Source of grant support: This work was supported in part by the Stanley Foundation and NIH Grant NS 12151-15.
5-Hydroxtryptamine 1D Receptor Agonism Predicts Antimigraine Efficacy
Article first published online: 20 MAY 2005
Headache: The Journal of Head and Face Pain
Volume 31, Issue 4, pages 228–231, April 1991
How to Cite
Anastasia, V., Deliganis, B.S. and Peroutka, S. J. (1991), 5-Hydroxtryptamine 1D Receptor Agonism Predicts Antimigraine Efficacy. Headache: The Journal of Head and Face Pain, 31: 228–231. doi: 10.1111/j.1526-4610.1991.hed3104228.x
- Issue published online: 20 MAY 2005
- Article first published online: 20 MAY 2005
- Accepted for Publication: January 3, 1991.
- Cited By
The interactions of four abortive anti-migraine agents and four prophylactic anti-migraine agents with 5-HT1D 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-HT1D 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-HT1D 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-HT1D receptor agonists and that this effect may underlie their anti-migraine efficacy.