Lorglumide
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| Other names | 4-[(3,4-dichlorobenzoyl)amino]-5-(dipentylamino)-5-oxopentanoic acid |
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| Formula | C22H32Cl2N2O4 |
| Molar mass | 459.406 g/mol g·mol−1 |
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Lorglumide (CR-1409) is a drug which inhibits gastrointestinal motility and reduces gastric secretions, acting as a cholecystokinin antagonist,[1] with fairly high selectivity for the CCKA subtype.[2] It has been suggested as a potential treatment for a variety of gastrointestinal problems including stomach ulcers, irritable bowel syndrome, dyspepsia, constipation and pancreatitis, as well as some forms of cancer, but animal and human testing has produced inconsistent results and no clear therapeutic role has been established, although it is widely used in scientific research.[3][4][5][6]
Synthesis
References
- ^ 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
- ^ F. Makovec, et al. Eur J. Med. Chem., 21, 9 (1986).