Lorglumid

Lorglumid
IUPAC ime
	N2-(3,4-dichlorobenzoyl-N,N-dipentyl-α-glutamine
Identifikatori
CAS broj	97964-56-2
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
	SMILES CCCCCN(CCCCC)C(=O)C(CCC(=O)O)NC(=O)C1=CC(=C(C=C1)Cl)Cl; ;

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 CCK_A 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

Референце

^ Makovec, F.; Bani, M.; Cereda, R.; Chisté, R.; Pacini, M. A.; Revel, L.; Rovati, L. A.; Rovati, L. C.; Setnikar, I. (1987). „Pharmacological properties of lorglumide as a member of a new class of cholecystokinin antagonists”. Arzneimittel-Forschung. 3440035 (11): 1265—1268. PMID 3440035.
^ González-Puga, C.; García-Navarro, A.; Escames, G.; León, J.; López-Cantarero, M.; Ros, E.; Acuña-Castroviejo, D. (2005). „Selective CCK-A but not CCK-B receptor antagonists inhibit HT-29 cell proliferation: Synergism with pharmacological levels of melatonin”. Journal of Pineal Research. 16150104 (3): 243—250. PMID 16150104. S2CID 20187767. doi:10.1111/j.1600-079X.2005.00239.x.
^ De Tullio, P.; Delarge, J.; Pirotte, B. (1999). „Recent advances in the chemistry of cholecystokinin receptor ligands (Agonists and antagonists)”. Current Medicinal Chemistry. 10213792 (6): 433—455. PMID 10213792.
^ De Tullio, P.; Delarge, J.; Pirotte, B. (2000). „Therapeutic and chemical developments of cholecystokinin receptor ligands”. Expert Opinion on Investigational Drugs. 11060666 (1): 129—146. PMID 11060666. S2CID 39985897. doi:10.1517/13543784.9.1.129.
^ Herranz, R. (2003). „Cholecystokinin antagonists: Pharmacological and therapeutic potential”. Medicinal Research Reviews. 12789687 (5): 559—605. PMID 12789687. S2CID 45758560. doi:10.1002/med.10042.
^ Berna, M. J.; Tapia, J. A.; Sancho, V.; Jensen, R. T. (2007). „Progress in developing cholecystokinin (CCK)/Gastrin receptor ligands that have therapeutic potential”. Current Opinion in Pharmacology. 17997137 (6): 583—592. PMC 2186776 . PMID 17997137. doi:10.1016/j.coph.2007.09.011.
^ Makovec F, Chistè R, Bani M, Revel, L, Setnikar I, Rovati LA (1986). „New glutamic and aspartic derivatives with potent CCK-antagonistic activity”. Eur J. Med. Chem. 21: 9—20.

[1] Makovec, F.; Bani, M.; Cereda, R.; Chisté, R.; Pacini, M. A.; Revel, L.; Rovati, L. A.; Rovati, L. C.; Setnikar, I. (1987). „Pharmacological properties of lorglumide as a member of a new class of cholecystokinin antagonists”. Arzneimittel-Forschung. 3440035 (11): 1265—1268. PMID 3440035.

[2] González-Puga, C.; García-Navarro, A.; Escames, G.; León, J.; López-Cantarero, M.; Ros, E.; Acuña-Castroviejo, D. (2005). „Selective CCK-A but not CCK-B receptor antagonists inhibit HT-29 cell proliferation: Synergism with pharmacological levels of melatonin”. Journal of Pineal Research. 16150104 (3): 243—250. PMID 16150104. S2CID 20187767. doi:10.1111/j.1600-079X.2005.00239.x.

[3] De Tullio, P.; Delarge, J.; Pirotte, B. (1999). „Recent advances in the chemistry of cholecystokinin receptor ligands (Agonists and antagonists)”. Current Medicinal Chemistry. 10213792 (6): 433—455. PMID 10213792.

[4] De Tullio, P.; Delarge, J.; Pirotte, B. (2000). „Therapeutic and chemical developments of cholecystokinin receptor ligands”. Expert Opinion on Investigational Drugs. 11060666 (1): 129—146. PMID 11060666. S2CID 39985897. doi:10.1517/13543784.9.1.129.

[5] Herranz, R. (2003). „Cholecystokinin antagonists: Pharmacological and therapeutic potential”. Medicinal Research Reviews. 12789687 (5): 559—605. PMID 12789687. S2CID 45758560. doi:10.1002/med.10042.

[6] Berna, M. J.; Tapia, J. A.; Sancho, V.; Jensen, R. T. (2007). „Progress in developing cholecystokinin (CCK)/Gastrin receptor ligands that have therapeutic potential”. Current Opinion in Pharmacology. 17997137 (6): 583—592. PMC 2186776 . PMID 17997137. doi:10.1016/j.coph.2007.09.011.

[7] Makovec F, Chistè R, Bani M, Revel, L, Setnikar I, Rovati LA (1986). „New glutamic and aspartic derivatives with potent CCK-antagonistic activity”. Eur J. Med. Chem. 21: 9—20.

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