Ladostigil (TV-3,326) je neuroprotektivni agens koji se istražuje za moguću primenu u lečenju neurodegenerativnih poremećaja poput Alchajmerove bolesti, demencije sa Levijevim telima, i Parkinsonove bolesti.[4] On deluje kao reversiblni inhibitor acetilholinesteraze i butirilholinesteraze, i kao ireverzibilni inhibitor monoamiske oksidaze B. On kombinuje mehanizme dejstva starijih lekova kao što su rivastigmin i rasagilin u jedan molekul.[5][6] Osim neuroprotektivnih svojstava, ladostigil poboljšava izražavanje neurotrofnih faktora poput GDNF i BDNF, a moguće je da ima sposobnost povraćanja dela oštećenja prisutnih kod neurodegenerativnih bolesti putem indukcije neutrogeneze.[7] Ladostigil takođe ima antidepresivno dejstvo, i može da bude koristan pri lečenju depresije i anksioznosti.[8][9]
Ladostigil
|
| (IUPAC) ime
|
| [(3R)-3-(prop-2-inilamino)indan-5-il]-N-propilkarbamat
|
| Klinički podaci
|
| Identifikatori
|
| CAS broj
|
209349-27-4
|
| ATC kod
|
nije dodeljen
|
| PubChem[1][2]
|
208907
|
| ChemSpider[3]
|
181005
|
| UNII
|
SW3H1USR4Q  Y
|
| Hemijski podaci
|
| Formula
|
C16H20N2O2
|
| Mol. masa
|
272,34 g/mol
|
| SMILES
|
eMolekuli & PubHem
|
| InChI |
|---|
InChI=1S/C16H20N2O2/c1-4-10-17-15-9-7-12-6-8-13(11-14(12)15)20-16(19)18(3)5-2/h1,6,8,11,15,17H,5,7,9-10H2,2-3H3 Y
Key: LHXOCOHMBFOVJS-UHFFFAOYSA-N Y |
|
| Sinonimi
|
[N-propargil-(3R)-aminoindan-5il]-N-propilkarbamat
|
| Farmakoinformacioni podaci
|
| Trudnoća
|
?
|
| Pravni status
|
Nije kontrolisan
|
| Način primene
|
Oralno
|
- ↑ 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. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519. edit
- ↑ 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.
- ↑ Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). „Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining”. J Cheminform 2 (1): 3. DOI:10.1186/1758-2946-2-3. PMID 20331846. edit
- ↑ Weinstock M, Bejar C, Wang RH, et al. (2000). „TV3326, a novel neuroprotective drug with cholinesterase and monoamine oxidase inhibitory activities for the treatment of Alzheimer's disease”. Journal of Neural Transmission. Supplementum (60): 157–69. PMID 11205137.
- ↑ Weinreb O, Mandel S, Bar-Am O, et al. (January 2009). „Multifunctional neuroprotective derivatives of rasagiline as anti-Alzheimer's disease drugs”. Neurotherapeutics : the Journal of the American Society for Experimental NeuroTherapeutics 6 (1): 163–74. DOI:10.1016/j.nurt.2008.10.030. PMID 19110207.
- ↑ Weinstock M, Luques L, Bejar C, Shoham S (2006). „Ladostigil, a novel multifunctional drug for the treatment of dementia co-morbid with depression”. Journal of Neural Transmission. Supplementum (70): 443–6. PMID 17017566.
- ↑ Weinreb O, Amit T, Bar-Am O, Youdim MB (December 2007). „Induction of neurotrophic factors GDNF and BDNF associated with the mechanism of neurorescue action of rasagiline and ladostigil: new insights and implications for therapy”. Annals of the New York Academy of Sciences 1122: 155–68. DOI:10.1196/annals.1403.011. PMID 18077571. [mrtav link]
- ↑ Weinstock M, Poltyrev T, Bejar C, Youdim MB (March 2002). „Effect of TV3326, a novel monoamine-oxidase cholinesterase inhibitor, in rat models of anxiety and depression”. Psychopharmacology 160 (3): 318–24. DOI:10.1007/s00213-001-0978-x. PMID 11889501.
- ↑ Weinstock M, Gorodetsky E, Poltyrev T, Gross A, Sagi Y, Youdim M (June 2003). „A novel cholinesterase and brain-selective monoamine oxidase inhibitor for the treatment of dementia comorbid with depression and Parkinson's disease”. Progress in Neuro-psychopharmacology & Biological Psychiatry 27 (4): 555–61. DOI:10.1016/S0278-5846(03)00053-8. PMID 12787840.
