The biology of serotonin receptors: focus on migraine pathophysiology and treatment.
Can
J Neurol Sci. 1999 Nov;26 Suppl 3:S2-6.
Hamel E
Montreal Neurological Institute, McGill University, QC, Canada.
Serotonin receptors are highly heterogeneous and they have been
regrouped within seven different families (5-HT1-5-HT7). With the
exception of the 5-HT3 which is a ligand-gated ion channel, all others
are G-protein coupled receptors with each family sharing structural,
pharmacological and transductional characteristics. 5-HT receptors have
been implicated in the regulation of several psychiatric and
neurological disorders related to serotonergic neurotransmission, and
specific receptor subtypes have recently been associated with either
the pathogenesis or the treatment of migraine headache. In this
respect, activation of vascular 5-HT2B and/or 5-HT7 receptors, possibly
as a consequence of the sudden rise in 5-HT levels reported at the
onset of a migraine attack, would hypothetically result in dilation of
cerebral blood vessels and concomitant activation of sensory
trigeminovascular afferents, hence initiating the manifestation of head
pain. At this stage in the migraine process, activation of specific
subtypes of 5-HT1 receptors has proven clinically effective in
relieving migraine pain. Neural 5-HT1D and/or 5-HT1F receptors
localized pre-junctionally on trigeminovascular afferents appear to
mediate the triptan-induced inhibition of the neurogenic inflammatory
response, with possible additional sites of action for brain penetrant
5-HT1 receptor
agonists in inhibiting the transmission of pain centrally. In contrast,
activation of vascular 5-HT1B receptors would constrict meningeal
vessels hence recovering their pre-migraine diameter. The recent
availability of subtype selective 5-HT1D and 5-HT1F receptor agonists
should allow a further test of the neural/vascular hypothesis and could
possibly lead to antimigraine drugs with a safer cardiovascular profile.
PMID: 10563226Entrez PubMed
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