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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。
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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 ]:

丙谷胺 钠盐生物活性

[ 描述 ]:

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。

[ 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
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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

Flavonoids from Sideritis Species: Human Monoamine Oxidase (hMAO) Inhibitory Activities, Molecular Docking Studies and Crystal Structure of Xanthomicrol.

Molecules 20 , 7454-73, (2015)

The inhibitory effects of flavonoids on monoamine oxidases (MAOs) have attracted great interest since alterations in monoaminergic transmission are reported to be related to neurodegenerative diseases...

Inhibition of LSD1 reduces herpesvirus infection, shedding, and recurrence by promoting epigenetic suppression of viral genomes.

Sci. Transl. Med. 6(265) , 265ra169, (2014)

Herpesviruses are highly prevalent and maintain lifelong latent reservoirs, thus posing challenges to the control of herpetic disease despite the availability of antiviral pharmaceuticals that target ...

Selective monoamine oxidase B inhibition by an Aphanizomenon flos-aquae extract and by its constitutive active principles phycocyanin and mycosporine-like amino acids.

Phytomedicine 21(7) , 992-7, (2014)

Aphanizomenon flos-aquae (AFA) is a fresh water unicellular blue-green alga that has been traditionally used for over 25 years for its health-enhancing properties. Recent studies have shown the abilit...


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价格：

联系人：徐经理

产品详情：丙谷胺钠

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价格：
￥需询单/1g

联系人：赖经理

产品详情：Proglumide sodium

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￥589.0/100mg ￥649.0/1g ￥需询单/1g ￥需询单/1g

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产品详情：Proglumide sodium salt

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价格：
￥401.9/50mg ￥556.9/100mg ￥2224.9/500mg ￥需询单/1g

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产品详情：丙谷酸钠

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￥588.0/100mg ￥需询单/1ml

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产品详情：Proglumide sodium salt

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