Repositioning Candidate Details
| Candidate ID: | R0244 |
| Source ID: | DB00850 |
| Source Type: | approved |
| Compound Type: | small molecule |
| Compound Name: | Perphenazine |
| Synonyms: | |
| Molecular Formula: | C21H26ClN3OS |
| SMILES: | OCCN1CCN(CCCN2C3=CC=CC=C3SC3=C2C=C(Cl)C=C3)CC1 |
| Structure: |
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| DrugBank Description: | An antipsychotic phenothiazine derivative with actions and uses similar to those of chlorpromazine. |
| CAS Number: | 58-39-9 |
| Molecular Weight: | 403.969 |
| DrugBank Indication: | For use in the management of the manifestations of psychotic disorders and for the control of severe nausea and vomiting in adults. |
| DrugBank Pharmacology: | Perphenazine is a piperazinyl phenothiazine, acts on the central nervous system, and has a greater behavioral potency than other phenothiazine derivatives whose side chains do not contain a piperazine moiety. It is a member of a class of drugs called phenothiazines, which are dopamine D1/D2 receptor antagonists. Perphenazine is 10 to 15 times as potent as chlorpromazine; that means perphenazine is a highly potent antipsychotic. In equivalent doses it has approximately the same frequency and severity of early and late extrapypramidal side-effects compared to Haloperidol. |
| DrugBank MoA: | Binds to the dopamine D1 and dopamine D2 receptors and inhibits their activity. The mechanism of the anti-emetic effect is due predominantly to blockage of the dopamine D2 neurotransmitter receptors in the chemoreceptor trigger zone and vomiting centre. Perphenazine also binds the alpha andrenergic receptor. This receptor's action is mediated by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. |
| Targets: | Dopamine D2 receptor; Dopamine D1 receptor; Calmodulin |
| Inclusion Criteria: |
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