Asperlicin
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Nazivi | |
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IUPAC naziv (S-(2α,9β,9(R*),9α,β))-6,7-Dihydro-7-((2,3,9,9a-tetrahydro-9-hydroxy-2-(2-methylpropyl)-3-oxo-1H-imidazo(1,2-a)indol-9-yl)methyl)quinazolino(3,2-a)(1,4)benzodiazepine-5,13-dione | |
Identifikacija | |
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3D model (Jmol) |
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PubChem[1][2] C ID |
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SMILES
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Svojstva | |
C31H29N5O4 | |
Molarna masa | 535,593 |
Ukoliko nije drugačije napomenuto, podaci se odnose na standardno stanje materijala (na 25 °C [77 °F], 100 kPa). | |
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Reference infokutije | |
Asperlicin je mikotoksin, izveden ih funguss Aspergillus alliaceus. On deluje kao selektivni antagonist holecistokininskog receptora CCKA.[3][4][5] On je bio vodeće jedinjenje za razvoj brojnih novih CCKA antagonista sa mogućim kliničkim primenama.[6][7][8][9]
Reference
- ^ 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. PMID 20970519. doi:10.1016/j.drudis.2010.10.003. уреди
- ^ 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.
- ^ Chang, R. S.; Lotti, V. J.; Monaghan, R. L.; Birnbaum, J.; Stapley, E. O.; Goetz, M. A.; Albers-Schönberg, G.; Patchett, A. A.; Liesch, J. M.; Hensens, O. D.; Springer, James P. (1985). „A potent nonpeptide cholecystokinin antagonist selective for peripheral tissues isolated from Aspergillus alliaceus”. Science. 2994227 (4722): 177—179. Bibcode:1985Sci...230..177C. PMID 2994227. doi:10.1126/science.2994227.
- ^ Goetz, M. A.; Lopez, M.; Monaghan, R. L.; Chang, R. S.; Lotti, V. J.; Chen, T. B. (1985). „Asperlicin, a novel non-peptidal cholecystokinin antagonist from Aspergillus alliaceus. Fermentation, isolation and biological properties”. The Journal of Antibiotics. 3005212 (12): 1633—1637. PMID 3005212. doi:10.7164/antibiotics.38.1633.
- ^ Liesch, J. M.; Hensens, O. D.; Springer, J. P.; Chang, R. S.; Lotti, V. J. (1985). „Asperlicin, a novel non-peptidal cholecystokinin antagonist from Aspergillus alliaceus. Structure elucidation”. The Journal of Antibiotics. 3841533 (12): 1638—1641. PMID 3841533. doi:10.7164/antibiotics.38.1638.
- ^ Bock, M. G.; Dipardo, R. M.; Rittle, K. E.; Evans, B. E.; Freidinger, R. M.; Veber, D. F.; Chang, R. S.; Chen, T. B.; Keegan, M. E.; Lotti, V. J. (1986). „Cholecystokinin antagonists. Synthesis of asperlicin analogues with improved potency and water solubility”. Journal of Medicinal Chemistry. 3761313 (10): 1941—1945. PMID 3761313. doi:10.1021/jm00160a024.
- ^ Evans, B. E.; Rittle, K. E.; Bock, M. G.; Dipardo, R. M.; Freidinger, R. M.; Whitter, W. L.; Gould, N. P.; Lundell, G. F.; Homnick, C. F.; Veber, D. F. (1987). „Design of nonpeptidal ligands for a peptide receptor: Cholecystokinin antagonists”. Journal of Medicinal Chemistry. 2885419 (7): 1229—1239. PMID 2885419. doi:10.1021/jm00390a019.
- ^ Van Der Bent, A.; Ter Laak, A. M.; Ijzerman, A. P.; Soudijn, W. (1992). „Molecular modelling of asperlicin derived cholecystokinin a receptor antagonists”. European Journal of Pharmacology. 226 (4): 327—334. PMID 1397061. doi:10.1016/0922-4106(92)90050-6.
- ^ Lattmann, E.; Billington, D. C.; Poyner, D. R.; Howitt, S. B.; Offel, M. (2001). „Synthesis and evaluation of asperlicin analogues as non-peptidal cholecystokinin-antagonists”. Drug Design and Discovery. 11469752 (3): 219—230. PMID 11469752.
Spoljašnje veze
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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-oslobađajuči 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 |