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格列波脲

格列波脲用途

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。

格列波脲名称

[ CAS 号 ]:
26944-48-9

[ 中文名 ]:
克糖利

[ 英文名 ]:
Glibornuride

[中文别名 ]:

格列波脲

[英文别名 ]:

Ro 6-4563
Glibornurida [INN-Spanish]
Glibornuridum [INN-Latin]
EINECS 248-124-6
Glibornuride
Glutril
Ro 6-4563/8

格列波脲生物活性

[ 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.

格列波脲物理化学性质

[ 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

格列波脲毒性和生态

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