Lorglumid

Из Википедије, слободне енциклопедије
Lorglumid
Lorglumide.svg
IUPAC ime
N2-(3,4-dichlorobenzoyl-N,N-dipentyl-α-glutamine
Identifikatori
CAS broj 97964-56-2 ДаY
ATC kod none
PubChem CID 3960
IUPHAR/BPS 891
ChEMBL CHEMBL24938
Sinonimi 4-[(3,4-dichlorobenzoyl)amino]-5-(dipentylamino)-5-oxopentanoic acid
Hemijski podaci
Formula C22H32Cl2N2O4
Molarna masa 459.406 g/mol
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Lorglumid (CR-1409) je lek koji inhibira gastrointestinalnu motilnost i redukuje želudačnu sekreciju. On deluje kao holecistokininski antagonist,[1] koji je u znatnoj meri selektivan za CCKA tip receptora.[2] 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.[3][4][5][6]

Sinteza[уреди]

Sinteza lorglumida:[7]

Literatura[уреди]

  1. 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
  2. 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
  3. 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
  4. 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
  5. Herranz R. Cholecystokinin antagonists: pharmacological and therapeutic potential. Medical Research Reviews. 2003 Sep;23(5):559-605. PMID 12789687
  6. 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
  7. F. Makovec, et al. Eur J. Med. Chem., 21, 9 (1986).