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5‐Hydroxtryptamine 1D Receptor Agonism Predicts Antimigraine Efficacy
Author(s) -
Anastasia V.,
Deliganis B.S.,
Peroutka Stephen J.
Publication year - 1991
Publication title -
headache: the journal of head and face pain
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.14
H-Index - 119
eISSN - 1526-4610
pISSN - 0017-8748
DOI - 10.1111/j.1526-4610.1991.hed3104228.x
Subject(s) - migraine , pharmacology , cyclase , methysergide , agonist , receptor , medicine , ergotamine , chemistry , endocrinology , serotonin
SYNOPSIS The interactions of four abortive anti‐migraine agents and four prophylactic anti‐migraine agents with 5‐HT 1D receptors in bovine brain were analyzed using radioligand binding techniques and adenylate cyclase assays. In bovine caudate, the affinities of abortive anti‐migraine agents (i.e. 5‐hydroxytryp‐tamine, ergotamine, dihydroergotamine, sumatriptan) for 5‐HT 1D receptors range from 4.0 – 34 nM while the affinities of prophylactic anti‐migraine agents (i.e. methysergide, amitriptyline, (‐)propranolol, verapamil) range from 46 – 11,000 nM. In adenylate cyclase studies in bovine substantia nigra, all four abortive anti‐migraine agents dose‐dependently inhibit forskolin‐stimulated adenylate cyclase activity, a biochemical effect mediated by 5‐HT 1D receptors. No agonist effect on cyclase activity is observed with the four prophylactic anti‐migraine agents. These date support the hypothesis that abortive anti‐migraine agents are 5‐HT 1D receptor agonists and that this effect may underlie their anti‐migraine efficacy.