26944-48-9

• 常用中文名：格列波脲
• 常用英文名：Glibornuride
• CAS号：26944-48-9
• 分子式：C₁₈H₂₆N₂O₄S
• 分子量：366.47500
• 相关类别： 原料药 激素及调节内分泌功能类药 胰腺激素及其它调节血糖药
• 发布时间：2018-03-23 08:00:00
• 更新时间：2024-01-09 17:49:28
• Glibornuride 是一种对 ATP 敏感的 K+ 通道 (KATP 通道) 阻滞剂,pKi 值为 5.75。Glibornuride 是一种抗糖尿病剂。

名称

• 中文名: 克糖利
• 英文名: 1-(3-hydroxy-4,7,7-trimethyl-2-bicyclo[2.2.1]heptanyl)-3-(4-methylphenyl)sulfonylurea
• 中文别名: 格列波脲
• 英文别名: Ro 6-4563; endo,endo-1-((1R)-(2-Hydroxy-3-bornyl))-3-(p-tolylsulfonyl)urea; 1-((1R)-2endo-hydroxy-bornan-3endo-yl)-3-(toluene-4-sulfonyl)-urea; Glibornurida [INN-Spanish]; 1-(p-Tolylsulfonyl)-3-(2-endo-hydroxy-3-endo-L-bornyl)harnstoff; Glibornuridum [INN-Latin]; EINECS 248-124-6; Glibornuride; Glutril; 1-((1R)-2-endo-Hydroxy-3-endo-bornyl)-3-(p-tolylsulfonyl)urea; 1-(p-Tolylsulfonyl)-3-(2-endo-hydroxy-3-endo-D-bornyl)harnstoff; Ro 6-4563/8

物化性质

• 密度: 1.3g/cm3
• 熔点: 192-195° (ethanol-water); also reported as 195-198°
• 分子式: C₁₈H₂₆N₂O₄S
• 分子量: 366.47500
• 精确质量: 366.16100
• PSA: 107.37000
• LogP: 3.84460
• 外观性状: 白色固体
• 折射率: 1.6
• 储存条件: 室温

生物活性

• 描述: Glibornuride 是一种对 ATP 敏感的 K+ 通道 (KATP 通道) 阻滞剂,pKi 值为 5.75。Glibornuride 是一种抗糖尿病剂。
• 相关类别:
  研究领域 >> 代谢疾病
  信号通路 >> 跨膜转运 >> 钾通道
• 靶点:

  pKi: 5.75 (KATP channel)[1]

• 体内研究: 给予格列本脲(5 mg/kg；灌胃,每天28天)28天,导致瑞士白化大鼠糖尿病组体重增加[2]。格列本脲治疗28天可降低糖尿病大鼠血清尿酸水平[2]。给予格列本脲28天,对糖尿病大鼠肝脏脂质过氧化水平无显著影响[2]。动物模型：6-6.5月龄雄性瑞士大白鼠,体重150-200g[2]剂量：5mg/kg给药：灌胃给药,每日28天结果：给药28天引起糖尿病组体重增加。治疗28天可降低糖尿病大鼠血清尿酸水平。
• 参考文献:

  [1]. Löffler C, et al. Pharmacological characterization of the sulphonylurea receptor in rat isolated aorta. Br J Pharmacol. 1997 Feb;120(3):476-80.

  [2]. Ozsoy-Sacan O, et al. Effects of parsley (Petroselinum crispum) extract versus Glibornuride on the liver of streptozotocin-induced diabetic rats. J Ethnopharmacol. 2006 Mar 8;104(1-2):175-81.

毒性和生态

CHEMICAL IDENTIFICATION RTECS NUMBER : YT4902000 CHEMICAL NAME : Urea, 1-(2-hydroxy-3-bornyl)-3-(p-tolylsulfonyl)-, (1R,2R,3S,4S)- CAS REGISTRY NUMBER : 26944-48-9 LAST UPDATED : 199612 DATA ITEMS CITED : 12 MOLECULAR FORMULA : C18-H26-N2-O4-S MOLECULAR WEIGHT : 366.52 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 : 18 gm/kg TOXIC EFFECTS : Behavioral - ataxia Lungs, Thorax, or Respiration - respiratory depression Kidney, Ureter, Bladder - urine volume increased REFERENCE : KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 6,1925,1972 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 1360 mg/kg TOXIC EFFECTS : Behavioral - somnolence (general depressed activity) Behavioral - ataxia Lungs, Thorax, or Respiration - respiratory depression REFERENCE : KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 6,1925,1972 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 10800 mg/kg TOXIC EFFECTS : Behavioral - somnolence (general depressed activity) Lungs, Thorax, or Respiration - respiratory depression Kidney, Ureter, Bladder - urine volume increased REFERENCE : KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 6,1925,1972 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : >20 gm/kg TOXIC EFFECTS : Behavioral - convulsions or effect on seizure threshold Behavioral - antipsychotic REFERENCE : KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 6,1925,1972 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Intraperitoneal SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 1530 mg/kg TOXIC EFFECTS : Behavioral - ataxia Lungs, Thorax, or Respiration - cyanosis Kidney, Ureter, Bladder - urine volume increased REFERENCE : KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 6,1925,1972 TYPE OF TEST : LD50 - Lethal dose, 50 percent kill ROUTE OF EXPOSURE : Subcutaneous SPECIES OBSERVED : Rodent - mouse DOSE/DURATION : 20 gm/kg TOXIC EFFECTS : Lungs, Thorax, or Respiration - dyspnea REFERENCE : KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 6,1925,1972 ** OTHER MULTIPLE DOSE TOXICITY DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 109 gm/kg/78W-C TOXIC EFFECTS : Brain and Coverings - changes in brain weight REFERENCE : ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 22,2188,1972 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 67 gm/kg/30D-I TOXIC EFFECTS : Behavioral - muscle weakness Kidney, Ureter, Bladder - other changes Nutritional and Gross Metabolic - weight loss or decreased weight gain REFERENCE : KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 6,1930,1972 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral SPECIES OBSERVED : Rodent - rat DOSE/DURATION : 390 gm/kg/26W-I TOXIC EFFECTS : Liver - changes in liver weight Kidney, Ureter, Bladder - changes in bladder weight Nutritional and Gross Metabolic - weight loss or decreased weight gain REFERENCE : KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 6,1943,1972 ** REPRODUCTIVE DATA ** TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 70 mg/kg SEX/DURATION : female 7-13 day(s) after conception TOXIC EFFECTS : Reproductive - Effects on Embryo or Fetus - extra-embryonic structures (e.g., placenta, umbilical cord) Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain) REFERENCE : KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 6,1969,1972 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 90 mg/kg SEX/DURATION : female 8-16 day(s) after conception TOXIC EFFECTS : Reproductive - Effects on Embryo or Fetus - extra-embryonic structures (e.g., placenta, umbilical cord) REFERENCE : KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 6,1983,1972 TYPE OF TEST : TDLo - Lowest published toxic dose ROUTE OF EXPOSURE : Oral DOSE : 2250 mg/kg SEX/DURATION : female 8-16 day(s) after conception TOXIC EFFECTS : Reproductive - Specific Developmental Abnormalities - musculoskeletal system REFERENCE : KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 6,1983,1972