[3H]Sumatriptan binding sites in human brain: regional-dependent labelling of 5-HT1D and 5-HT1F receptors

Inhibition of trigeminal neurones after intravenous administration of naratriptan through an action at 5‐hydroxy‐tryptamine (5‐HT1B/1D) receptors

“…Functional anatomical evidence from autoradiographic studies is consistent with the data of this study. By use of [ 3 H]‐sumatriptan, binding has been found in the dorsal horn of the upper cervical spinal cord and caudal trigeminal nucleus caudalis in cat (Mills & Martin, 1995), guinea‐pig (Waeber & Moskowitz, 1995) and man (Pascual et al , 1996). A similar distribution can be seen for [ 3 H]‐dihydroergotamine (Goadsby & Gundlach, 1991), which binds 5‐HT receptors that sumatriptan activates (Hamblin et al , 1987; Humphrey et al , 1991), and for another member of this drug class, zolmitriptan (Goadsby & Knight, 1997).…”

Neurobiology in primary headaches

“…In an attempt to characterize the receptors involved it has been suggested that the 5HT 1B receptors are present in very low concentrations in all these nuclei in man (below 12% of total specific binding), while the 5HT 1D receptors account for about 50% of the total specific sumatriptan binding [126]. In addition, a significant amount of 5HT 1F -binding sites can be seen [25,153]. The 5HT 1F site has been examined using a specific agonist LY334370 [170].…”

New targets in the acute treatment of headache

“…Unfortunately development was stopped because of a nonhuman toxicity problem. 5HT 1F receptors are found in the trigeminal nucleus [20][21][22][23] and trigeminal ganglion [24]. 5HT 1F receptor activation is inhibitory in the trigeminal nucleus in rat [25] and cat, albeit seeming less potent in cat than 5HT 1B or 5HT 1D receptor activation [26].…”