Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C21H30Cl2N2O5 |
Molecular Weight | 461.379 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 1 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
CCCCCN(CCCOC)C(=O)[C@@H](CCC(O)=O)NC(=O)C1=CC(Cl)=C(Cl)C=C1
InChI
InChIKey=QNQZBKQEIFTHFZ-GOSISDBHSA-N
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)/t18-/m1/s1
DescriptionSources: https://www.drugbank.ca/drugs/DB04856
Sources: https://www.drugbank.ca/drugs/DB04856
Dexloxiglumide is a selective antagonist of cholecystokinin receptor A (CCKA, CCK1). It is the dextro isomeric form of loxiglumide, Dexloxiglumide was investigated for treatment of irritable bowel syndrome. Its development in USA was discontinued.
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: P32238 Gene ID: 886.0 Gene Symbol: CCKAR Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/17684117 |
7.53 null [pKi] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
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Primary | Unknown Approved UseUnknown |
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Primary | Unknown Approved UseUnknown |
PubMed
Title | Date | PubMed |
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Effect of three nonpeptide cholecystokinin antagonists on human isolated gallbladder. | 2001 Dec |
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Development and validation of a bioanalytical method for the determination of the cholecystokinin type-1 (CCK(1)) receptor antagonist dexloxiglumide in human plasma. | 2003 Jan 25 |
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Absorption, distribution, metabolism and excretion of the cholecystokinin-1 antagonist dexloxiglumide in the rat. | 2003 Jul-Sep |
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Effect of multiple-dose dexloxiglumide on the pharmacokinetics of oral contraceptives in healthy women. | 2005 Mar |
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Pharmacokinetic profile of dexloxiglumide. | 2006 |
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Regulation of fat-stimulated neurotensin secretion in healthy subjects. | 2008 May |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/27590736
In phase 2 clinical trials for treatment of constipation predominant irritable bowel syndrome dexloxiglumide was administered at doses 200 mg tid.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/17684117
Binding of dexloxiglumide to cholecystokinin receptor 1 (CCK1) was studied using radioligand binding assay. CHO cells were transfected with CCK1. Cell membanes rere incubated with 60 pM 125I-BH-CCK-8S (Bolton Hunter-sulfated cholecystokinin octapeptide), and treated with varying concentration of dexloxiglumide. The bound radioactivity was separated by filtration, and radioactivity retained on the filters was measured by liquid scintillation counting.
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Classification Tree | Code System | Code | ||
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NCI_THESAURUS |
C29701
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NCI_THESAURUS |
C28197
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C96871
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C103490
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DEXLOXIGLUMIDE
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DB04856
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m6916
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119817-90-2
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SUB07036MIG
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CHEMBL550781
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65937
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100000083408
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6782
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69DY40RH9B
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DTXSID50152604
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834
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ACTIVE MOIETY