期刊
BRITISH JOURNAL OF PHARMACOLOGY
卷 179, 期 3, 页码 400-415出版社
WILEY
DOI: 10.1111/bph.15710
关键词
5-HT receptor; 5-hydroxytryptamine; ditans; migraine; serotonin; trigeminal nerve; triptans
资金
- Russian Foundation for Basic Research [17-00-00053]
- Suomalainen Tiedeakatemia [325392]
5-hydroxytryptamine (5-HT) is considered a key mediator in migraine, but the role of 5-HT3 receptors in pain transmission remains controversial. The applicability of currently available 5-HT3 antagonists in migraine treatment is not clearly supported by clinical data.
5-hydroxytryptamine (5-HT; serotonin) is traditionally considered as a key mediator implicated in migraine. Multiple 5-HT receptor subtypes contribute to a variety of region-specific functional effects. The raphe nuclei control nociceptive inputs by releasing 5-HT in the brainstem, whereas dural mast cells provide the humoral source of 5-HT in the meninges. Triptans (5-HT1B/D agonists) and ditans (5-HT1F agonists) are the best established 5-HT anti-migraine agents. However, activation of meningeal afferents via ionotropic 5-HT3 receptors results in long-lasting excitatory drive suggesting a pro-nociceptive role for these receptors in migraine. Nevertheless, clinical data do not clearly support the applicability of currently available 5-HT3 antagonists to migraine treatment. The reasons for this might be the presence of 5-HT3 receptors on inhibitory interneurons dampening the excitatory drive, a lack of 5-HT(3)A-E subunit-selective antagonists and gender/age-dependent effects. This review is focusing on the controversial role of 5-HT3 receptors in migraine pathology and related pharmacological perspectives of 5-HT ligands.
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