Hostname: page-component-745bb68f8f-lrblm Total loading time: 0 Render date: 2025-01-23T19:07:52.474Z Has data issue: false hasContentIssue false
  • English
  • Français

The Role of 5-HT1B/1D Receptors in the Treatment of Migraine

Published online by Cambridge University Press:  07 November 2014

Christian Waeber
Get access Rights & Permissions [Opens in a new window]

Abstract

Of all known neurotransmitters, 5-HT is the one most frequently mentioned in the pathophysiology of migraine. This review focuses on the relationship between the efficacy of sumatriptan and other migraine agents and their effects on specific 5-HT receptors in rodent models. These agents are seen to have effects on vascular constriction and the release of vasoactive and inflammatory peptides from trigeminovascular sensory neurons. Specific subtypes of the 5-HT1 receptors appear to mediate these effects.

Type
Feature Article
Information
CNS Spectrums , Volume 3 , Issue 8: Serotonin Subsystems , September 1998 , pp. 30 - 39
Copyright
Copyright © Cambridge University Press 1998

Access options

Get access to the full version of this content by using one of the access options below. (Log in options will check for institutional or personal access. Content may require purchase if you do not have access.)

References

REFERENCES

1.Lipton, RB, Stewart, WF. Epidemiology and comorbidity of migraine. In: Goadsby, PJ, Silberstein, SD, eds. Headache. Boston, Mass: Butterworth-Heinemann; 1997:75–95.Google Scholar
2.Ferrari, MD, Saxena, PR. On serotonin and migraine: a clinical and pharmacological review. Cephalalgia. 1993;13:151–165.Google Scholar
3.Hoyer, D, Clarke, DE, Fozard, JR, et al.Seventh International Union of Pharmacology classification of receptors for 5-hydroxytryptamine (serotonin). Pharmacol Rev. 1994;46:157–203.Google Scholar
4.Fozard, JR, Kalkman, HO. 5-Hydroxytryptamine (5-HT) and the initiation of migraine: new perspectives. Naunyn Schmiedeberg's Arch Pharmacol. 1994;350:225–229.Google Scholar
5.Graham, JR, Wolff, HG. Mechanism of migraine headache and action of ergotamine tartrate. Arch Neurol Psychiatry. 1938;39:737–763.Google Scholar
6.Saxena, PR, Tfelt-Hansen, P. Sumatriptan. In: Olesen, J, Tfelt-Hansen, P, Welch, KMA, eds. The Headaches. New York, NY: Raven Press; 1993:329–341.Google Scholar
7.Moskowitz, MA. Neurogenic versus vascular mechanisms of sumatriptan and ergot alkaloids in migraine. Trends Pharmacol Sci. 1992;13:307–311.Google Scholar
8.Ray, BS, Wolff, HG. Experimental studies on headache: pain-sensitive structures of the head and their significance in headache. Arch Surg. 1940;41:813–856.Google Scholar
9.Bove, GM, Moskowitz, MA. Trigeminal organization with special reference to the trigeminovascular system and cranial pain. In: Yaksh, TL, Lynch, C III, Zapol, WM, Maze, M, Biebuyck, JF, Saidman, LJ, eds. Anesthesia: Biologic Foundations. Philadelphia, Pa: Lippincott-Raven; 1997:859–868.Google Scholar
10.Scharff, L, Turk, DC, Marcus, DA. Triggers of headache episodes and coping responses of headache diagnostic groups. Headache. 1995;35:397–403.CrossRefGoogle ScholarPubMed
11.Ophoff, RA, Terwindt, GM, Vergouwe, MN, et al.Familial hémiplégie migraine and episodic ataxia type-2 are caused by mutations in the Ca2+ channel gene CACNL1A4. Cell. 1996;87:543–552.Google Scholar
12.Page, IH, McCubbin, MD. The variable arterial pressure response to serotonin in laboratory animals and man. Circ Res. 1953;1:354–362.Google Scholar
13.Hamel, E. 5-HT1D Receptors: pharmacology and therapeutic potential. Serotonin. 1996;1:19–29.Google Scholar
14.Hamel, E, Grégoire, L, Lau, B. 5-HT1 receptor mediating contraction in bovine cerebral arteries: a model for human cerebrovascular 5-HT1D/1B receptors. Eur J Pharmacol. 1993;242:75–82.Google Scholar
15.Hamel, E, Fan, E, Linville, D, Ting, V, Villemure, JG, Chia, LS. Expression of mRNA for the serotonin 5-hydrox-ytryptamine1D/1B receptor subtype in human and bovine cerebral arteries. Mol Pharmacol. 1993;44:242–246.Google Scholar
16.Bouchelet, I, Cohen, Z, Case, B, Séguéla, P, Hamel, E. Differential expression of sumatriptan-sensitive 5-hydroxytryptamine receptors in human trigeminal ganglia and cerebral blood vessels. Mol Pharmacol. 1996;50:219–223.Google Scholar
17.MacIntyre, PD, Bhargava, B, Hogg, KJ, Gemmill, JD, Hillis, WS. Effect of subcutaneous sumatriptan, a selective 5-HT1 agonist, on the systemic pulmonary and coronary circulation. Circulation. 1993;87:401–405.Google Scholar
18.Rebeck, GW, Maynard, KI, Hyman, BT, Moskowitz, MA. Selective 5-HT1Dα serotonin receptor gene expression in trigeminal ganglia: implications for antimigraine drug development. Proc Natl Acad Sci USA. 1994;91:3666–3669.Google Scholar
19.Longmore, J, Shaw, D, Smith, D, et al.Differential distribution of 5HT1D- and 5HT1B-immunoreactivity within the human trigemino-cerebrovascular system: implications for the discovery of new antimigraine drugs. Cephalalgia. 1997;17:833–842.Google Scholar
20.Ullmer, C, Schmuck, K, Kalkman, HO, Lübbert, H. Expression of serotonin receptor mRNAs in blood vessels. FEBS Lett. 1995;370:215–221.Google Scholar
21.Markowitz, S, Saito, K, Moskowitz, MA. Neurogenically mediated leakage of plasma protein occurs from blood vessels in dura mater but not brain. J Neurosci. 1987;7:4129–4136.Google Scholar
22.Saito, K, Markowitz, S, Moskowitz, MA. Ergot alkaloids block neurogenic extravasation in dura mater: proposed action in vascular headaches. Ann Neurol. 1988;24:732–737.Google Scholar
23.Buzzi, MG, Moskowitz, MA. The antimigraine drug, sumatriptan (GR43175), selectively blocks neurogenic plasma extravasation from blood vessels in dura mater. Br J Pharmacol. 1990;99:202–206.Google Scholar
24.Buzzi, MG, Moskowitz, MA, Peroutka, SJ, Byun, B. Further characterization of the putative 5-HT receptor which mediates blockade of neurogenic plasma protein extravasation in rat dura mater. Br J Pharmacol. 1991;103:1421–1428.Google Scholar
25.Johnson, KW, Schaus, JM, Durkin, MM, et al.5-HT1F receptor agonists inhibit neurogenic durai inflammation in guinea pigs. Neuroreport. 1997;8:2237–2240.Google Scholar
26.Phebus, LA, Johnson, KW, Zgombick, JM, et al.Characterization of LY344864 as a pharmacological tool to study 5-HT1F receptor: binding affinities, brain penetration and activity in the neurogenic durai inflammation model of migraine. Life Sci. 1997;61:2117–2126.Google Scholar
27.Pauwels, PJ, Tardif, S, Palmier, C, Wurch, T, Colpaert, FC. How efficacious are 5-HT1B/D receptor ligands: an answer from GTPγS binding studies with stably trans-fected C6-glial cell lines. Neuropharmacology. 1997;36:499–512.Google Scholar
28.Lee, WS, Moskowitz, MA. Conformationally restricted sumatriptan analogues, CP-122,288 and CP-122,638 exhibit enhanced potency against neurogenic inflammation in dura mater. Brain Res. 1993;626:303–305.Google Scholar
29.Skingle, M, Beattie, DT, Scopes, DIC, et al.GR127935: a potent and selective 5-HT1D receptor antagonist. Behav Brain Res. 1996;73:157–161.Google Scholar
30.Yu, X-J, Cutrer, FM, Moskowitz, MA, Waeber, C. The 5-HT1D receptor antagonist GR-127,935 prevents inhibitory effects of sumatriptan but not CP-122,288 and 5-CT on neurogenic plasma extravasation within guinea pig dura mater. Neuropharmacology. 1996;36:83–91.Google Scholar
31.Saudou, F, Amara, DA, Dierich, A, et al.Enhanced aggressive behavior in mice lacking 5-HT1B receptor. Science. 1994;265:1875–1878.Google Scholar
32.Yu, X-J, Waeber, C, Castanon, N, et al.5-carboxami-dotryptamine, CP-122,288 and dihydroergotamine but not sumatriptan, CP-93,129 and serotonin-5-O-car-boxymethyl-glycyl-tyrosinamide block durai plasma protein extravasation in knockout mice that lack 5-hydroxytryptamine?B receptors. Mol Pharmacol. 1996;49:761–765.Google ScholarPubMed
33.Waeber, C, Grailhe, R, Yu, XJ, Hen, R, Moskowitz, MA. Putative 5-HT5 receptors: localization in the mouse CNS and lack of effect in the inhibition of durai protein extravasation. Ann NY Acad Sci. In press.Google Scholar
34.Sheng, M, Greenberg, ME. The regulation and function of c-fos and other immediate early genes in the nervous system. Neuron. 1990;4:477–485.Google Scholar
35.Nozaki, K, Moskowitz, MA, Boccalini, P. CP-93,129, sumatriptan, dihydroergotamine block c-fos expression within rat trigeminal nucleus caudalis caused by chemical stimulation of the meninges. Br J Pharmacol. 1992;106:409–415.Google Scholar
36.Nozaki, K, Boccalini, P, Moskowitz, MA. Expression of c-fos-like immunoreactivity in brain stem after meningeal irritation by blood in subarachnoid space. Neuroscience. 1992;49:669–680.Google Scholar
37.Strassman, AM, Vos, BP. Somatotopic and laminar organization of fos-like immunoreactivity in the medullary and upper cervical dorsal horn induced by noxious facial stimulation in the rat. J Comp Neurol. 1993;331:495–516.Google Scholar
38.Cutrer, FM, Schoenfeld, D, Limmroth, V, Panahian, N, Moskowitz, MA. Suppression by the sumatriptan analogue, CP-122,288 of c-fos immunoreactivity in trigeminal nucleus caudalis induced by intracisternal capsaicin. Br J Pharmacol. 1995;114:987–992.Google Scholar
39.Shepheard, SL, Williamson, DJ, Williams, J, Hill, RG, Hargreaves, RJ. Comparison of the effects of sumatriptan and the NK1 antagonist CP-99,994 on plasma extravasation in dura mater and c-fos mRNA expression in trigeminal nucleus caudalis of rats. Neuropharmacology. 1995;34:255–261.Google Scholar
40.Battaglia, G, Rustioni, A. Coexistence of glutamate and substance P in dorsal root ganglion cells of the rat and monkey. J Comp Neurol. 1988;277:302–312.Google Scholar
41.Dougherty, PM, Willis, WD. Enhancement of spinothalamic neuron responses to chemical and mechanical stimuli following combined microiontophoretic application of N-methyl-D-aspartic acid and substance P. Pain. 1991;47:85–93.Google Scholar
42.Cutrer, FM, Moussaoui, S, Garret, C, Moskowitz, MA. The non-peptide neurokinin-1 antagonist, RPR 100893, decreases c-fos expression in trigeminal nucleus caudalis following noxious chemical meningeal stimulation. Neuroscience. 1995;64:741–750.Google Scholar
43.Moskowitz, MA, Nozaki, K, Kraig, RP. Neocortical spreading depression provokes the expression of c-fos protein-like immunoreactivity within trigeminal nucleus caudalis via trigeminovascular mechanisms. J Neurosci. 1993;13:1167–1177.Google Scholar
44.Lauritzen, M. Pathophysiology of the migraine aura. The spreading depression theory. Brain. 1994;117:199–210.Google Scholar