Roxindole (EMD-49,980) is a dopaminergic and serotonergic drug which was originally developed by Merck KGaA 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] It has also been investigated as a therapy for Parkinson's disease and prolactinoma.[5][6]
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Formula | C23H26N2O |
Molar mass | 346.474 g·mol−1 |
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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] Weaker activity at the serotonin 1B and 1D receptors has been seen.[11] 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][12]