5-HT1F
5-HT1F receptor is a subtype of 5-HT receptor that binds the endogenous neurotransmitter serotonin. It is a G protein-coupled receptor (GPCR) that is coupled to Gi/Go and is expressed throughout the central nervous system (CNS).
Function[edit | edit source]
The 5-HT1F receptor is thought to play a role in the pathophysiology of migraine. Activation of this receptor has been shown to inhibit the release of calcitonin gene-related peptide (CGRP) from neurons in the trigeminal ganglion. CGRP is thought to play a key role in the pathogenesis of migraine. Therefore, 5-HT1F receptor agonists may be useful in the treatment of migraine.
Ligands[edit | edit source]
Several selective 5-HT1F receptor agonists are available for experimental use, including LY334370 and LY344864. These compounds have been shown to be effective in animal models of migraine. In addition, the non-selective 5-HT1F receptor agonist sumatriptan, which is used clinically for the treatment of migraine, has been shown to activate the 5-HT1F receptor.
Clinical significance[edit | edit source]
The 5-HT1F receptor is a potential target for the treatment of migraine. Several 5-HT1F receptor agonists are currently under development for this indication. These include lasmiditan, which is in phase III clinical trials, and LY334370, which has completed phase II clinical trials.
See also[edit | edit source]
References[edit | edit source]
External links[edit | edit source]
- 5-HT1F at the IUPHAR Database
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