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氯谷胺

氯谷胺用途

Loxiglumide 是缩胆囊素 (CCK-1) 受体拮抗剂。

氯谷胺名称

[ CAS 号 ]:
107097-80-3

[ 中文名 ]:
氯谷胺

[ 英文名 ]:
Loxiglumide

[英文别名 ]:

Loxiglumide
LOXIGLUMIDE
Loxizin
CR-1505

氯谷胺生物活性

[ 描述 ]:

Loxiglumide 是缩胆囊素 (CCK-1) 受体拮抗剂。

[ 相关类别 ]:

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 >> 代谢疾病

[ 靶点 ]

CCK-1 receptor[1]

[体内研究]

通过口服CCK-1受体拮抗剂Loxiglumide和胰腺刺激对胰腺休息的影响通过po蛋白酶抑制剂camostat诱导的内源性CCK释放对胰腺分泌功能的恢复以及急性出血性胰腺炎后胰腺的生化和组织学变化进行了研究。。口服施用剂量为50mg/kg体重的CCK-1受体拮抗剂Loxiglumide抑制胰腺外分泌超过12小时。因此,每12小时施用Loxiglumide可能完全阻断内源性释放的CCK对胰腺的影响(胰腺休息)[1]。

[动物实验]

大鼠[1]在诱导急性出血性胰腺炎后24小时，将大鼠分成四个不同的治疗组：标准大鼠食物（AP-C）;标准大鼠食物与胰腺休息（AP-R）;标准大鼠食物与胰腺刺激（AP-S）;和标准的大鼠食物，胰腺休息，然后胰腺刺激（AP-R / S）。 AP-C组大鼠每天两次（09:00和21:00）通过口胃管口服（po）2mL / kg体重的盐水，持续10天; AP-R组每天两次接受50 mg / kg体重的CCK-1受体拮抗剂Loxiglumide溶于2 mL蒸馏水中10 d; AP-S组接受25mg / kg体重的蛋白酶抑制剂Camostat，已知其刺激内源性CCK释放，每天两次溶于2mL蒸馏水中，持续10天;并且AP-R / S组在前5天每天两次接受50mg / kg体重的Loxiglumide，然后在接下来的5天每天两次接受25mg / kg体重的camostat。随意喂养大鼠。在最后一次治疗后24小时和禁食过夜的第12天，进行胰腺外分泌功能和胰腺的组织学检查。

[参考文献]

[1]. Jia D, et al. Effect of endogenous cholecystokinin on the course of acute pancreatitis in rats. World J Gastroenterol. 2015 Jul 7;21(25):7742-53.

[相关活性小分子]

氯谷胺物理化学性质

[ 密度 ]:
1.233g/cm3

[ 沸点 ]:
632.2ºC at 760mmHg

[ 分子式 ]:
C₂₁H₃₀Cl₂N₂O₅

[ 分子量 ]:
461.37900

[ 闪点 ]:
336.1ºC

[ 精确质量 ]:
460.15300

[ PSA ]:
95.94000

[ LogP ]:
4.40280

[ 外观性状 ]:
off white solid

[ 蒸汽压 ]:
7.51E-17mmHg at 25°C

[ 折射率 ]:
1.537

[ 储存条件 ]:
-20℃

氯谷胺MSDS

详细MSDS(安全技术说明书)

氯谷胺毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: SA3680800

CHEMICAL NAME :: Pentanoic acid, 4-((3,4-dichlorobenzoyl)amino)-5-((3-methoxypropyl)pe ntylamino)-5-oxo-, (+-)-

CAS REGISTRY NUMBER :: 107097-80-3

LAST UPDATED :: 199607

DATA ITEMS CITED :: 4

MOLECULAR FORMULA :: C21-H30-Cl2-N2-O5

MOLECULAR WEIGHT :: 461.43

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 460 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: JSONAU Journal of Surgical Oncology. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1969- Volume(issue)/page/year: 53,47,1993

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

ROUTE OF EXPOSURE :: Intraperitoneal

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 450 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: JSONAU Journal of Surgical Oncology. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1969- Volume(issue)/page/year: 53,47,1993

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 500 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: JSONAU Journal of Surgical Oncology. (Alan R. Liss, Inc., 41 E. 11th St., New York, NY 10003) V.1- 1969- Volume(issue)/page/year: 53,47,1993

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 396 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: USXXAM United States Patent Document. (U.S. Patent Office, Box 9, Washington, DC 20231) Volume(issue)/page/year: #4769389

氯谷胺安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302

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

[ 海关编码 ]:
2924299090

氯谷胺海关

[ 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%

氯谷胺文献

Involvement of capsaicin-sensitive afferent nerves and cholecystokinin 2/gastrin receptors in gastroprotection and adaptation of gastric mucosa to Helicobacter pylori-lipopolysaccharide.

J. Pharmacol. Exp. Ther. 310(1) , 116-25, (2004)

Lipopolysaccharide (LPS) is one of the virulence factors in the Helicobacter pylori (Hp)-infected stomach, but it remains unknown whether single and prolonged pretreatment with Hp-LPS can affect the c...

Effect of cholecystokinin-A receptor blockade on postprandial insulinaemia and gastric emptying in humans.

Neurogastroenterol. Motil. 14(5) , 519-25, (2002)

Our aim was determine the relationship between cholecystokinin (CCK)-A receptor blockade, glucose levels, insulin secretion and gastric emptying in humans, and to assess the effect of CCK-A blockade o...

Stimulatory effect of N-methyltyramine, a congener of beer, on pancreatic secretion in conscious rats.

Alcohol. Clin. Exp. Res. 34 Suppl 1 , S14-7, (2010)

Alcoholic beverages stimulate gastric acid secretion and increase the appetite. Although ingested ethanol stimulates pancreatic secretion, alcoholic beverages contain several congeners. N-methyltyrami...

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氯谷胺