Loxiglumide

[Description]:

Loxiglumide is a cholecystokinin (CCK-1) receptor antagonist.

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Cholecystokinin Receptor

Research Areas >> Metabolic Disease

[Target]

CCK-1 receptor[1]

[In Vivo]

The effects of pancreatic rest by oral administration of CCK-1 receptor antagonist Loxiglumide and pancreas stimulation are investigated via endogenous CCK release induced by po protease inhibitor camostat on the recovery of pancreatic secretory function, and biochemical and histological changes of the pancreas after acute hemorrhagic pancreatitis. Oral administration of CCK-1 receptor antagonist Loxiglumide with a dose of 50 mg/kg body weight inhibits pancreatic exocrine secretion for more than 12 h. Thus, every 12-h administration of Loxiglumide might have completely blocks the effect of endogenously released CCK on the pancreas (pancreatic rest)[1].

[Animal admin]

Rats[1] At 24 h after induction of acute hemorrhagic pancreatitis, rats are divided into four different treatment groups: standard rat chow (AP-C); standard rat chow with pancreatic rest (AP-R); standard rat chow with pancreatic stimulation (AP-S); and standard rat chow with pancreatic rest, followed by pancreatic stimulation (AP-R/S). Rats in the AP-C group receive 2 mL/kg body weight saline orally (po) via an orogastric tube twice daily (09:00 and 21:00 h) for 10 d; the AP-R group receive 50 mg/kg body weight of CCK-1 receptor antagonist Loxiglumide dissolved in 2 mL distilled water po twice daily for 10 d; the AP-S group receive 25 mg/kg body weight protease inhibitor Camostat, which is known to stimulate endogenous CCK release, dissolved in 2 mL distilled water po twice daily for 10 d; and the AP-R/S group receive 50 mg/kg body weight Loxiglumide twice daily for the first 5 d followed by 25 mg/kg body weight camostat twice daily for the next 5 d. Rats are fed ad libitum. On day 12 at 24 h after the last treatment and overnight fasting, pancreatic exocrine function and histological examination of the pancreas are performed.

[References]

[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.

[Related Small Molecules]

[ Density]:
1.233g/cm3

[ Boiling Point ]:
632.2ºC at 760mmHg

[ Molecular Formula ]:
C₂₁H₃₀Cl₂N₂O₅

[ Molecular Weight ]:
461.37900

[ Flash Point ]:
336.1ºC

[ Exact Mass ]:
460.15300

[ PSA ]:
95.94000

[ LogP ]:
4.40280

[ Appearance of Characters ]:
off white solid

[ Vapour Pressure ]:
7.51E-17mmHg at 25°C

[ Index of Refraction ]:
1.537

[ Storage condition ]:
-20℃

Click to get detail MSDS

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

[ Symbol ]:

GHS07

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H302

[ RIDADR ]:
NONH for all modes of transport

[ HS Code ]:
2924299090

[ HS Code ]: 2924299090

[ 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%

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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