Loxiglumide - CAS 107097-80-3
Catalog number: 107097-80-3
Category: Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C21H30Cl2N2O5
Molecular Weight:
461.38
COA:
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Targets:
Cholecystokinin A(CCKA)
Description:
Loxiglumide is an orally active, potent and selective small-molecule antagonist of the cholecystokinin receptor CCKA. It stimulates calorie intake and hunger feelings in humans. It could antagonize the CCK-induced reduction of gastric emptying in rats, accelerate the intestinal transport and accelerate the gallbladder emptying in mice. It inhibits pancreatic secretion of digestive enzymes, and also blocks CCK-induced gastric secretions and emptying.
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Purity:
95%
Appearance:
White to beige powder
Synonyms:
D,L-4-(3,4-dichlorobenzoylamino)-5-(n-3-methoxypropylpentylamino)-5-oxo-pentanoicacid;Pentanoicacid,4-((3,4-dichlorobenzoyl)amino)-5-((3-methoxypropyl)pentylamino);CR-1505;CR1505;4-(3,4-Dichlorobenzamido)-5-((3-methoxypropyl)(pentyl)amino)-5-oxopentanoic acid
Solubility:
DMSO: ≥5 mg/mL
Storage:
2-8°C
MSDS:
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Application:
Loxiglumide stimulates calorie intake and hunger feelings in humans. It inhibits pancreatic secretion of digestive enzymes.
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Quantity:
Grams to Kilograms
Boiling Point:
632.2±55.0 °C | Condition: Press: 760 Torr
Melting Point:
113-115 °C
Density:
1.233±0.06 g/cm3 | Condition: Temp: 20 °C Press: 760 Torr
InChIKey:
QNQZBKQEIFTHFZ-UHFFFAOYSA-N
InChI:
InChI=1S/C21H30Cl2N2O5/c1-3-4-5-11-25(12-6-13-30-2)21(29)18(9-10-19(26)27)24-20(28)15-7-8-16(22)17(23)14-15/h7-8,14,18H,3-6,9-13H2,1-2H3,(H,24,28)(H,26,27)
Canonical SMILES:
CCCCCN(CCCOC)C(=O)C(CCC(=O)O)NC(=O)C1=CC(=C(C=C1)Cl)Cl
1.Modulation of acetylcholine release by cholecystokinin in striatum: receptor specificity; role of dopaminergic neuronal activity.
Petkova-Kirova P1, Giovannini MG, Kalfin R, Rakovska A. Brain Res Bull. 2012 Dec 1;89(5-6):177-84. doi: 10.1016/j.brainresbull.2012.08.009. Epub 2012 Sep 5.
Cholecystokinin, a neuroactive peptide functioning as a neurotransmitter and neuromodulator in the central nervous system, mediates a number of processes and is implicated in neurological and psychiatric disorders such as Parkinson's disease, anxiety and schizophrenia. Striatum is one of the brain structures with the highest concentrations of CCK in the brain, rich in CCK receptors as well. The physiological effect of CCK on cholinergic interneurons, which are the major interneurons in striatum and the modulatory interactions which exist between dopamine, acetylcholine and cholecystokinin in this brain structure are still unclear. We studied the effect of cholecystokinin octapeptide (CCK-8) on the release of acetylcholine (ACh) from striatal slices of the rat brain. CCK-8 (0.01-0.1μM) showed no statistically significant effect on the basal but enhanced dose-dependently the electrically (2Hz)-evoked release of [(3)H]ACh. When slices were preperfused with 100μM sulpiride, a selective dopamine D(2) receptor antagonist, the CCK-8 (0.
2.CCK1 receptor antagonist, dexloxiglumide: effects on human isolated gallbladder. Potential clinical applications.
Maselli MA1, Mennuni L. Minerva Gastroenterol Dietol. 2003 Sep;49(3):211-6.
Cholecystokinin is the main hormonal regulator of gallbladder motility. Dexloxiglumide, the active enantiomer of loxiglumide, interacts competitively with CCK1 receptors as determined in preclinical studies, such as specific radioligand binding assays or functional studies on isolated guinea pig gallbladder, where it inhibited smooth muscle cell contractions induced by cholecystokinin-octapeptide (CCK-8), the most prominent active forms of cholecystokinin. Dexloxiglumide has a potent antagonistic effect, of a competitive nature, on human gallbladder cholecystokinin type 1 receptors. In isolated human gallbladder, dexloxiglumide produced a concentration-dependent rightward shift of the cholecystokinin-octapeptide curve, without affecting its maximal response. Gallbladder motility was evaluated in clinical studies. Dexloxiglumide, orally administered to healthy volunteers at putative therapeutic doses, did not interfere with post-prandial gallbladder kinetics, despite an increase of fasting gallbladder volume.
3.The effects on diet, anastomotic type, and loxiglumide on gastric emptying following gastrojejunostomy.
Yucel T1, Gonullu D, Orhan Gurer A, Duzman R, Nihat Koksoy F, Yilmaz N, Sit M. Int J Surg. 2009 Apr;7(2):163-7. doi: 10.1016/j.ijsu.2009.01.010. Epub 2009 Feb 13.
PURPOSE: The effects on gastric emptying of feeding with a normal diet (ND), an early high-calorie and hyperosmolar diet (HCHOD) or normal diet plus intraperitoneal loxiglumide (LOX) were investigated in rats with antecolic (ACGJ) or retrocolic (RCGJ) gastrojejunostomy.
4.Mechanism of action of cholecystokinin on colonic motility in isolated, vascularly perfused rat colon.
Ko BS1, Han JH, Jeong JI, Chae HB, Park SM, Youn SJ, Lee KY. J Neurogastroenterol Motil. 2011 Jan;17(1):73-81. doi: 10.5056/jnm.2011.17.1.73. Epub 2011 Jan 26.
BACKGROUND/AIMS: It is generally believed that cholecystokinin (CCK) stimulates colonic motility, although there are controversial reports. It has also been suggested that postprandial peptide YY (PYY) release is CCK-dependent. Using a totally isolated, vascularly perfused rat colon, we investigated: (1) the roles of CCK and PYY on colonic motility, (2) to determine if CCK modulates PYY release from the colon to influence the motility and (3) to clarify whether the action of CCK and PYY on colonic motility is mediated via the influence of cholinergic input.
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