Repositioning Candidate Details
| Candidate ID: | R1239 |
| Source ID: | DB09194 |
| Source Type: | withdrawn |
| Compound Type: | small molecule |
| Compound Name: | Etoperidone |
| Synonyms: | Etoperidone |
| Molecular Formula: | C19H28ClN5O |
| SMILES: | CCN1C(=O)N(CCCN2CCN(CC2)C2=CC=CC(Cl)=C2)N=C1CC |
| Structure: |
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| DrugBank Description: | Etoperidone is an atypical antidepressant introduced in Europe in 1977. It is a phenylpiperazine-substituted triazole derivative with a composition that classifies it as an analog of tradozone and presents a similar pharmacological profile. Etoperidone was developed by Angelini Francesco ACRAF. |
| CAS Number: | 52942-31-1 |
| Molecular Weight: | 377.92 |
| DrugBank Indication: | Etoperidone has been studied for the treatment of depression, tremors in Parkinson, extrapyramidal symptoms and male impotence. It is not certain if it was ever approved and marketed but its current status is withdrawn. |
| DrugBank Pharmacology: | Etoperidone has a biphasic effect on the central transmission of serotonin. It presents the capacity to inhibit serotonin receptor but also to inhibit the reuptake of serotonin, norepinephrine and dopamine. As part of its actions, etoperidone also inhibits the α-adrenergic receptors which directly corresponds to the sedative and cardiovascular effects. The presence of both effects caused that the effective dose of etoperidone was poorly tolerated thus, efforts have been made to separate the serotonergic and adrenergic functions in order to generate etoperidone-derivatives like nefazodone. |
| DrugBank MoA: | The activity of etoperidone is made mainly by its major metabolite 1-(3'-chlorophenyl)piperazine (mCPP). mCPP binds with different affinity to most of the serotonergic receptors and adrenergic receptors. This metabolite is an agonist of 5-HT2c and an antagonist of 5-HT2a. Part of etoperidone structure contibutes to the activity in the α-adrenergic receptors. |
| Targets: | Alpha-1 adrenergic receptors antagonist; Alpha-2 adrenergic receptors antagonist; Dopamine D2 receptor antagonist; Muscarinic acetylcholine receptor antagonist; 5-hydroxytryptamine receptor 2A antagonist; 5-hydroxytryptamine receptor 2C agonist |
| Inclusion Criteria: | Indication associated |
| Strategy ID | Strategy | Synonyms | Related Targets | Related Drugs |
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