Lorglumid
(IUPAC) ime | |||
---|---|---|---|
N2-(3,4-dichlorobenzoyl-N,N-dipentyl-α-glutamine | |||
Klinički podaci | |||
Identifikatori | |||
CAS broj | 97964-56-2 | ||
ATC kod | nije dodeljen | ||
PubChem[1][2] | 3960 | ||
ChEMBL[3] | CHEMBL24938 | ||
Hemijski podaci | |||
Formula | C22H32Cl2N2O4 | ||
Mol. masa | 459.406 g/mol | ||
SMILES | eMolekuli & PubHem | ||
| |||
Sinonimi | 4-[(3,4-dichlorobenzoyl)amino]-5-(dipentylamino)-5-oxopentanoic acid | ||
Farmakoinformacioni podaci | |||
Trudnoća | ? | ||
Pravni status |
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]
Literatura
- ↑ 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
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Neuropeptidni ligandi
CCKA | Agonisti: Holecistokinin • CCK-4 Antagonisti: Asperlicin • Proglumid • Lorglumid • Devazepid • Deksloksiglumid |
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CCKB |
CRF1 | |
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CRF2 | Agonisti: Kortikotropin-oslobađajući hormon |
GAL1 | |
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GAL2 | |
GAL3 |
MCH1 | Agonisti: Melanin-koncentrirajući hormon Antagonisti: ATC-0175 • GW-803,430 • NGD-4715 • SNAP-7941 • SNAP-94847 |
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MCH2 | Agonisti: Melanin-koncentrirajući hormon |
MC1 | |
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MC2 | |
MC3 | |
MC4 | |
MC5 | Agonisti: alfa-MSH • Melanotan II |
Y1 | |
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Y2 | |
Y4 | |
Y5 |
NTS1 | |
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NTS2 |
vidi Opioidi
OX1 | |
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OX2 |
Agonisti: Karbetocin • Demoksitocin • Oksitocin • WAY-267,464
Antagonisti: Atosiban • L-371,257 • L-368,899
Antagonisti: Atosiban • L-371,257 • L-368,899
NK1 | Agonisti: Supstanca P Antagonisti: Aprepitant • Befetupitant • Kasopitant • CI-1021 • CP-96,345 • CP-99,994 • CP-122,721 • Dapitant • Ezlopitant • FK-888 • Fosaprepitant • GR-203,040 • GW-597,599 • HSP-117 • L-733,060 • L-741,671 • L-743,310 • L-758,298 • Lanepitant • LY-306,740 • Maropitant • Netupitant • NKP-608 • Nolpitantium • Orvepitant • RP-67,580 • SDZ NKT 343 • Vestipitant • Vofopitant |
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NK2 | |
NK3 |
V1A | Agonisti: Dezmopresin • Felipresin • Ornipresin • Terlipresin • Vazopresin Antagonisti: Konivaptan • Demeklociklin • Relkovaptan |
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V1B | |
V2 | Agonisti: Dezmopresin • Ornipresin • Vazopresin Antagonisti: Konivaptan • Demeklociklin • Liksivaptan • Mozavaptan • Satavaptan • Tolvaptan |