29876-14-0

• 常用中文名：尼可曲多
• 常用英文名：Nicotredole
• CAS号：29876-14-0
• 分子式：C₁₆H₁₅N₃O
• 分子量：265.310
• 相关类别： 研究领域 炎症/免疫
• 发布时间：2018-05-17 08:00:00
• 更新时间：2024-01-09 11:57:01
• Nicotredole (Tryptamide) 是一种口服活性的消炎镇痛剂。Nicotredole 显示出与 Phenylbutazone 相当的明显抗炎作用。Nicotredole 仅具有弱的致溃疡活性。

名称

• 中文名: 尼可曲朵
• 英文名: N-[2-(1H-indol-3-yl)ethyl]pyridine-3-carboxamide
• 中文别名: 尼可曲多
• 英文别名: nicotredole; 3-Pyridinecarboxamide, N-[2-(1H-indol-3-yl)ethyl]-; Tryptamide; N-Nicotinoyltryptamide; N-[2-(1H-Indol-3-yl)ethyl]nicotinamide

物化性质

• 密度: 1.2±0.1 g/cm3
• 沸点: 588.4±35.0 °C at 760 mmHg
• 分子式: C₁₆H₁₅N₃O
• 分子量: 265.310
• 闪点: 309.7±25.9 °C
• 精确质量: 265.121521
• PSA: 57.78000
• LogP: 1.94
• 蒸汽压: 0.0±1.6 mmHg at 25°C
• 折射率: 1.669
• 储存条件: 室温，干燥

生物活性

• 描述: Nicotredole (Tryptamide) 是一种口服活性的消炎镇痛剂。Nicotredole 显示出与 Phenylbutazone 相当的明显抗炎作用。Nicotredole 仅具有弱的致溃疡活性。
• 相关类别:
  信号通路 >> 其他 >> 其他
  研究领域 >> 炎症/免疫
• 体外研究: 尼古曲多尔在体外抑制前列腺素合成酶活性[1]。
• 体内研究: 尼克tredole对角叉菜胶诱导的大鼠足肿胀产生抗炎作用[1]。尼可替多尔逆转热原诱导的大鼠体温升高,诱导大鼠镇痛作用,延长大鼠己巴比妥睡眠时间,抑制大鼠和小鼠的运动活动[1]。尼可曲多尔(i.p.)对雄性大鼠和雄性小鼠的LD50分别为1260 mg/kg和1980 mg/kg[1]。尼可曲多尔(p.o.)对雄性大鼠和雄性小鼠的LD50分别为8.5 g/kg和9.3 g/kg[1]。尼可替洛尔(25mg/kg；p.o.或i.p.)经历快速吸收(t1/2=4.92-17.5min)和消除(t1/2=55.72-74.52min),30min后可达到Cmax(11-13μg/cm3),AUC值在21.40-27.30(μg•h/cm3)[2]。
• 参考文献:

  [1]. Herman ZS, et, al. Basic pharmacological properties of a novel antiinflammatory drug tryptamide. Pol J Pharmacol Pharm. Nov-Dec 1987;39(6):729-36.

  [2]. Szumiło H. Pharmacokinetics of tryptamide following oral and intraperitoneal administration in rats. Acta Pol Pharm. 1990;47(1-2):19-22.

  [3]. Kulig D, et, al. A comparison of anti-inflammatory, analgesic and ulcerogenic action of tryptamide, ibuprofen and piroxicam. Pol J Pharmacol Pharm. Nov-Dec 1987;39(6):769-72.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : QS4476800 CHEMICAL NAME : Nicotinamide, N-(2-indol-3-ylethyl)- CAS REGISTRY NUMBER : 29876-14-0 BEILSTEIN REFERENCE NO. : 0242441 LAST UPDATED : 199612 DATA ITEMS CITED : 3 MOLECULAR FORMULA : C16-H15-N3-O MOLECULAR WEIGHT : 265.34 WISWESSER LINE NOTATION : T56 BMJ D2MV- CT6NJ HEALTH HAZARD DATA ACUTE TOXICITY DATA TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 1250 mg/kg TOXIC EFFECTS : Behavioral - somnolence (general depressed activity) REFERENCE : DPHFAK Dissertationes Pharmaceuticae et Pharmacologicae. (Warsaw, Poland) V.18-24, 1966-72. For publisher information, see PJPPAA. Volume(issue)/page/year: 22,313,1970 ** REPRODUCTIVE DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 90 mg/kg SEX/DURATION : female 6-14 day(s) after conception TOXIC EFFECTS : Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) REFERENCE : PJPPAA Polish Journal of Pharmacology and Pharmacy. (ARS Polona, POB 1001, 00-068 Warsaw 1, Poland) V.25- 1973- Volume(issue)/page/year: 39,779,1987 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 4500 mg/kg SEX/DURATION : female 6-14 day(s) after conception TOXIC EFFECTS : Reproductive - Effects on Embryo or Fetus - fetal death REFERENCE : PJPPAA Polish Journal of Pharmacology and Pharmacy. (ARS Polona, POB 1001, 00-068 Warsaw 1, Poland) V.25- 1973- Volume(issue)/page/year: 39,779,1987

安全

• 危害码 (欧洲): Xi

合成路线

59-67-6 61-54-1 ~% 29876-14-0

文献：Journal of the American Chemical Society, , vol. 126, # 40 p. 12897 - 12906

500-22-1 61-54-1 ~60% 29876-14-0

文献：Rodriguez-Lugo, Rafael E.; Trincado, Monica; Gruetzmacher, Hansjoerg ChemCatChem, 2013 , vol. 5, # 5 p. 1079 - 1083

61-54-1 20260-53-1 ~81% 29876-14-0

文献：Bodor; Farag; Polgar Journal of Pharmacy and Pharmacology, 2001 , vol. 53, # 6 p. 889 - 894

61-54-1 78348-28-4 ~62% 29876-14-0

文献：Lo, Kenneth Kam-Wing; Tsang, Keith Hing-Kit; Hui, Wai-Ki; Zhu, Nianyong Chemical Communications, 2003 , # 21 p. 2704 - 2705

10400-19-8 61-54-1 ~% 29876-14-0

文献：Canadian Journal of Research, Section B: Chemical Sciences, , vol. 24, p. 224,229

上下游产品

上游产品  6
59-67-6 61-54-1 500-22-1 20260-53-1
78348-28-4 10400-19-8
下游产品  0