Delucemin — разлика између измена
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'''Delucemin''' ('''NPS-1506''') je lek koji deluje kao [[NMDA antagonist]] i [[serotonin reuptake inhibitor|inhibitor ponovnog uzimanja serotonina]], i ima [[neuroprotective|neuroprotektivna]] dejstva.<ref>{{cite journal | vauthors = Mueller AL, Artman LD, Balandrin MF, Brady E, Chien Y, Delmar EG, George K, Kierstead A, Marriott TB, Moe ST, Newman MK, Raszkiewicz JL, Sanguinetti EL, van Wagenen BC, Wells D | display-authors = 6 | title = NPS 1506, a novel NMDA receptor antagonist and neuroprotectant. Review of preclinical and clinical studies | journal = Annals of the New York Academy of Sciences | volume = 890 | pages = 450–7 | date = December 1999 | pmid = 10668449 | doi = 10.1111/j.1749-6632.1999.tb08023.x | s2cid = 5629889 }}</ref><ref>{{cite journal | vauthors = Leoni MJ, Chen XH, Mueller AL, Cheney J, McIntosh TK, Smith DH | title = NPS 1506 attenuates cognitive dysfunction and hippocampal neuron death following brain trauma in the rat | journal = Experimental Neurology | volume = 166 | issue = 2 | pages = 442–9 | date = December 2000 | pmid = 11085909 | doi = 10.1006/exnr.2000.7513 | s2cid = 39222349 }}</ref> Prvobitno je ispitivan za lečenje [[stroke|moždanog udara]], a 2004. je proučavan kao potencijalni [[antidepressant|antidepresiv]].<ref name="NPS-Pharmaceuticals-Inc-May-2004-10-Q">{{cite web|url=http://edgar.secdatabase.com/173/119312504090111/filing-main.htm |title=NPS Pharmaceuticals Inc, Form 10-Q, Quarterly Report, Filing Date May 17, 2004 |publisher=secdatabase.com |access-date =May 14, 2018}}</ref><ref>{{cite patent | country = CA | number = 2599721 | title = Pharmaceutical compositions for the treatment and/or prevention of depression | inventor = Pyke R, Ceci A}}</ref><ref>{{cite patent | country = WO | number = 2014015047 | title = Compositions and methods to treat neurodegenerative diseases | inventor = Ichinose F, Marutani E, Kida K }}</ref> |
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== Poreklo == |
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Osnovna struktura Delucemina bila je zasnovana na [[Argiotoxin|argiotoksinu 636]], NMDA antagonistu izolovanom iz otrova Araneid ''[[Argiope aurantia]]''.<ref>{{Cite book|title = Spider Ecophysiology|url = https://books.google.com/books?id=sur9JSvSOX0C|publisher = Springer Science & Business Media|date = 2013-02-15|isbn = 9783642339899|first = Wolfgang|last = Nentwig }}</ref><ref>{{cite book | chapter=Spider Venom Components as Drug Candidates | vauthors = Oldrati V, Bianchi E, Stöcklin R | title = Spider Ecophysiology | date=February 2013 | pages=491–503 | doi=10.1007/978-3-642-33989-9_37|isbn = 978-3-642-33988-2}}</ref><ref>{{cite journal | vauthors = Monge-Fuentes V, Gomes FM, Campos GA, ((Silva Jd)), Biolchi AM, Dos Anjos LC, Gonçalves JC, Lopes KS, Mortari MR | display-authors = 6 | title = Neuroactive compounds obtained from arthropod venoms as new therapeutic platforms for the treatment of neurological disorders | journal = The Journal of Venomous Animals and Toxins Including Tropical Diseases | volume = 21 | issue = 31 | pages = 31 | date = August 2015 | pmid = 26257776 | pmc = 4529710 | doi = 10.1186/s40409-015-0031-x | doi-access = free }}</ref> |
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== Reference == |
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== Literatura == |
== Literatura == |
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* [http://www.drugbank.ca/drugs/ -{Delucemine}-] |
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[[Категорија:Антагонисти NMDA рецептора]] |
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[[Категорија:Амини]] |
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Верзија на датум 18. децембар 2023. у 02:37
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| Klinički podaci | |
|---|---|
| Drugs.com | Monografija |
| Identifikatori | |
| CAS broj | 186495-49-8  |
| ATC kod | none |
| PubChem | CID 156421 |
| ChemSpider | 137745 |
| UNII | 124LSR3H2X |
| Hemijski podaci | |
| Formula | C16H17F2N |
| Molarna masa | 261,310 |
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Delucemin (NPS-1506) je lek koji deluje kao NMDA antagonist i inhibitor ponovnog uzimanja serotonina, i ima neuroprotektivna dejstva.[1][2] Prvobitno je ispitivan za lečenje moždanog udara, a 2004. je proučavan kao potencijalni antidepresiv.[3][4][5]
Poreklo
Osnovna struktura Delucemina bila je zasnovana na argiotoksinu 636, NMDA antagonistu izolovanom iz otrova Araneid Argiope aurantia.[6][7][8]
Osobine
Delucemin je organsko jedinjenje, koje sadrži 16 atoma ugljenika i ima molekulsku masu od 261,310 Da.
| Osobina | Vrednost |
|---|---|
| Broj akceptora vodonika | 1 |
| Broj donora vodonika | 1 |
| Broj rotacionih veza | 5 |
| Particioni koeficijent[9] (ALogP) | 3,8 |
| Rastvorljivost[10] (logS, log(mol/L)) | -5,4 |
| Polarna površina[11] (PSA, Å2) | 12,0 |
Reference
- ^ Mueller AL, Artman LD, Balandrin MF, Brady E, Chien Y, Delmar EG, et al. (децембар 1999). „NPS 1506, a novel NMDA receptor antagonist and neuroprotectant. Review of preclinical and clinical studies”. Annals of the New York Academy of Sciences. 890: 450—7. PMID 10668449. S2CID 5629889. doi:10.1111/j.1749-6632.1999.tb08023.x.
- ^ Leoni MJ, Chen XH, Mueller AL, Cheney J, McIntosh TK, Smith DH (децембар 2000). „NPS 1506 attenuates cognitive dysfunction and hippocampal neuron death following brain trauma in the rat”. Experimental Neurology. 166 (2): 442—9. PMID 11085909. S2CID 39222349. doi:10.1006/exnr.2000.7513.
- ^ „NPS Pharmaceuticals Inc, Form 10-Q, Quarterly Report, Filing Date May 17, 2004”. secdatabase.com. Приступљено 14. 5. 2018.
- ^ CA 2599721, Pyke R, Ceci A, "Pharmaceutical compositions for the treatment and/or prevention of depression"
- ^ WO 2014015047, Ichinose F, Marutani E, Kida K, "Compositions and methods to treat neurodegenerative diseases"
- ^ Nentwig, Wolfgang (2013-02-15). Spider Ecophysiology. Springer Science & Business Media. ISBN 9783642339899.
- ^ Oldrati V, Bianchi E, Stöcklin R (фебруар 2013). „Spider Venom Components as Drug Candidates”. Spider Ecophysiology. стр. 491—503. ISBN 978-3-642-33988-2. doi:10.1007/978-3-642-33989-9_37.
- ^ Monge-Fuentes V, Gomes FM, Campos GA, Silva Jd, Biolchi AM, Dos Anjos LC, et al. (август 2015). „Neuroactive compounds obtained from arthropod venoms as new therapeutic platforms for the treatment of neurological disorders”. The Journal of Venomous Animals and Toxins Including Tropical Diseases. 21 (31): 31. PMC 4529710
. PMID 26257776. doi:10.1186/s40409-015-0031-x .
- ^ Ghose, A.K.; Viswanadhan V.N. & Wendoloski, J.J. (1998). „Prediction of Hydrophobic (Lipophilic) Properties of Small Organic Molecules Using Fragment Methods: An Analysis of AlogP and CLogP Methods”. J. Phys. Chem. A. 102: 3762—3772. doi:10.1021/jp980230o.
- ^ Tetko IV, Tanchuk VY, Kasheva TN, Villa AE (2001). „Estimation of Aqueous Solubility of Chemical Compounds Using E-State Indices”. Chem Inf. Comput. Sci. 41: 1488—1493. PMID 11749573. doi:10.1021/ci000392t.
- ^ Ertl P.; Rohde B.; Selzer P. (2000). „Fast calculation of molecular polar surface area as a sum of fragment based contributions and its application to the prediction of drug transport properties”. J. Med. Chem. 43: 3714—3717. PMID 11020286. doi:10.1021/jm000942e.
Literatura
- Hardman JG, Limbird LE, Gilman AG (2001). Goodman & Gilman's The Pharmacological Basis of Therapeutics (10. изд.). New York: McGraw-Hill. ISBN 0071354697. doi:10.1036/0071422803.
- Thomas L. Lemke; David A. Williams, ур. (2007). Foye's Principles of Medicinal Chemistry (6. изд.). Baltimore: Lippincott Willams & Wilkins. ISBN 0781768799.
