Roksindol

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	219050
ChemSpider	189880
UNII	43227SMS0O
Hemijski podaci
Formula	C23H26N2O
Mol. masa	346,47 g/mol
SMILES	eMolekuli & PubHem
InChI
	InChI=1S/C23H26N2O/c26-21-9-10-23-22(16-21)20(17-24-23)8-4-5-13-25-14-11-19(12-15-25)18-6-2-1-3-7-18/h1-3,6-7,9-11,16-17,24,26H,4-5,8,12-15H2 ; Key: HGEYJZMMUGWEOT-UHFFFAOYSA-N
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]

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

↑ 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
↑ ^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.
↑ ^5,0 ^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.
↑ ^6,0 ^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.
↑ ^7,0 ^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.
↑ 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.
↑ 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.
↑ 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.
↑ 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.

Spoljašnje veze

	Portal Medicina
	Portal Hemija

[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

[pmid7870927-4] 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.

[pmid1684439-5] 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.

[pmid1353388-6] 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.

[pmid8811507-7] 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.

[pmid8097280-8] 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.

[pmid7950157-9] 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.

[pmid10431754-10] 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.

[pmid15341483-11] 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.

[1]

[2]

[3]

[4]

[5]

[6]

[7]

[8]

[9]

[10]

[11]