Repositioning Candidate Details
| Candidate ID: | R0160 |
| Source ID: | DB00472 |
| Source Type: | approved; vet_approved |
| Compound Type: | small molecule |
| Compound Name: | Fluoxetine |
| Synonyms: | (+-)-N-Methyl-3-phenyl-3-((alpha,alpha,alpha-trifluoro-P-tolyl)oxy)propylamine; (+-)-N-Methyl-gamma-(4-(trifluoromethyl)phenoxy)benzenepropanamine; Fluoxetine |
| 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). 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. |
| 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. Fluoxetine may also be used in combination with olanzapine to treat depression related to Bipolar I Disorder, and treatment resistant depression. |
| 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. 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. |
| DrugBank MoA: | The monoaminergic hypothesis of depression emerged in 1965 and linked depression with dysfunction of neurotransmitters such as noradrenaline and serotonin. Indeed, low levels of serotonin have been observed in the cerebrospinal fluid of patients diagnosed with depression. As a result of this hypothesis, drugs that modulate levels of serotonin such as fluoxetine were developed. 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. As a result, levels of 5-hydroxytryptamine (5-HT) are increased in various parts of the brain. 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. 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. |
| Targets: | Sodium-dependent serotonin transporter inhibitor; 5-hydroxytryptamine receptor 2C antagonist; Neuronal acetylcholine receptor subunit alpha-2 antagonist; Neuronal acetylcholine receptor subunit alpha-3 antagonist; Neuronal acetylcholine receptor subunit beta-4 antagonist; Cyclin-dependent kinases regulatory subunit 1; Potassium voltage-gated channel subfamily H member 2 inhibitor |
| Inclusion Criteria: | Indication associated |
