Tesofenzin
(преусмерено саTezofensin)
 | |
| IUPACime | |
|---|---|
(1R,2R,3S)-3-(3,4-dihlorofenil)-2-(etoksimetil)-8-metil-8-azabiciklo[3.2.1]oktan | |
| Klinički podaci | |
| Kategorija trudnoće |
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| Način primene | Oralno |
| Pravni status | |
| Pravni status |
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| Farmakokinetičkipodaci | |
| Bioraspoloživost | 90% |
| Metabolizam | 15–20% renalno; hepatički: CYP3A4 |
| Poluvreme eliminacije | 220 sata |
| Izlučivanje | Nije aplikabilno |
| Identifikatori | |
| CAS broj | 195875-84-4 |
| ATC kod | None |
| PubChem | CID11370864 |
| ChemSpider | 9545781 |
| UNII | BLH9UKX9V1 |
| Hemijski podaci | |
| Formula | C17H23Cl2NO |
| Molarna masa | 328,28 g·mol−1 |
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Tesofenzin(NS2330) jeinhibitor ponovnog preuzimanja serotonin–noradrenalin–dopaminaizfeniltropanskeporodice lekova, koji se razvija za lečenjegojaznosti.[1]Tesofenzin je prvobitno razvila danska biotehnološka kompanija NeuroSearch, koja je prenela prava na Sanionu 2014. godine.[2]
Prema podacima iz 2019. godine, razvoj tezofenzin je prekinut za lečenje Alchajmerove i Parkinsonove bolesti, ali je ufaziIIIkliničkog ispitivanjaza gojaznost.[3]
Osobine
[уреди|уреди извор]Tesofenzin jeorgansko jedinjenje,koje sadrži 17atomaugljenikai imamolekulsku masuod 328,277Da.
| Osobina | Vrednost |
|---|---|
| Broj akceptora vodonika | 2 |
| Broj donora vodonika | 0 |
| Broj rotacionih veza | 4 |
| Particioni koeficijent[4](ALogP) | 4,2 |
| Rastvorljivost[5](logS,log(mol/L)) | -5,0 |
| Polarna površina[6](PSA,Å2) | 12,5 |
Reference
[уреди|уреди извор]- ^Doggrell SA. "Tesofensine – a novel potent weight loss medicine. Evaluation of: Astrup A, Breum L, Jensen TJ, Kroustrup JP, Larsen TM. Effect of tesofensine on bodyweight loss, body composition, and quality of life in obese patients: a randomised, double-blind, placebo-controlled trial.Lancet2009372;1906–13 "Doggrell SA (јул 2009).„Tesofensine--a novel potent weight loss medicine. Evaluation of: Astrup A, Breum L, Jensen TJ, Kroustrup JP, Larsen TM. Effect of tesofensine on bodyweight loss, body composition, and quality of life in obese patients: a randomised, double-blind, placebo-controlled trial. Lancet 2008;372:1906-13”(PDF).Expert Opinion on Investigational Drugs.18(7): 1043—6.PMID19548858.S2CID207475155.doi:10.1517/13543780902967632.
- ^„NeuroSearch A/S signs agreement to transfer Phase I-II projects NS2359 and NS2330 (Tesofensine)”.NeuroSearch company announcement.Приступљено30. 10. 2014.
- ^„Tesofensine - Saniona”.AdisInsight.Springer Publishing.29. 1. 2019.Приступљено31. 10. 2019.
- ^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.PMID11749573.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.PMID11020286.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.ISBN0071354697.doi:10.1036/0071422803.
- Thomas L. Lemke; David A. Williams, ур. (2007).Foye's Principles of Medicinal Chemistry(6. изд.). Baltimore: Lippincott Willams & Wilkins.ISBN0781768799.
