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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 ]:

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 ]:

研究领域 >> 炎症/免疫

[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]

[1]. O Shimada, et al. Hydroxyl radical scavenging action of tinoridine. Agents Actions. 1986 Nov;19(3-4):208-14.

[2]. Yasuda H, et al. The protective effect of tinoridine against carbon tetrachloride hepatotoxicity. Toxicol Appl Pharmacol. 1980 Mar 15;52(3):407-13.


[相关活性小分子]

RSL3 1S,3R- | AZD5904 | PF-06282999 | AZD3241

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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产品详情：2-氨基-6-苄基-4,5,6,7-四氢噻吩并[2,3-c]吡啶-3-羧酸乙酯盐酸盐

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

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产品详情：Tinoridine hydrochloride

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

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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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