Roksindol

Roksindol
IUPAC ime
	3-[4-(4-fenil-3,6-dihidro-2H-piridin-1-il)butil]-1H-indol-5-ol
Identifikatori
CAS broj	112192-04-8
ATC kod	none
PubChem	CID 219050
IUPHAR/BPS	52
ChemSpider	189880
UNII	43227SMS0O
Hemijski podaci
Formula	C23H26N2O
Molarna masa	346,47 g/mol
	SMILES Oc1ccc2c(c1)c(cn2)CCCCN4C/C=C(/c3ccccc3)CC4; ;

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 (pK_i = 8.55)
D₃ receptor (pK_i = 8.93)
D₄ receptor (pK_i = 8.23)
5-HT_1A receptor (pK_i = 9.42)

Reference

^ ^а ^б 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.
^ ^а ^б 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.
^ ^а ^б 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.
^ ^а ^б 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.
^ 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.
^ 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.
^ 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 11. 02. 2013. г. Приступљено 24. 04. 2012.
^ 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.

Spoljašnje veze

Molimo Vas, obratite pažnju na važno upozorenje
u vezi sa temama iz oblasti medicine (zdravlja).

[pmid7870927-1] а ^б 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.

[pmid1684439-2] а ^б 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.

[pmid1353388-3] а ^б 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.

[pmid8811507-4] а ^б 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.

[pmid8097280-5] 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.

[pmid7950157-6] 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.

[pmid10431754-7] 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 11. 02. 2013. г. Приступљено 24. 04. 2012.

[pmid15341483-8] 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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