5-HT1F receptor agonists in acute migraine treatment: a hypothesis.

Abstract

Serotonin-1F receptor (5-HT1F) agonists may relieve acute migraine without vasoconstriction. We conducted a review of preclinical and clinical data that assessed the potential link between migraine and 5-HT1F activation. (i) A high correlation exists between the potency of various 5-HT1 receptor agonists in the guinea pig dural plasma protein extravasation assay and their 5-HT1F receptor binding affinity. (ii) 5-HT1F receptors are on the trigeminal system, and may participate in blocking migraine pain transmission through the trigeminal ganglion and nucleus caudalis. (iii) 5-HT1F receptors are located on glutamate-containing neurones and their activation might inhibit glutamate release; glutamate excess may play a role in migraine. (iv) Selective 5-HT1F receptor agonists (LY334370; LY344864) are effective in preclinical migraine models and are non-vasoconstrictive. (v) LY334370 is effective in acute migraine, and does not cause any symptoms/signs of coronary vasoconstriction. Preclinical experiments and clinical observations argue for a role of selective 5-HT1F agonists in migraine.

• Authors: N M Ramadan, V Skljarevski, L A Phebus, K W Johnson
• Journal: Cephalalgia : an international journal of headache (Cephalalgia) Vol. 23 Issue 8 Pg. 776-85 (Oct 2003) ISSN: 0333-1024 [Print] England
• PMID: 14510923 (Publication Type: Journal Article, Review)

Chemical References

• Receptors, Serotonin
• Serotonin Receptor Agonists
• serotonin 1F receptor

Topics

• Acute Disease
• Animals
• Clinical Trials as Topic (statistics & numerical data)
• Humans
• Migraine Disorders (drug therapy, metabolism)
• Receptors, Serotonin (metabolism)
• Serotonin Receptor Agonists (therapeutic use)