Evidence for serotonin (5-HT)1B, 5-HT1D and 5-HT1F receptor inhibitory effects on trigeminal neurons with craniovascular input.

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Goadsby PJ, Classey JD

Evidence for serotonin (5-HT)1B, 5-HT1D and 5-HT1F receptor inhibitory effects on trigeminal neurons with craniovascular input.

Neuroscience. 2003;122(2):491-8.

PubMed ID

14614913 [ View in PubMed

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Abstract

Development of serotonin (5HT(1B/1D)) agonists for the acute attack of migraine resulted in considerable interest in their action. The superior sagittal sinus (SSS) was isolated in alpha-chloralose (60 mg/kg, i.p. and 20 mg/kg i.v.i. supplementary 2 hourly) anaesthetised cats. The SSS was stimulated electrically (100 V, 250 micros duration, 0.3 Hz) and neurons of the trigeminocervical complex monitored using electrophysiological methods. To test 5-HT(1B) receptor-mediated activity common carotid blood flow (CCF) was monitored with a transonic flow probe placed around the vessel. Naratriptan (5-HT(1B/1D/1F) receptor agonist) and alniditan (5-HT(1B/1D) receptor agonist) produced reductions in carotid blood flow of 38+/-5% and 42+/-6%, respectively. These effects were attenuated by the 5-HT(1B) receptor antagonist SB224289 (P<0.05). LY344864 (5-HT(1F) receptor agonist) had no effect on CCF. Naratriptan inhibited SSS-evoked activity (61+/-7%), an effect partially inhibited by the 5-HT(1B) receptor antagonist SB224289 (30+/-5%), or by the 5-HT(1D) receptor antagonist BRL-15572 (37+/-6%). There remained an inhibitory effect of naratriptan after both 5-HT(1B) and 5-HT(1D) receptor blockade (22+/-5%). Alniditan inhibited SSS-evoked trigeminal activity (53+/-6%), an effect abolished after 5-HT(1B) and 5-HT(1D) receptor blockade. LY344864 (5-HT(1F) receptor agonist) inhibited SSS-evoked trigeminal activity (28+/-5%), an effect unaltered by either SB224289 or BRL-15572. It can be concluded that there are inhibitory 5-HT(1B), 5-HT(1D) and 5-HT(1F) receptors in the trigeminocervical complex of the cat. 5-HT(1B) receptor-mediated inhibition is the most potent of the three in terms of inhibition of trigeminovascular nociceptive traffic.

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Naratriptan	5-hydroxytryptamine receptor 1F	Protein	Humans	Yes	Agonist	Details
Rizatriptan	5-hydroxytryptamine receptor 1F	Protein	Humans	Unknown	Agonist	Details