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Rizatriptan has central antinociceptive effects against durally evoked responses
M J Cumberbatch1, R G Hill, R J Hargreaves
1Merck Sharp & Dohme Research Laboratories, Neuroscience Research Center, Harlow, Essex, UK.
European Journal of Pharmacology
|June 5, 1997
Summary
Rizatriptan, a migraine treatment, shows central nervous system activity. This drug inhibits nociceptive dural responses, suggesting a mechanism for its effectiveness in treating migraine headaches.
Area of Science:
- Neuroscience
- Pharmacology
Background:
- Rizatriptan is a 5-HT(1B/1D) receptor agonist effective for migraine.
- Its peripheral actions include vasoconstriction and inhibition of neurogenic inflammation.
Purpose of the Study:
- To investigate potential central nervous system (CNS) activity of rizatriptan.
- To determine if CNS effects contribute to rizatriptan's antimigraine efficacy.
Main Methods:
- Extracellular recording of action potentials from trigeminal nucleus caudalis neurons in anesthetized rats.
- Electrical stimulation of the dura-mater to evoke nociceptive responses.
Main Results:
- Rizatriptan demonstrated dose-dependent inhibition of nociceptive dural responses.
- A maximum inhibition of 63 +/- 9% was observed at 3 mg/kg, i.v.
Conclusions:
- Rizatriptan exhibits significant central activity.
- This central action likely contributes to its therapeutic effects in migraine treatment.