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Roksindol Reference Spoljašnje veze Мени за навигацију112192-04-82190505218988043227SMS0O787092710.1007/BF02257418168443910.1055/s-2007-1014451„Early clinical results with the neuroleptic roxindole (EMD 49,980) in the treatment of schizophrenia--an open study”135338810.1016/0924-977X(92)90041-68811507809728010.1002/mds.8700802147950157„Actions of roxindole at recombinant human dopamine D2, D3 and D4 and serotonin 5-HT1A, 5-HT1B and 5-HT1D receptors”10431754оригинала1534148310.1021/jm040792yуууу

Допамински агонистиАнтидепресантиИндолиПиридиниФеноли


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Roksindol




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Roksindol
Roxindole.png

IUPAC ime
3-[4-(4-fenil-3,6-dihidro-2H-piridin-1-il)butil]-1H-indol-5-ol
Identifikatori
CAS broj
112192-04-8 ДаY
ATC kodnone
PubChemCID 219050
IUPHAR/BPS52
ChemSpider189880
UNII
43227SMS0O ДаY
Hemijski podaci
Formula
C23H26N2O
Molarna masa346,47 g/mol



Roksindol (EMD-49,980) je dopaminergični i serotonergični lek koji je originalno bio razvijen za lečenje šizofrenije.[1][2][3] U kliničkim ispitivanjima njegova antipsihotička efikasnost je bila skromna, ali je neočekivano nađeno da proizvodi potentne i brze antidepresantne i anksiolitičke efekte.[2][3] Konsekventno, roksindol je dalje istražen za primenu u lečenju depresije.[1][4][4] On je takođe istražen kao terapija za Parkinsonovu bolest i lečenje prolaktinoma.[5][6]


Roksindol deluje kao agonist na sledećim receptorima:[7][8]



  • D2 receptor (pKi = 8.55)


  • D3 receptor (pKi = 8.93)


  • D4 receptor (pKi = 8.23)


  • 5-HT1A receptor (pKi = 9.42)


Reference




  1. ↑ 1,01,1 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. PMID 7870927. doi:10.1007/BF02257418. 


  2. ↑ 2,02,1 Klimke A, Klieser E (1991). „Antipsychotic efficacy of the dopaminergic autoreceptor agonist EMD 49980 (Roxindol). Results of an open clinical study”. Pharmacopsychiatry. 24 (4): 107—12. PMID 1684439. doi:10.1055/s-2007-1014451. 


  3. ↑ 3,03,1 Kasper S, Fuger J, Zinner HJ, Bäuml J, Möller HJ (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. PMID 1353388. doi:10.1016/0924-977X(92)90041-6. 


  4. ↑ 4,04,1 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. 


  5. ^ Bravi D, Davis TL, Mouradian MM, Chase TN (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. PMID 8097280. doi:10.1002/mds.870080214. 


  6. ^ Jaspers C, Benker G, Reinwein D (1994). „Treatment of prolactinoma patients with the new non-ergot dopamine agonist roxindol: first results”. The Clinical Investigator. 72 (6): 451—6. PMID 7950157. 


  7. ^ Newman-Tancredi A, Cussac D, Audinot V, Millan MJ (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. Архивирано из оригинала на датум 11. 02. 2013. Приступљено 24. 04. 2012. 


  8. ^ Heinrich T, Böttcher H, Bartoszyk GD, Greiner HE, Seyfried CA, Van Amsterdam C (2004). „Indolebutylamines as selective 5-HT(1A) agonists”. Journal of Medicinal Chemistry. 47 (19): 4677—83. PMID 15341483. doi:10.1021/jm040792y. 



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