盐酸替诺立定
盐酸替诺立定用途
Tinoridine hydrochloride是一种非甾体抗炎药,也具有强效的自由基清除和抗过氧化物活性。
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盐酸替诺立定名称
[ CAS 号 ]:
25913-34-2
[ 中文名 ]:
盐酸替诺立定
[ 英文名 ]:
Tinoridine hydrochloride
[中文别名 ]:
[英文别名 ]:
- Tinoridine Hydrochloride
- Dimaten
- Tinoridine HCl
- Tenocyclidine hydrochloride
- Nonflamin
- Einecs 247-342-9
盐酸替诺立定生物活性
[ 描述 ]:
Tinoridine hydrochloride是一种非甾体抗炎药,也具有强效的自由基清除和抗过氧化物活性。
[ 相关类别 ]:
[体外研究]
Tinoridine以约1：2的摩尔比还原稳定的自由基二苯基-对-苦基肼基,表明其自由基清除能力。在ADP和Fe2 +存在下,Tinoridine抑制由黄嘌呤-黄嘌呤氧化酶系统诱导的大鼠肝微粒体中的脂质过氧化,其中形成羟基。通过跟踪来自锡诺定的氧化产物的荧光,证明了氟哌啶在脂质过氧化过程中被氧化。它也被黄嘌呤-黄嘌呤氧化酶系统在Fe2 +存在下氧化,但是在没有Fe2 +的情况下它的氧化很慢并且几乎完全被过氧化氢酶抑制。碘化氢也被H2O2-Fe2 +体系氧化,产生OH(芬顿反应),但它不会影响超氧化物自由基引起的细胞色素c的减少[1]。
[体内研究]
CCl4给药使肝微粒体细胞色素P-450和G6Pase的浓度显着降低,表明肝内质网功能被破坏。用氯噻嗪(100mg/kg)预处理动物可显着降低CCl4诱导的酶活性改变,并观察到向正常值的快速恢复[2]。
[激酶实验]
CCl4给药使肝微粒体细胞色素P-450和G6Pase的浓度显着降低，表明肝内质网功能被破坏。用氯噻嗪（100mg / kg）预处理动物可显着降低CCl4诱导的酶活性改变，并观察到向正常值的快速恢复[2]。
[动物实验]
大鼠：雄性Wistar大鼠（180-220g）用于实验。在CCl4给药前1小时，药物（Tinoridine）作为0.5％甲基纤维素溶液中的悬浮液口服给药。对照动物接受等量的载体。腹膜内施用CCl4，剂量为0.25ml / kg，为橄榄油中的5％（v / v）溶液。 CCl4给药后不同时间通过颈动脉切除杀死动物;将肝脏快速取出，称重并加工用于生化或组织学分析[2]。
[参考文献]
[相关活性小分子]
盐酸替诺立定物理化学性质
[ 密度 ]:
1.256g/cm3
[ 沸点 ]:
493.5ºC at 760mmHg
[ 熔点 ]:
234-235° (dec)
[ 分子式 ]:
C17H21ClN2O2S
[ 分子量 ]:
352.87900
[ 闪点 ]:
252.3ºC
[ 精确质量 ]:
352.10100
[ PSA ]:
83.80000
[ LogP ]:
4.38640
[ 外观性状 ]:
固体;White to Light yellow powder to crystal
[ 蒸汽压 ]:
7E-10mmHg at 25°C
[ 储存条件 ]:
库房通风低温干燥
盐酸替诺立定毒性和生态
CHEMICAL IDENTIFICATION
- RTECS NUMBER :
- XJ9088600
- CHEMICAL NAME :
- Thieno(2,3-c)pyridine-3-carboxylic acid, 4,5,6,7-tetrahydro-2-amino-6-benzyl-, ethyl ester, hydrochloride
- CAS REGISTRY NUMBER :
- 25913-34-2
- LAST UPDATED :
- 199706
- DATA ITEMS CITED :
- 11
- MOLECULAR FORMULA :
- C17-H20-N2-O2-S.Cl-H
- MOLECULAR WEIGHT :
- 352.91
- WISWESSER LINE NOTATION :
- T56 BS HN&TJ CZ DVO2 H1R &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 :
- 1200 mg/kg
- TOXIC EFFECTS :
- Behavioral - tremor Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - respiratory depression
- REFERENCE :
- YKKZAJ Yakugaku Zasshi. Journal of Pharmacy. (Nippon Yakugakkai, 2-12-15 Shibuya, Shibuya-ku, Tokyo 150, Japan) No.1- 1881- Volume(issue)/page/year: 99,240,1979
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Intraperitoneal
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 1350 mg/kg
- TOXIC EFFECTS :
- Behavioral - altered sleep time (including change in righting reflex) Behavioral - ataxia
- REFERENCE :
- YKKZAJ Yakugaku Zasshi. Journal of Pharmacy. (Nippon Yakugakkai, 2-12-15 Shibuya, Shibuya-ku, Tokyo 150, Japan) No.1- 1881- Volume(issue)/page/year: 90,1439,1970
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Subcutaneous
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- >10200 mg/kg
- TOXIC EFFECTS :
- Skin and Appendages - dermatitis, other (after systemic exposure)
- REFERENCE :
- YKKZAJ Yakugaku Zasshi. Journal of Pharmacy. (Nippon Yakugakkai, 2-12-15 Shibuya, Shibuya-ku, Tokyo 150, Japan) No.1- 1881- Volume(issue)/page/year: 90,1439,1970
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 1601 mg/kg
- TOXIC EFFECTS :
- Details of toxic effects not reported other than lethal dose value
- 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: 2,1028,1974
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Intraperitoneal
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 510 mg/kg
- TOXIC EFFECTS :
- Behavioral - altered sleep time (including change in righting reflex) Behavioral - ataxia
- REFERENCE :
- YKKZAJ Yakugaku Zasshi. Journal of Pharmacy. (Nippon Yakugakkai, 2-12-15 Shibuya, Shibuya-ku, Tokyo 150, Japan) No.1- 1881- Volume(issue)/page/year: 90,1439,1970
- TYPE OF TEST :
- LD50 - Lethal dose, 50 percent kill
- ROUTE OF EXPOSURE :
- Subcutaneous
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- >10200 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: 6,463,1982 ** OTHER MULTIPLE DOSE TOXICITY DATA **
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 13580 mg/kg/2W-I
- TOXIC EFFECTS :
- Nutritional and Gross Metabolic - weight loss or decreased weight gain Related to Chronic Data - death
- REFERENCE :
- YKKZAJ Yakugaku Zasshi. Journal of Pharmacy. (Nippon Yakugakkai, 2-12-15 Shibuya, Shibuya-ku, Tokyo 150, Japan) No.1- 1881- Volume(issue)/page/year: 90,1447,1970
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Rodent - rat
- DOSE/DURATION :
- 12 gm/kg/4W-I
- TOXIC EFFECTS :
- Liver - changes in liver weight Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - phosphatases Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - transaminases
- REFERENCE :
- YKKZAJ Yakugaku Zasshi. Journal of Pharmacy. (Nippon Yakugakkai, 2-12-15 Shibuya, Shibuya-ku, Tokyo 150, Japan) No.1- 1881- Volume(issue)/page/year: 90,1439,1970
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- SPECIES OBSERVED :
- Rodent - mouse
- DOSE/DURATION :
- 26460 mg/kg/2W-I
- TOXIC EFFECTS :
- Nutritional and Gross Metabolic - weight loss or decreased weight gain Related to Chronic Data - death
- REFERENCE :
- YKKZAJ Yakugaku Zasshi. Journal of Pharmacy. (Nippon Yakugakkai, 2-12-15 Shibuya, Shibuya-ku, Tokyo 150, Japan) No.1- 1881- Volume(issue)/page/year: 90,1447,1970 ** REPRODUCTIVE DATA **
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- DOSE :
- 4900 mg/kg
- SEX/DURATION :
- female 9-14 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
- REFERENCE :
- YKKZAJ Yakugaku Zasshi. Journal of Pharmacy. (Nippon Yakugakkai, 2-12-15 Shibuya, Shibuya-ku, Tokyo 150, Japan) No.1- 1881- Volume(issue)/page/year: 90,1447,1970
- TYPE OF TEST :
- TDLo - Lowest published toxic dose
- ROUTE OF EXPOSURE :
- Oral
- DOSE :
- 600 mg/kg
- SEX/DURATION :
- female 7-12 day(s) after conception
- TOXIC EFFECTS :
- Reproductive - Effects on Newborn - weaning or lactation index (e.g., # alive at weaning per # alive at day 4)
- REFERENCE :
- YKKZAJ Yakugaku Zasshi. Journal of Pharmacy. (Nippon Yakugakkai, 2-12-15 Shibuya, Shibuya-ku, Tokyo 150, Japan) No.1- 1881- Volume(issue)/page/year: 90,1447,1970
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公司名：上海源溪生物科技有限公司
区域：上海市浦东新区
价格：
￥需询单/1g
联系人：赖经理
公司名：上海阿拉丁生化科技股份有限公司
区域：上海市浦东新区
价格：
￥1111.9/50mg
￥301.9/5mg
￥291.9/1ml
￥需询单/1g
联系人：阿拉丁李高志
产品详情：盐酸替诺立定
公司名：上海创赛科技有限公司
区域：上海市嘉定区
价格：
￥1780.0/10mg
￥1174.0/5mg
联系人：夏言
产品详情：[Perfemiker]Tinoridine hydrochloride,≥98%
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