Roksindol

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Roksindol
(IUPAC) ime
3-[4-(4-fenil-3,6-dihidro-2H-piridin-1-il)butil]-1H-indol-5-ol
Klinički podaci
Identifikatori
CAS broj 112192-04-8
ATC kod nije dodeljen
PubChem[1][2] 219050
ChemSpider[3] 189880
UNII 43227SMS0O DaY
Hemijski podaci
Formula C23H26N2O 
Mol. masa 346,47 g/mol
SMILES eMolekuli & PubHem
Farmakoinformacioni podaci
Trudnoća ?
Pravni status

Roksindol (EMD-49,980) je dopaminergični i serotonergični lek koji je originalno bio razvijen za lečenje šizofrenije.[4][5][6] U kliničkim ispitivanjima njegova antipsihotička efikasnost je bila skromna, ali je neočekivano nađeno da proizvodi potentne i brze antidepresantne i anksiolitičke efekte.[5][6] Konsekventno, roksindol je dalje istražen za primenu u lečenju depresije.[4][7][7] On je takođe istražen kao terapija za Parkinsonovu bolest i lečenje prolaktinoma.[8][9]

Roksindol deluje kao agonist na sledećim receptorima:[10][11]

Reference[uredi | uredi kod]

  1. 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
  2. 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. 
  3. 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
  4. 4,0 4,1 Gründer G, Wetzel H, Hammes E, Benkert O (1993). „Roxindole, a dopamine autoreceptor agonist, in the treatment of major depression”. Psychopharmacology 111 (1): 123–6. DOI:10.1007/BF02257418. PMID 7870927. 
  5. 5,0 5,1 Klimke A, Klieser E (July 1991). „Antipsychotic efficacy of the dopaminergic autoreceptor agonist EMD 49980 (Roxindol). Results of an open clinical study”. Pharmacopsychiatry 24 (4): 107–12. DOI:10.1055/s-2007-1014451. PMID 1684439. 
  6. 6,0 6,1 Kasper S, Fuger J, Zinner HJ, Bäuml J, Möller HJ (March 1992). „Early clinical results with the neuroleptic roxindole (EMD 49,980) in the treatment of schizophrenia--an open study”. European Neuropsychopharmacology : the Journal of the European College of Neuropsychopharmacology 2 (1): 91–5. DOI:10.1016/0924-977X(92)90041-6. PMID 1353388. 
  7. 7,0 7,1 Maj J, Kolodziejczyk K, Rogóz Z, Skuza G (1996). „Roxindole, a potential antidepressant. I. Effect on the dopamine system”. Journal of Neural Transmission (Vienna, Austria : 1996) 103 (5): 627–41. PMID 8811507. 
  8. Bravi D, Davis TL, Mouradian MM, Chase TN (April 1993). „Treatment of Parkinson's disease with the partial dopamine agonist EMD 49980”. Movement Disorders : Official Journal of the Movement Disorder Society 8 (2): 195–7. DOI:10.1002/mds.870080214. PMID 8097280. 
  9. Jaspers C, Benker G, Reinwein D (June 1994). „Treatment of prolactinoma patients with the new non-ergot dopamine agonist roxindol: first results”. The Clinical Investigator 72 (6): 451–6. PMID 7950157. 
  10. Newman-Tancredi A, Cussac D, Audinot V, Millan MJ (June 1999). „Actions of roxindole at recombinant human dopamine D2, D3 and D4 and serotonin 5-HT1A, 5-HT1B and 5-HT1D receptors”. Naunyn-Schmiedeberg's Archives of Pharmacology 359 (6): 447–53. PMID 10431754. 
  11. Heinrich T, Böttcher H, Bartoszyk GD, Greiner HE, Seyfried CA, Van Amsterdam C (September 2004). „Indolebutylamines as selective 5-HT(1A) agonists”. Journal of Medicinal Chemistry 47 (19): 4677–83. DOI:10.1021/jm040792y. PMID 15341483. 

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