丙谷胺钠盐

丙谷胺钠盐用途

Proglumide sodium 是一种非肽和口服活性胆囊收缩素 (CCK)-A/B 受体拮抗剂。Proglumide sodium 选择性阻断 CCK 在中枢神经系统中的作用。Proglumide sodium 具有抑制胃分泌和保护胃十二指肠粘膜的能力,还具有抗癫痫和抗氧化活性。

丙谷胺钠盐名称

[ CAS 号 ]:
99247-33-3

[ 中文名 ]:
丙谷胺

[ 英文名 ]:
Proglumide sodium salt

[英文别名 ]:

Proglumide sodium salt
Proglumide sodium

丙谷胺钠盐生物活性

[ 描述 ]:

[ 相关类别 ]:

研究领域 >> 癌症

研究领域 >> 内分泌

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 胆囊收缩素受体

研究领域 >> 神经疾病

[ 靶点 ]

Cholecystokinin (CCK)-A/B receptors[1][2]

[体外研究]

在体外研究中,0.3-10 mM浓度的丙谷胺对CCK刺激的淀粉酶释放具有剂量依赖性抑制作用,而0-3 mM浓度的丙谷胺对基础淀粉酶释放无影响。随着丙谷胺浓度的增加,CCK对淀粉酶释放的剂量-反应曲线右移。丙谷胺的这种抑制作用是可逆的。此外,丙谷胺对CCK及其相关肽具有选择性作用[2]。用丙谷胺孵育HT29细胞可显著减少[3H]-胸腺嘧啶核苷以剂量依赖的方式掺入HT29细胞,IC50为6.5mm。丙谷胺以剂量依赖的方式减少坏死的百分比,同时细胞凋亡增加到70%[3]。

[体内研究]

丙谷胺(250~750毫克/公斤；腹腔注射；成年雄性Sprague Dawley大鼠)治疗对改善癫痫活动、认知功能障碍和脑氧化应激有显著的效果(1)。动物模型：成年雄性Sprague-Dawley大鼠(200-250 g；2个月龄)诱发癫痫持续状态(SE)[1]剂量：250 mg/kg、500 mg/kg和750 mg/kg给药：腹腔注射结果：剂量依赖性,显著增加癫痫发作和SE的潜伏期。显著和剂量依赖性地减弱Li-PC(SE)诱导的海马和纹状体硫代巴比妥酸(TBARS)和过氧化氢酶(CAT)的升高,减弱Li-PC诱导的超氧化物歧化酶(SOD)的降低,以及GSH和谷胱甘肽-S转移酶(GST)的耗竭。

[参考文献]

[1]. Ahmad M, et al. The effects of quinacrine, proglumide, and pentoxifylline on seizure activity, cognitive deficit, and oxidative stress in rat lithium-pilocarpine model of status epilepticus. Oxid Med Cell Longev. 2014;2014:630509.

[2]. Iwamoto Y, et al. In vitro and in vivo effect of proglumide on cholecystokinin-stimulated amylase release in mouse pancreatic acini. Gastroenterol Jpn. 1984 Feb;19(1):53-8.

[3]. González-Puga C, et al. Selective CCK-A but not CCK-B receptor antagonists inhibit HT-29 cell proliferation: synergism with pharmacological levels of melatonin. J Pineal Res. 2005 Oct;39(3):243-50.

[4]. Bunney BS, et al. Further studies on the specificity of proglumide as a selective cholecystokinin antagonist in the central nervous system. Ann N Y Acad Sci. 1985;448:345-51.

[5]. Tariq M, et al. Gastric and duodenal antiulcer and cytoprotective effects of proglumide in rats. J Pharmacol Exp Ther. 1987 May;241(2):602-7.

丙谷胺钠盐物理化学性质

[ 分子式 ]:
C₁₈H₂₅N₂NaO₄

[ 分子量 ]:
356.39200

[ 精确质量 ]:
356.17100

[ PSA ]:
93.03000

[ LogP ]:
1.53850

[ 储存条件 ]:
2-8°C，干燥，充氩

丙谷胺钠盐MSDS

详细MSDS(安全技术说明书)

丙谷胺钠盐毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: MA2815000

CHEMICAL NAME :: Glutaramic acid, 4-benzamido-N,N-dipropyl-, sodium salt, dl-

CAS REGISTRY NUMBER :: 99247-33-3

LAST UPDATED :: 198806

DATA ITEMS CITED :: 7

MOLECULAR FORMULA :: C18-H25-N2-O4.Na

MOLECULAR WEIGHT :: 356.44

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 :: 8200 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - respiratory depression Kidney, Ureter, Bladder - hematuria

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 5,203,1971

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 2360 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - respiratory depression Kidney, Ureter, Bladder - hematuria

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 5,203,1971

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 6110 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - respiratory depression Kidney, Ureter, Bladder - hematuria

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 5,203,1971

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 8900 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - respiratory depression Kidney, Ureter, Bladder - hematuria

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 5,203,1971

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 2811 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - respiratory depression Kidney, Ureter, Bladder - hematuria

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 5,203,1971

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 5886 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - respiratory depression Kidney, Ureter, Bladder - hematuria

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 5,203,1971

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 2968 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - respiratory depression Kidney, Ureter, Bladder - hematuria

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 5,203,1971

丙谷胺钠盐安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
3

[ 海关编码 ]:
2924299090

丙谷胺钠盐海关

[ 海关编码 ]: 2924299090

[ 中文概述 ]:
2924299090. 其他环酰胺（包括环氨基甲酸酯）（包括其衍生物以及他们的盐）. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:30.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 包装

[ Summary ]:
2924299090. other cyclic amides (including cyclic carbamates) and their derivatives; salts thereof. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:30.0%

丙谷胺钠盐文献

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丙谷胺钠盐

丙谷胺钠盐用途

丙谷胺钠盐名称

丙谷胺钠盐生物活性

丙谷胺钠盐物理化学性质

丙谷胺钠盐MSDS

详细MSDS(安全技术说明书)

丙谷胺钠盐毒性和生态

CHEMICAL IDENTIFICATION

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

丙谷胺钠盐安全信息

丙谷胺钠盐海关

丙谷胺钠盐文献

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丙谷胺 钠盐

丙谷胺 钠盐用途

丙谷胺 钠盐名称

丙谷胺 钠盐生物活性

丙谷胺 钠盐物理化学性质

丙谷胺 钠盐MSDS

详细MSDS(安全技术说明书)

丙谷胺 钠盐毒性和生态

CHEMICAL IDENTIFICATION

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

丙谷胺 钠盐安全信息

丙谷胺 钠盐海关

丙谷胺 钠盐文献

推荐生产厂家/供应商：

热门化合物

丙谷胺钠盐

丙谷胺钠盐用途

丙谷胺钠盐名称

丙谷胺钠盐生物活性

丙谷胺钠盐物理化学性质

丙谷胺钠盐MSDS

丙谷胺钠盐毒性和生态

丙谷胺钠盐安全信息

丙谷胺钠盐海关

丙谷胺钠盐文献