Delucemin
(преусмерено са NPS-1506)
 | |
| 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 |
| |
| |
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
[уреди | уреди извор]Osnovna struktura Delucemina bila je zasnovana na argiotoksinu 636, NMDA antagonistu izolovanom iz otrova Araneid Argiope aurantia.[6][7][8]
Osobine
[уреди | уреди извор]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
[уреди | уреди извор]- ^ 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
[уреди | уреди извор]- 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.
