Repositioning Candidate Details
| Candidate ID: | R0295 |
| Source ID: | DB00998 |
| Source Type: | approved; investigational |
| Compound Type: | small molecule |
| Compound Name: | Frovatriptan |
| Synonyms: | |
| Molecular Formula: | C14H17N3O |
| SMILES: | CN[C@@H]1CCC2=C(C1)C1=C(N2)C=CC(=C1)C(N)=O |
| Structure: |
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| DrugBank Description: | Frovatriptan is a triptan drug developed by Vernalis for the treatment of migraine headaches, in particular those associated with menstruation. Frovatriptan causes vasoconstriction of arteries and veins that supply blood to the head. |
| CAS Number: | 158747-02-5 |
| Molecular Weight: | 243.3043 |
| DrugBank Indication: | For the acute treatment of migraine attacks with or without aura in adults. |
| DrugBank Pharmacology: | Frovatriptan is a second generation triptan 5-HT receptor agonist that binds with high affinity for 5-HT<sub>1B</sub> and 5-HT<sub>1D</sub> receptors. It is structurally distinct from, but pharmacologically related to other selective 5-HT<sub>1B/1D</sub> receptor agonists. Frovatriptan has no significant effects on GABA<sub>A</sub> mediated channel activity and has no significant affinity for benzodiazepine binding sites. Frovatriptan is believed to act on extracerebral, intracranial arteries and to inhibit excessive dilation of these vessels in migraine. Research has shown that migraine can be caused by the swelling of blood vessels around the brain. Frovatriptan eases the pain associated with migraine by narrowing these blood vessels. Frovatriptan has one of the highest affinities for the 5-HT<sub>1B</sub> of the second-generation triptan agonists. |
| DrugBank MoA: | Three distinct pharmacological actions have been implicated in the antimigraine effect of the triptans: (1) stimulation of presynaptic 5-HT<sub>1D</sub> receptors, which serves to inhibit both dural vasodilation and inflammation; (2) direct inhibition of trigeminal nuclei cell excitability via 5-HT<sub>1B/1D</sub> receptor agonism in the brainstem and (3) vasoconstriction of meningeal, dural, cerebral or pial vessels as a result of vascular 5-HT<sub>1B</sub> receptor agonism. |
| Targets: | 5-hydroxytryptamine receptor 1D; 5-hydroxytryptamine receptor 1B |
| Inclusion Criteria: |
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