Roxindole

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Roxindole
File:Roxindole.png
Systematic (IUPAC) name
3-[4-(4-phenyl-3,6-dihydro-2H-pyridin-1-yl)butyl]-1H-indol-5-ol
Identifiers
CAS Number 112192-04-8
ATC code none
PubChem CID 219050
IUPHAR/BPS 52
ChemSpider 189880
Chemical data
Formula C23H26N2O
Molar mass 346.47 g/mol[[Script error: No such module "String".]]
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Roxindole (EMD-49,980) is a dopaminergic and serotonergic drug which was originally developed for the treatment of schizophrenia.[1][2][3] In clinical trials its antipsychotic efficacy was only modest but it was unexpectedly found to produce potent and rapid antidepressant and anxiolytic effects.[2][3] As a result, roxindole was further researched for the treatment of depression instead.[1][4][4] It has also been investigated as a therapy for Parkinson's disease and prolactinoma.[5][6]

Roxindole acts as an agonist at the following receptors:[7][8]

At D2 and possibly D3 receptors roxindole is a partial agonist with preferential actions at autoreceptors and has been touted as a 'selective' autoreceptor agonist, hence the justification of its application as an antipsychotic.[9][10] It is also a serotonin reuptake inhibitor (IC50 = 1.4 nM) and has been reported to act as a 5-HT2A receptor antagonist as well.[8][9][10][11]

References

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  1. 1.0 1.1 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. 
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  4. 4.0 4.1 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. 
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