25913-34-2

• 常用中文名：盐酸替诺立定
• 常用英文名：Tinoridine hydrochloride
• CAS号：25913-34-2
• 分子式：C₁₇H₂₁ClN₂O₂S
• 分子量：352.87900
• 相关类别： 原料药 解热镇痛药 非甾抗炎药
• 发布时间：2018-07-15 16:42:52
• 更新时间：2024-01-11 16:01:45
• 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。

名称

• 中文名: 盐酸替诺立定
• 英文名: ethyl 2-amino-6-benzyl-4,5,6,7-tetrahydrothieno[2,3-c]pyridine-3-carboxylate monohydrochloride
• 中文别名: 2-氨基-6-苄基-4,5,6,7-四氢噻吩并[2,3-C]吡啶-3-甲酸乙酯盐酸盐
• 英文别名: Tinoridine Hydrochloride; Dimaten; Thieno(2,3-C)pyridine-3-carboxylic acid,4,5,6,7-tetrahydro-2-amino-6-benzyl-,ethyl ester,monohydrochloride; Tinoridine HCl; 2-Amino-3-ethoxycarbonyl-6-benzyl-4,5,6,7-tetrahydrothieno[2,3-c]pyridine hydrochloride; Tenocyclidine hydrochloride; 2-Amino-3-ethoxycarbonyl-6-benzyl-4,5,6,7-tetrahydrothieno(2,3-C)pyridine monohydrochloride; Nonflamin; Einecs 247-342-9

物化性质

• 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

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.

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