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5-HT2 receptor antagonists and migraine therapy
1Department of Pharmacology, University of Sydney, NSW, Australia.
Journal of Neurology
|January 1, 1991
Summary
Several 5-HT2 receptor antagonists are effective for migraine prophylaxis. Pizotifen is preferred due to efficacy and fewer side effects, suggesting 5-HT1C receptor involvement in migraine pathogenesis.
Area of Science:
- Neuroscience
- Pharmacology
Background:
- 5-Hydroxytryptamine (5-HT; serotonin) plays a role in migraine pathophysiology.
- Several 5-HT2 receptor antagonists (methysergide, pizotifen, cyproheptadine, mianserin) are effective in migraine prophylaxis.
Purpose of the Study:
- To evaluate the efficacy of 5-HT2 receptor antagonists in migraine prophylaxis.
- To investigate the potential role of 5-HT1C receptors in migraine pathogenesis.
Main Methods:
- Clinical efficacy assessment of various 5-HT2 receptor antagonists.
- Receptor binding affinity studies to determine interactions with 5-HT2 and 5-HT1C sites.
Main Results:
- Pizotifen demonstrates superior efficacy and a better side-effect profile compared to cyproheptadine, methysergide, and mianserin.
- Ketanserin, a selective 5-HT2 antagonist, was ineffective, while agents with 5-HT1C affinity showed efficacy.
- Agents with non-5-HT receptor antagonism provided no benefit.
Conclusions:
- 5-HT2 receptor antagonism is beneficial for migraine prophylaxis.
- High affinity for 5-HT1C binding sites may be crucial for antimigraine action, suggesting its involvement in migraine pathogenesis.