BTS 74,398
 | |
| IUPAC ime | |
|---|---|
1-([1-(3,4-dihlorofenil)ciklobutil]-2-(3-diamintilaminopropiltio)etanon | |
| Klinički podaci | |
| Drugs.com | 74,398.html Monografija |
| Identifikatori | |
| CAS broj | 548491-50-5  |
| ATC kod | None |
| PubChem | CID 24838024 |
| ChemSpider | 26325181 |
| UNII | I3W0WCC63A |
| Hemijski podaci | |
| Formula | C19H29Cl2N3OS |
| Molarna masa | 418,424 |
| |
| |
BTS 74,398 je stimulativni lek sa centralnim dejstvom koji je razvijen za lečenje Parkinsonove bolesti. On inhibira sinaptičko ponovno uzimanje dopamina, serotonina i noradrenalina, što ga čini trostrukim inhibitorom ponovnog uzimanja.[1] Bio je efikasan na životinjskim modelima Parkinsonove bolesti,[2][3] ali je bio neuspešan u ispitivanjima na ljudima.[4]
Osobine
[уреди | уреди извор]BTS 74,398 je organsko jedinjenje, koje sadrži 19 atoma ugljenika i ima molekulsku masu od 418,424 Da.
| Osobina | Vrednost |
|---|---|
| Broj akceptora vodonika | 5 |
| Broj donora vodonika | 2 |
| Broj rotacionih veza | 12 |
| Particioni koeficijent[5] (ALogP) | 2,9 |
| Rastvorljivost[6] (logS, log(mol/L)) | -6,4 |
| Polarna površina[7] (PSA, Å2) | 97,7 |
Reference
[уреди | уреди извор]- ^ Lane EL, Cheetham S, Jenner P (март 2005). . „Dopamine uptake inhibitor-induced rotation in 6-hydroxydopamine-lesioned rats involves both D1 and D2 receptors but is modulated through 5-hydroxytryptamine and noradrenaline receptors”. The Journal of Pharmacology and Experimental Therapeutics. 312 (3): 1124—31. PMID 15542624. S2CID 8208352. doi:10.1124/jpet.104.076554.
- ^ Hansard MJ, Smith LA, Jackson MJ, Cheetham SC, Jenner P (јануар 2004). . „The monoamine reuptake inhibitor BTS 74 398 fails to evoke established dyskinesia but does not synergise with levodopa in MPTP-treated primates”. Movement Disorders. 19 (1): 15—21. PMID 14743355. S2CID 26120965. doi:10.1002/mds.10596.
- ^ Lane EL, Cheetham SC, Jenner P (јануар 2005). . „Repeated administration of the monoamine reuptake inhibitor BTS 74 398 induces ipsilateral circling in the 6-hydroxydopamine lesioned rat without sensitizing motor behaviours”. The European Journal of Neuroscience. 21 (1): 179—86. PMID 15654855. S2CID 22417785. doi:10.1111/j.1460-9568.2004.03834.x.
- ^ Lane EL, Cheetham S, Jenner P (2008). . „Striatal output markers do not alter in response to circling behaviour in 6-OHDA lesioned rats produced by acute or chronic administration of the monoamine uptake inhibitor BTS 74 398”. Journal of Neural Transmission. 115 (3): 423—9. PMID 18250952. S2CID 195993. doi:10.1007/s00702-007-0854-x.
- ^ Ghose, Arup K.; Viswanadhan, Vellarkad N.; Wendoloski, John J. (1998). . „Prediction of Hydrophobic (Lipophilic) Properties of Small Organic Molecules Using Fragmental Methods: An Analysis of ALOGP and CLOGP Methods”. The Journal of Physical Chemistry A. 102 (21): 3762—3772. Bibcode:1998JPCA..102.3762G. doi:10.1021/jp980230o.
- ^ Tetko, Igor V.; Tanchuk, Vsevolod Yu.; Kasheva, Tamara N.; Villa, Alessandro E. P. (2001). . „Estimation of Aqueous Solubility of Chemical Compounds Using E-State Indices”. Journal of Chemical Information and Computer Sciences. 41 (6): 1488—1493. PMID 11749573. doi:10.1021/ci000392t.
- ^ Ertl, Peter; Rohde, Bernhard; Selzer, Paul (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”. Journal of Medicinal Chemistry. 43 (20): 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.
