Repositioning Candidate Details
| Candidate ID: | R0083 |
| Source ID: | DB00216 |
| Source Type: | approved; investigational |
| Compound Type: | small molecule |
| Compound Name: | Eletriptan |
| Synonyms: | Eletriptan |
| Molecular Formula: | C22H26N2O2S |
| SMILES: | CN1CCC[C@@H]1CC1=CNC2=C1C=C(CCS(=O)(=O)C1=CC=CC=C1)C=C2 |
| Structure: |
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| DrugBank Description: | Eletriptan is a second generation triptan drug developed by Pfizer Inc for the treatment of migraine headaches. |
| CAS Number: | 143322-58-1 |
| Molecular Weight: | 382.519 |
| DrugBank Indication: | For the acute treatment of migraine with or without aura in adults. |
| DrugBank Pharmacology: | Eletriptan is a selective 5-hydroxytryptamine 1B/1D receptor agonist. In the anesthetized dog, eletriptan has been shown to reduce carotid arterial blood flow, with only a small increase in arterial blood pressure at high doses. While the effect on blood flow was selective for the carotid arterial bed, decreases in coronary artery diameter were observed. Eletriptan has also been shown to inhibit trigeminal nerve activity in the rat. |
| DrugBank MoA: | Eletriptan binds with high affinity to 5-HT1B, 5-HT1D and 5-HT1F receptors, has modest affinity for 5-HT1A, 5-HT1E, 5-HT2B and 5-HT7 receptors, and little or no affinity for 5-HT2A, 5-HT2C, 5-HT3, 5-HT4, 5-HT5A and 5-HT6 receptors. In contrast, eletriptan displays insignificant pharmacological activity at adrenergic alpha1, alpha2, or beta; dopaminergic D1 or D2; muscarinic; or opioid receptors. While the full mechanism of action of 5-HT receptor agonists in relieving migrains is not fully elucidated, it is proposed that the activation of 5-HT1 receptors located on intracranial blood vessels leads to vasoconstriction that correlates with the relief of migraine headaches. It is also proposed that the activation of 5-HT1 receptors on sensory nerve endings in the trigeminal system leads to the inhibition of release of pro-inflammatory neuropeptides. |
| Targets: | 5-hydroxytryptamine receptor 1D agonist; 5-hydroxytryptamine receptor 1B agonist; 5-hydroxytryptamine receptor 1F agonist; 5-hydroxytryptamine receptor 1A agonist |
| Inclusion Criteria: | Therapeutic strategy associated |
| Strategy ID | Strategy | Synonyms | Related Targets | Related Drugs | |
|---|---|---|---|---|---|
| S05 | Anti-inflammatory | inflammatory | Bile acid; TNF-a inhibitor; Dual PPAR-α and -δ agonists; Toll-Like Receptor; (TLR)-4 antagonist; Caspase inhibitor; ASK-1 inhibitor | Ursodeoxycholic Acid; Pentoxifylline; Elafibranor; JKB-121; Emricasan; Selonsertib; | Details |
| Target ID | Target Name | GENE | Action | Class | UniProtKB ID | Entry Name |
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| Diseases ID | DO ID | Disease Name | Definition | Class |
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