Lorglumid (CR-1409) je lek koji inhibira gastrointestinalnu motilnost i redukuje želudačnu sekreciju. On deluje kao holecistokininski antagonist,[4] koji je u znatnoj meri selektivan za CCKA tip receptora.[5] Smatralo se da on može da služi kao potencijalni lek za niz gastrointestinalnih problema, među kojima su čir na dvanaestopalačnom crevu, upalna bolest creva, dispepsija, konstipacija i pankreatitis, kao i neke forme raka, ali su ispitivanja na životinjama i ljudima proizvela nedosledne rezultate i jasna terapeutska uloga nije uspostavljena. On je u širokoj upotrebi u naučnim istraživanjima.[6][7][8][9]
Lorglumid
|
| (IUPAC) ime
|
| N2-(3,4-dichlorobenzoyl-N,N-dipentyl-α-glutamine
|
| Klinički podaci
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| Identifikatori
|
| CAS broj
|
97964-56-2
|
| ATC kod
|
nije dodeljen
|
| PubChem[1][2]
|
3960
|
| ChEMBL[3]
|
CHEMBL24938
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| Hemijski podaci
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| Formula
|
C22H32Cl2N2O4
|
| Mol. masa
|
459.406 g/mol
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| SMILES
|
eMolekuli & PubHem
|
| InChI |
|---|
InChI=1S/C22H32Cl2N2O4/c1-3-5-7-13-26(14-8-6-4-2)22(30)19(11-12-20(27)28)25-21(29)16-9-10-17(23)18(24)15-16/h9-10,15,19H,3-8,11-14H2,1-2H3,(H,25,29)(H,27,28)  Y
Key: IEKOTSCYBBDIJC-UHFFFAOYSA-N Y |
|
| Sinonimi
|
4-[(3,4-dichlorobenzoyl)amino]-5-(dipentylamino)-5-oxopentanoic acid
|
| Farmakoinformacioni podaci
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| Trudnoća
|
?
|
| Pravni status
|
|
Literatura
uredi
- ↑ Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519. edit
- ↑ Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1.
- ↑ Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP. (2012). „ChEMBL: a large-scale bioactivity database for drug discovery”. Nucleic Acids Res 40 (Database issue): D1100-7. DOI:10.1093/nar/gkr777. PMID 21948594. edit
- ↑ Makovec F, Bani M, Cereda R, Chisté R, Pacini MA, Revel L, Rovati LA, Rovati LC, Setnikar I. Pharmacological properties of lorglumide as a member of a new class of cholecystokinin antagonists. Arzneimittelforschung. 1987 Nov;37(11):1265-8. PMID 3440035
- ↑ González-Puga C, García-Navarro A, Escames G, León J, López-Cantarero M, Ros E, Acuña-Castroviejo D. Selective CCK-A but not CCK-B receptor antagonists inhibit HT-29 cell proliferation: synergism with pharmacological levels of melatonin. Journal of Pineal Research. 2005 Oct;39(3):243-50. DOI 10.1111/j.1600-079X.2005.00239.x PMID 16150104
- ↑ de Tullio P, Delarge J, Pirotte B. Recent advances in the chemistry of cholecystokinin receptor ligands (agonists and antagonists). Current Medicinal Chemistry. 1999 Jun;6(6):433-55. PMID 10213792
- ↑ de Tullio P, Delarge J, Pirotte B. Therapeutic and chemical developments of cholecystokinin receptor ligands. Expert Opinion on Investigational Drugs. 2000 Jan;9(1):129-46. PMID 11060666
- ↑ Herranz R. Cholecystokinin antagonists: pharmacological and therapeutic potential. Medical Research Reviews. 2003 Sep;23(5):559-605. PMID 12789687
- ↑ Berna MJ, Tapia JA, Sancho V, Jensen RT. Progress in developing cholecystokinin (CCK)/gastrin receptor ligands that have therapeutic potential. Current Opinion in Pharmacology. 2007 Dec;7(6):583-92. PMID 17997137
