Repositioning Candidate Details
| Candidate ID: | R0131 |
| Source ID: | DB00472 |
| Source Type: | approved; vet_approved |
| Compound Type: | small molecule |
| Compound Name: | Fluoxetine |
| Synonyms: | |
| Molecular Formula: | C17H18F3NO |
| SMILES: | CNCCC(OC1=CC=C(C=C1)C(F)(F)F)C1=CC=CC=C1 |
| Structure: |
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| DrugBank Description: | Fluoxetine is a 2nd generation antidepressant categorized as a selective serotonin reuptake inhibitor (SSRI).[A181673] It gained FDA approval in 1987 and although it was initially intended for the treatment of depression, today it is commonly prescribed to manage depression in addition to various other pathologies.[L7721] |
| CAS Number: | 54910-89-3 |
| Molecular Weight: | 309.3261 |
| DrugBank Indication: | Fluoxetine is indicated for both acute and maintenance treatment of major depressive disorder, obsessive compulsive disorder, and bulimia nervosa; however, it is only indicated for acute treatment of panic disorder independent of whether agoraphobia is present.[L7664] Fluoxetine may also be used in combination with olanzapine to treat depression related to Bipolar I Disorder, and treatment resistant depression.[L7664] |
| DrugBank Pharmacology: | Fluoxetine blocks the serotonin reuptake transporter in the presynaptic terminal, which ultimately results in sustained levels of 5-hydroxytryptamine (5-HT) in certain brain areas.[L7721] However, fluoxetine binds with relatively poor affinity to 5-HT, dopaminergic, adrenergic, cholinergic, muscarinic, and histamine receptors which explains why it has a far more desirable adverse effect profile compared to earlier developed classes of antidepressants such as tricyclic antidepressants.[L7721][A181673] |
| DrugBank MoA: | The monoaminergic hypothesis of depression emerged in 1965 and linked depression with dysfunction of neurotransmitters such as noradrenaline and serotonin.[L7721] Indeed, low levels of serotonin have been observed in the cerebrospinal fluid of patients diagnosed with depression.[A181793] As a result of this hypothesis, drugs that modulate levels of serotonin such as fluoxetine were developed.[L7721] Fluoxetine is a selective serotonin reuptake inhibitor (SSRI) and as the name suggests, it exerts it's therapeutic effect by inhibiting the presynaptic reuptake of the neurotransmitter serotonin.[A181673] As a result, levels of 5-hydroxytryptamine (5-HT) are increased in various parts of the brain.[L7721] Further, fluoxetine has high affinity for 5-HT transporters, weak affinity for noradrenaline transporters and no affinity for dopamine transporters indicating that it is 5-HT selective.[L7721] Fluoxetine interacts to a degree with the 5-HT<sub>2C</sub> receptor and it has been suggested that through this mechanism, it is able to increase noradrenaline and dopamine levels in the prefrontal cortex.[L7721] |
| Targets: | Sodium-dependent serotonin transporter; 5-hydroxytryptamine receptor 2C; Neuronal acetylcholine receptor subunit alpha-2; Neuronal acetylcholine receptor subunit alpha-3; Neuronal acetylcholine receptor subunit beta-4; Cyclin-dependent kinases regulatory subunit 1; Potassium voltage-gated channel subfamily H member 2 |
| Inclusion Criteria: |
| Strategy ID | Strategy | Synonyms | Related Targets | Related Drugs |
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| Target ID | Target Name | GENE | Action | Class | UniProtKB ID | Entry Name |
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| Diseases ID | DO ID | Disease Name | Definition | Class | |
|---|---|---|---|---|---|
| I02 | 1184 | nephrotic syndrome | "A nephrosis characterized by marked increase in glomerular protein permeability resulting in marked elevation of urine protein levels, hypoalbuminemia, hyperlipidemia, and hypercoagulability." [url:https\://en.wikipedia.org/wiki/Nephrotic_syndrome, url:https\://www.niddk.nih.gov/health-information/kidney-disease/nephrotic-syndrome-adults] | Details |