMBER :: 53885-35-1

LAST UPDATED :: 199706

DATA ITEMS CITED :: 16

MOLECULAR FORMULA :: C14-H14-Cl-N-S.Cl-H

MOLECULAR WEIGHT :: 300.26

WISWESSER LINE NOTATION :: T56 BS GN&TJ G1R BG &GH

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 :: 1780 mg/kg

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

REFERENCE :: MEPHDN Medical Pharmacy. (Daiichi Seiyaku K.K., 3-14-10 Nihonbashi, Chuo-ku, Tokyo 103, Japan) V.1- 1966- Volume(issue)/page/year: 15,272,1981

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: >3 gm/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - other changes Nutritional and Gross Metabolic - body temperature decrease

REFERENCE :: YKYUA6 Yakkyoku. Pharmacy. (Nanzando, 4-1-11, Yushima, Bunkyo-ku, Tokyo, Japan) V.1- 1950- Volume(issue)/page/year: 32,1499,1981

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 70 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: 12,1204,1981

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 600 mg/kg

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

REFERENCE :: MEPHDN Medical Pharmacy. (Daiichi Seiyaku K.K., 3-14-10 Nihonbashi, Chuo-ku, Tokyo 103, Japan) V.1- 1966- Volume(issue)/page/year: 15,272,1981

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 2690 mg/kg

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

REFERENCE :: MEPHDN Medical Pharmacy. (Daiichi Seiyaku K.K., 3-14-10 Nihonbashi, Chuo-ku, Tokyo 103, Japan) V.1- 1966- Volume(issue)/page/year: 15,272,1981

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 55 mg/kg

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

REFERENCE :: USXXAM United States Patent Document. (U.S. Patent Office, Box 9, Washington, DC 20231) Volume(issue)/page/year: #4051141

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Primate - monkey

DOSE/DURATION :: 500 mg/kg

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

REFERENCE :: NDADD8 New Drugs Annual: Cardiovascular Drugs. (New York, NY) V.1-2, 1983-84. For publisher information, see NCDREP. Volume(issue)/page/year: 1,295,1983 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 17400 mg/kg/29D-I

TOXIC EFFECTS :: Liver - changes in liver weight Kidney, Ureter, Bladder - other changes in urine composition Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol)

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 18,781,1979

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 27375 mg/kg/1Y-I

TOXIC EFFECTS :: Liver - other changes Liver - changes in liver weight

REFERENCE :: YKYUA6 Yakkyoku. Pharmacy. (Nanzando, 4-1-11, Yushima, Bunkyo-ku, Tokyo, Japan) V.1- 1950- Volume(issue)/page/year: 32,1499,1981

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 4500 mg/kg/30D-I

TOXIC EFFECTS :: Liver - fatty liver degeneration Kidney, Ureter, Bladder - changes in tubules (including acute renal failure, acute tubular necrosis) Kidney, Ureter, Bladder - other changes in urine composition

REFERENCE :: YKYUA6 Yakkyoku. Pharmacy. (Nanzando, 4-1-11, Yushima, Bunkyo-ku, Tokyo, Japan) V.1- 1950- Volume(issue)/page/year: 32,1499,1981

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 46800 mg/kg/26W-I

TOXIC EFFECTS :: Liver - changes in liver weight Endocrine - other changes Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - transaminases

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 18,797,1979 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 10800 mg/kg

SEX/DURATION :: female 17-22 day(s) after conception lactating female 21 day(s) post-birth

TOXIC EFFECTS :: Reproductive - Maternal Effects - parturition Reproductive - Effects on Newborn - weaning or lactation index (e.g., # alive at weaning per # alive at day 4) Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain)

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: 11,276,1980

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 220 mg/kg

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

TOXIC EFFECTS :: Reproductive - Effects on Newborn - stillbirth Reproductive - Effects on Newborn - live birth index (measured after birth) Reproductive - Effects on Newborn - behavioral

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: 11,265,1980

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 4400 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)

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: 11,265,1980

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 220 mg/kg

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

TOXIC EFFECTS :: Reproductive - Effects on Newborn - physical

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: 11,265,1980

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 650 mg/kg

SEX/DURATION :: female 6-18 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Specific Developmental Abnormalities - musculoskeletal system Reproductive - Effects on Newborn - viability index (e.g., # alive at day 4 per # born alive)

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: 11,287,1980

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盐酸噻氯匹定安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302

[ 警示性声明 ]:
P301 + P312 + P330

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

[ 危害码 (欧洲) ]:
Xn:Harmful

[ 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 ]:
XJ9089100

[ 海关编码 ]:
2934999090

盐酸噻氯匹定上下游产品

盐酸噻氯匹定上游产品

盐酸噻氯匹定下游产品

盐酸噻氯匹定制备

1. 2-氯甲基噻吩的制备

在反应瓶中加入噻吩42g(39.2ml,0.5mol)和浓盐酸20ml,用冰盐浴冷却,在剧烈搅拌下使快速的HCl气体气流连续地通入混合物.当温度到达0ºC时,滴加37%甲醛水溶液50ml(0.666mol),控制加入速度,使温度保持在5ºC以下,需30~50min加完.当全部甲醛液加完后,将反应混合物用乙醚(50ml×3)提取,合并乙醚提取液,依次用水和饱和NaHCO3溶液洗涤,无水CaCl2干燥,过滤,滤液蒸除溶剂,剩余物减压蒸馏(应采用合适的分馏柱),收集73~75ºC/2.26 kPa(17mmHg)馏分,得无色油状液体2-氯甲基噻吩25.7~26.7g,收率40%~41%.

2. 氯化(2-噻吩甲基)六次甲基四铵的制备

在反应瓶中加入上步反应产物2-氯甲基噻吩67g(0.5mol)、氯仿400ml和六次甲基四胺70g(0.5mol),加热至回流,搅拌缓和回流反应30min.冷却,过滤,滤饼用冷氯仿100l洗涤,压干抽干后,晾干,得氯化(2-噻吩甲基)六次甲基四铵128~136g,收率94%~99%,为白色粉末产物.

3. 2-噻吩甲醛的制备

在2000ml圆底烧瓶中加入400ml温水和上步制

备的化合物氯化(2-噻吩甲基)六次甲基四铵一批量(128~136g),把烧瓶装配成水蒸气蒸馏装置,通入水蒸气至所有的醛被蒸出为止(蒸出所有的2-噻吩甲醛要收集大约1.5L馏出液).馏出液冷却后,加6mol/L乙酸10ml(如果2-噻吩甲醛要贮存一段时间,应加入少量对苯二酚),含醛馏出液用乙醚提取0次,每次用乙醚100ml.乙醚溶液用无水氯化钙干燥,过滤,滤液蒸至体积减少到500ml左右,然后将此溶液转移到100ml克氏烧瓶中,蒸去乙醚,再减压蒸馏,收集89~91ºC/2.799kPa(21mmHg)馏分,得无色油状物2-噻吩甲醛27~30g,收率48%~53%.

4. 2-硝基乙烯噻吩的制备

在反应瓶中加入上步制备的化合物2-噻吩甲醛56g(0.5mol)、硝基甲烷61g(1mol)、甲醇1000ml,用冰盐浴冷却至0ºC以下,搅拌滴加40%氢氧化钠水溶液100g(1mol),滴加过程中维持温度在5ºC以下,约2h滴毕,继续搅拌4h.加入水300ml ,在搅拌下慢慢倒入含浓盐酸100ml的冰水中,析出黄色沉淀.过滤,水洗,干燥,得黄色固体2-硝基乙烯噻吩54g,收率70%,mp80~82ºC.

5. 2-噻吩乙胺的制备

在反应瓶中加入硼氢化钾54g(1mol)、四氢呋喃(THF)500ml,搅拌降温至0ºC,于0ºC慢慢滴加三氟化硼乙醚液150ml(1.2mol),加毕,于0~5ºC下搅拌反应2h.再搅拌滴加化合物2-硝基乙烯噻吩31g(0.2mol)的THF300ml溶液,约1h滴毕.于室温下搅拌反应24h.加入甲苯500ml.蒸馏,当内温达到90ºC时,改成回流,搅拌回流1h.冷至0ºC.加水100ml,用1mol/L盐酸500ml慢慢酸化.加热至80ºC,搅拌1h.冷至40~50ºC.分取水层,甲苯层用1mol/L盐酸200ml洗,合并水层,用NaOH溶液调pH至13.用二氯甲烷(500ml×3)提取,合并提取液,用水200ml洗涤,无水MgSO4干燥,过滤,滤液浓缩回收二氯甲烷,剩余物为油状物2-噻吩乙胺约19.5g,收率80%.

6. 2-噻吩乙基亚甲胺的制备

在反应瓶中加入上步制备的化合物2-噻吩乙胺12.7g(0.1mol),在搅拌下于室温滴加36%~37%甲醛水溶液10g(0.12mol).滴毕,搅拌回流反应3h.冷却,#用二氯甲烷(150ml×3)提取,合并提取液,用水50ml洗涤,无水MgSO4干燥,过滤,滤液浓缩,得淡黄色油状物2-噻吩乙基亚甲胺12.8g,收率92%.

7. 4,5,6,7-四氢噻吩并[3,2-c]吡啶的制备

在反应瓶中加入上步制备的化合物2-噻吩乙基亚甲胺13.9g(0.1mol)和6mol/L盐酸28ml,于室温搅拌反应6h.加入NaOH水溶液调pH至13,用二氯甲烷(200ml×3)提取,合并有机层,用水100ml洗涤,用无水MgSO4干燥.过滤,滤液浓缩回收二氯甲烷,得浅黄色油状物4,5,6,7-四氢噻吩并[3,2-c]吡啶粗品13.9g,收率100%.无需纯化,直接用于噻氯匹定的合成.

8. 2-氯氯苄的制备

在反应瓶中加入邻氯甲苯108g(0.854mol)、过氧化苯甲酰0.4g、三氯化磷0.3g,在搅拌和光照下加热至90~95ºC,通入干燥的氯气,维持反应液温度在95~100ºC,至反应液的相对密度达1.20~1.22即停止通氯气.冷却,用温水洗涤反应液数次后,用无水Na2SO4干燥,过滤,将滤液减压蒸馏,收集93~98ºC/1.33kPa馏分,得无色液体2-氯氯苄11.2g,收率82%.

9. 5-[(2-氯苯基)甲基]-4,5,6,7-四氢噻吩并[3,2-c]吡啶盐酸盐(盐酸噻氯匹定)的合成

在反应瓶中加入第七步制备的化合物4,5,6,7-四氢噻吩并[3,2-c]吡啶13.9g(0.1mol)、上步制备的化合物2-氯氯苄16.1g(0.1mol)、三乙胺15g(0.15mol)和乙腈150ml,于室温下搅拌反应4h.减压浓缩回收乙腈,加入甲苯100ml和水100ml,充分搅拌后静置分层,分取甲苯层,水层用甲苯(50ml×3)提取,合并甲苯液,用水(50ml×3)洗涤,无水MgSO4干燥.过滤,滤液用氯化氢异丙醇溶液调pH至2,搅拌30min.放冷,析出固体,过滤,得浅黄色固体.用无水乙醇重结晶,得白色固体5-[(2-氯苯基)甲基]-4,5,6,7-四氢噻吩并[3,2-c]吡啶盐酸盐(盐酸噻氯匹定)23g,收率75%,mp206~207ºC.

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盐酸噻氯匹定海关

[ 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%

盐酸噻氯匹定文献

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盐酸噻氯匹定

盐酸噻氯匹定用途

盐酸噻氯匹定名称

盐酸噻氯匹定生物活性

盐酸噻氯匹定物理化学性质

盐酸噻氯匹定MSDS

详细MSDS(安全技术说明书)

盐酸噻氯匹定毒性和生态

CHEMICAL IDENTIFICATION

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

盐酸噻氯匹定安全信息

盐酸噻氯匹定上下游产品

盐酸噻氯匹定上游产品

盐酸噻氯匹定下游产品

盐酸噻氯匹定制备

盐酸噻氯匹定海关

盐酸噻氯匹定文献

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