Activation of 5-hydroxytryptamine1B/1D/1F receptors as a mechanism of action of antimigraine drugs

Expert Opinion on Pharmacotherapy

Volumn 14, Issue 12, 2013, Pages 1599-1610

  Ramírez Rosas, Martha B ^a   Labruijere, Sieneke ^a   Villalón, Carlos M ^b   Maassen Vandenbrink, Antoinette ^a  

^a ERASMUS MEDICAL CENTER   (Netherlands)

^b Cinvestav Coapa   (Mexico)

Author keywords

5 HT; 5 HT receptor; Antimigraine drugs; Migraine; Sumatriptan; Triptan

Indexed keywords

1 [2 [4 (4 CARBAMOYLPHENYL) 1 PIPERAZINYL]ETHYL] N METHYLISOCHROMAN 6 CARBOXAMIDE; 3 [2 [2 (4 METHYL 1 PIPERIDINYL)ETHYL] 1 PYRROLIDINESULFONYL]PHENOL; 5 (4 FLUOROBENZAMIDO) 3 (1 METHYL 4 PIPERIDINYL) 1H INDOLE FUMARATE; 5 CARBAMOYLTRYPTAMINE; 5 HYDROXYINDOLEACETIC ACID; ALPHA 1 ADRENERGIC RECEPTOR; ALPHA 1A ADRENERGIC RECEPTOR; ALPHA 1B ADRENERGIC RECEPTOR; ALPHA 1D ADRENERGIC RECEPTOR; ALPHA 2 ADRENERGIC RECEPTOR; ALPHA ADRENERGIC RECEPTOR; ANTIMIGRAINE AGENT; AS 19; CALCITONIN GENE RELATED PEPTIDE; DIHYDROERGOTAMINE; DOPAMINE RECEPTOR; ERGOT ALKALOID; ERGOTAMINE; GLUTAMATE RECEPTOR; LISURIDE; METHYSERGIDE; NEUROPEPTIDE; NEUROTRANSMITTER; RESERPINE; SEROTONIN; SEROTONIN 1B RECEPTOR; SEROTONIN 1D AGONIST; SEROTONIN 1D RECEPTOR; SEROTONIN 1F RECEPTOR; SEROTONIN 7 RECEPTOR; SUMATRIPTAN; TRIPTAN DERIVATIVE; UNCLASSIFIED DRUG; UNINDEXED DRUG; VASOCONSTRICTOR AGENT;

ANALGESIA; CLINICAL TRIAL (TOPIC); CORONARY ARTERY CONSTRICTION; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG DESIGN; DRUG DIFFUSION; DRUG EFFICACY; DRUG HALF LIFE; DRUG MECHANISM; DRUG POTENCY; DRUG PROTEIN BINDING; DRUG SAFETY; DRUG SYNTHESIS; DRUG TOLERABILITY; DRUG WITHDRAWAL; FIRST PASS EFFECT; HEART VALVE FIBROSIS; HUMAN; IC 50; IN VITRO STUDY; IN VIVO STUDY; MIGRAINE; NAUSEA AND VOMITING; NONHUMAN; PATHOPHYSIOLOGY; PLEUROPULMONARY FIBROSIS; PROTEIN FUNCTION; RETROPERITONEAL FIBROSIS; REVIEW; SEROTONINERGIC SYSTEM; THROMBOCYTE AGGREGATION; VASOCONSTRICTION; VASODILATATION;

ANIMALS; CALCITONIN GENE-RELATED PEPTIDE; GLUTAMIC ACID; HUMANS; MIGRAINE DISORDERS; RECEPTORS, SEROTONIN; SEROTONIN RECEPTOR AGONISTS; TRYPTAMINES;

EID: 84880312001     PISSN: 14656566     EISSN: 17447666     Source Type: Journal    
DOI: 10.1517/14656566.2013.806487     Document Type: Review

References (137)

1. Arulmani U, MaassenVanDenBrink A, Villalon CM, et al. Calcitonin gene-related peptide and its role in migraine pathophysiology. Eur J Pharmacol 2004;500:315-30
2. Link AS, Kuris A, Edvinsson L. Treatment of migraine attacks based on the interaction with the trigemino-cerebrovascular system. J Headache Pain 2008;9:5-12
3. Villalon CM, Olesen J. The role of CGRP in the pathophysiology of migraine and efficacy of CGRP receptor antagonists as acute antimigraine drugs. Pharmacol Ther 2009;124:309-23
4. Lipton RB, Stewart WF. The epidemiology of migraine. Eur Neurol 1994;34(Suppl 2):6-11
5. Headache Classification Subcommittee of the International Headache S. The International Classification of Headache Disorders: 2nd edition. Cephalalgia 2004;24(Suppl 1):9-160
6. Humphrey PPA. 5-Hydroxytryptamine and the pathophysiology of migraine. J Neurol 1991;238(Suppl 1):S38-44
7. Villalon CM, Centurion D, Valdivia LF, et al. Migraine: pathophysiology, pharmacology, treatment and future trends. Curr Vasc Pharmacol 2003;1:71-84
8. Humphrey PPA, Feniuk W, Perren MJ, et al. The pharmacology of the novel 5-HT1-like receptor agonist, GR43175. Cephalalgia 1989;9(Suppl 9):23-33
9. Humphrey PPA, Apperley E, Feniuk W, et al. A rational approach to identifying a fundamentally new drug for the treatment of migraine. In: Saxena PR, Wallis DI, Wouters W, Bevan P, editors. Cardiovascular pharmacology of 5-Hydroxytryptamine. Kluwer Academic Press, The Netherlands: 1990. p. 417-31
10. Dalessio DJ. Wolff's headaches and other head pain. Oxford University Press; New York: 1972
11. Saxena PR. 5-Hydroxytryptamine and migraine. In: Saxena PR, editor. Pharmacology of 5-Hydroxytryptamine: prospective therapeutic applications. Kluwer Academic Press; The Netherlands: 1990
12. Sicuteri F, Testi A, Anselmi B. Biochemical investigations in headache: increase in hydroxyindoleacetic excretion during migraine attacks. Int Arch Allergy 1961;19:55-8
13. Kimball RW, Friedman AP, Vallejo E. Effect of serotonin in migraine patients. Neurology 1960;10:107-11
14. Anthony M, Hinterberger H, Lance JW. Plasma serotonin in migraine and stress. Arch Neurol 1967;16:544-52
15. Saxena PR, Villalon CM. Cardiovascular effects of serotonin agonists and antagonists. J Cardiovasc Pharmacol 1990;15(Suppl 7):S17-34
16. Thompson WH. Ergot in the treatment of periodic neuralgias. J Nerv Ment Dis 1894;21:124
17. Baron EP, Tepper SJ. Revisiting the role of ergots in the treatment of migraine and headache. Headache 2010;50:1353-61
18. Stoll A. Zur Kenntnis der Mutterkornalkaloide. Verh Naturf Gest 1920;101:190-1
19. Feniuk W, Humphrey PP, Perren MJ, et al. Rationale for the use of 5-HT1-like agonists in the treatment of migraine. J Neurol 1991;238(Suppl 1):S57-61
20. Saxena PR. The effects of antimigraine drugs on the vascular responses by-5-hydroxytryptamine and related biogenic substances on the external carotid bed of dogs: possible pharmacological implications to their antimigraine action. Headache 1972;12:44-54
21. Saxena PR. Selective vasoconstriction in carotid vascular bed by methysergide: possible relevance to its antimigraine effect. Eur J Pharmacol 1974;27:99-105
22. Hoyer D, Clarke DE, Fozard JR, et al. International Union of Pharmacology classification of receptors for 5-hydroxytryptamine (Serotonin). Pharmacol Rev 1994;46:157-203
23. Saxena PR, De Vries P, Villalon CM. 5-HT1-like receptors: a time to bid goodbye. Trends Pharmacol Sci 1998;19:311-16
24. Humphrey PP, Feniuk W, Perren MJ, et al. The pharmacology of the novel 5-HT1-like receptor agonist, GR43175. Cephalalgia 1989;9(Suppl 9):23-33
25. Villalon CM, Ramirez-San Juan E, Castillo C, et al. Pharmacological profile of the receptors that mediate external carotid vasoconstriction by 5-HT in vagosympathectomized dogs. Br J Pharmacol 1995;116:2778-84
26. Villalon CM, Sanchez-Lopez A, Centurion D. Operational characteristics of the 5-HT1-like receptors mediating external carotid vasoconstriction in vagosympathectomized dogs. Close resemblance to the 5-HT1D receptor subtype. Naunyn Schmiedebergs Arch Pharmacol 1996;354:550-6
27. Villalon CM, Centurion D, Sanchez-Lopez A, et al. 5-HT receptors mediating external carotid vasoconstriction in vagosympathectomized dogs. Zhongguo Yao Li Xue Bao 1999;20:1057-67
28. Ferrari MD, Saxena PR. Clinical and experimental effects of sumatriptan in humans. Trends Pharmacol Sci 1993;14:129-33
29. MaassenVanDenBrink A, Reekers M, Bax WA, et al. Coronary side-effect potential of current and prospective antimigraine drugs. Circulation 1998;98:25-30
30. Tfelt-Hansen PC, Koehler PJ. History of the use of ergotamine and dihydroergotamine in migraine from 1906 and onward. Cephalalgia 2008;28:877-86
31. Silberstein SD, McCrory DC. Ergotamine and dihydroergotamine: history, pharmacology, and efficacy. Headache 2003;43:144-66
32. Silberstein SD. Methysergide. Cephalalgia 1998;18:421-35
33. Koehler PJ, Tfelt-Hansen PC. History of methysergide in migraine. Cephalalgia 2008;28:1126-35
34. Tfelt-Hansen PC, Jensen RH. Management of cluster headache. CNS Drugs 2012;26:571-80
35. Halker R, Vargas B, Dodick DW. Cluster headache: diagnosis and treatment. Semin Neurol 2010;30:175-85
36. Dahlof C, MaassenVanDenBrink A. Dihydroergotamine, ergotamine, methysergide and sumatriptan-basic science in relation to migraine treatment. Headache 2012;52:707-14
37. D'Andrea G, D'Arrigo A, Dalle Carbonare M, et al. Pathogenesis of migraine: role of neuromodulators. Headache 2012;52:1155-63
38. Edvinsson L, Villalon CM, MaassenVanDenBrink A. Basic mechanisms of migraine and its acute treatment. Pharmacol Ther 2012;136:319-33
39. Tfelt-Hansen PC, Koehler PJ. One hundred years of migraine research: major clinical and scientific observations from 1910 to 2010. Headache 2011;51:752-78
40. Halloul Z, Meyer F, Lippert H, et al. Ergotamine-induced acute vascular insufficiency of the lower limb-a case report. Angiology 2001;52:217-21
41. Silberstein S. MAP0004: dihydroergotamine mesylate inhalation aerosol for acute treatment of migraine. Expert Opin Pharmacother 2012;13:1961-8
42. Tepper SJ, Kori SH, Borland SW, et al. Efficacy and safety of MAP0004, orally inhaled DHE in treating migraines with and without allodynia. Headache 2012;52:37-47
43. Saxena PR, Den Boer MO. Pharmacology of antimigraine drugs. J Neurol 1991;238(Suppl 1):S28-35
44. Humphrey PPA. The discovery and development of the triptans, a major therapeutic breakthrough. Headache 2008;48:685-7
45. Goadsby PJ, Lipton RB, Ferrari MD. Migraine-current understanding and treatment. N Engl J Med 2002;346:257-70
46. Van den Broek RW, Bhalla P, MaassenVanDenBrink A, et al. Characterization of sumatriptan-induced contractions in human isolated blood vessels using selective 5-HT1B and 1D receptor antagonists and in situ hybridization. Cephalalgia 2002;22:83-93
47. Longmore J, Razzaque Z, Shaw D, et al. Comparison of the vasoconstrictor effects of rizatriptan and sumatriptan in human isolated cranial arteries: immunohistological demonstration of the involvement of 5-HT1B-receptors. Br J Clin Pharmacol 1998;46:577-82
48. Nilsson T, Longmore J, Shaw D, et al. Contractile 5-HT1B receptors in human cerebral arteries: pharmacological characterization and localization with immunocytochemistry. Br J Pharmacol 1999;128:1133-40
49. Deleu D, Hanssens Y. Current and emerging second-generation triptans in acute migraine therapy: a comparative review. J Clin Pharmacol 2000;40:687-700
50. Neeb L, Meents J, Reuter U. 5-HT(1F) Receptor agonists: a new treatment option for migraine attacks? Neurotherapeutics 2010;7:176-82
51. Castro ME, Pascual J, Romon T, et al. Differential distribution of [3H] sumatriptan binding sites (5-HT1B, 5-HT1D and 5-HT1F receptors) in human brain: focus on brainstem and spinal cord. Neuropharmacology 1997;36:535-42
52. Edvinsson L, Villalon CM. MaassenVanDenBrink A. Basic mechanisms of migraine and its acute treatment. Pharmacol Ther 2012;136:319-33
53. Ahn AH, Basbaum AI. Where do triptans act in the treatment of migraine? Pain 2005;115:1-4
54. Nelson DL, Phebus LA, Johnson KW, et al. Preclinical pharmacological profile of the selective 5-HT1F receptor agonist lasmiditan. Cephalalgia 2010;30:1159-69
55. Kalra AA, Elliott D. Acute migraine: current treatment and emerging therapies. Ther Clin Risk Manag 2007;3:449-59
56. Goadsby PJ, Edvinsson L, Ekman R. Vasoactive peptide release in the extracerebral circulation of humans during migraine headache. Ann Neurol 1990;28:183-7
57. Bellamy JL, Cady RK, Durham PL. Salivary levels of CGRP and VIP in rhinosinusitis and migraine patients. Headache 2006;46:24-33
58. Goadsby PJ, Edvinsson L. The trigeminovascular system and migraine: studies characterizing cerebrovascular and neuropeptide changes seen in humans and cats. Ann Neurol 1993;33:48-56
59. Shields KG, Goadsby PJ. Serotonin receptors modulate trigeminovascular responses in ventroposteromedial nucleus of thalamus: a migraine target? Neurobiol Dis 2006;23:491-501
60. De Hoon JN, Willigers JM, Troost J, et al. Vascular effects of 5-HT1B/1Dreceptor agonists in patients with migraine headaches. Clin Pharmacol Ther 2000;68:418-26
61. Vanmolkot FH, de Hoon JN. Acute effects of sumatriptan on aortic blood pressure, stiffness, and pressure waveform. Clin Pharmacol Ther 2006;80:85-94
62. MacIntyre PD, Bhargava B, Hogg KJ, et al. Effect of subcutaneous sumatriptan, a selective 5HT1 agonist, on the systemic, pulmonary, and coronary circulation. Circulation 1993;87:401-5
63. Dodick DW, Lipton RB, Martin V, et al. Consensus statement: cardiovascular safety profile of triptans (5-HT agonists) in the acute treatment of migraine. Headache 2004;44:414-25
64. MaassenVanDenBrink A, van den Broek RW, de Vries R, et al. Craniovascular selectivity of eletriptan and sumatriptan in human isolated blood vessels. Neurology 2000;55:1524-30
65. Ferrari A, Tiraferri I, Neri L, et al. Why pharmacokinetic differences among oral triptans have little clinical importance: a comment. J Headache Pain 2011;12:5-12
66. Johnston MM, Rapoport AM. Triptans for the management of migraine. Drugs 2010;70:1505-18
67. Fowler PA, Lacey LF, Thomas M, et al. The clinical pharmacology, pharmacokinetics and metabolism of sumatriptan. Eur Neurol 1991;31:291-4
68. Tfelt-Hansen P, Hougaard A. Sumatriptan : a review of its pharmacokinetics, pharmacodynamics and efficacy in the acute treatment of migraine. Expert Opin Drug Metab Toxicol 2013;9:91-103
69. Isaac M, Slassi A. Recent advances in 5-HT(1D)-selective agonists. IDrugs 2001;4:189-96
70. Villalon CM, Centurion D, Valdivia LF, et al. Migraine: pathophysiology, pharmacology, treatment and future trends. Curr Vasc Pharmacol 2003;1:71-84
71. Tfelt-Hansen P, De Vries P, Saxena PR. Triptans in migraine: a comparative review of pharmacology, pharmacokinetics and efficacy. Drugs 2000;60:1259-87
72. Ferrari MD, Roon KI, Lipton RB, et al. Oral triptans (serotonin 5-HT(1B/1D) agonists) in acute migraine treatment: a meta-analysis of 53 trials. Lancet 2001;358:1668-75
73. Valade D. Early treatment of acute migraine: new evidence of benefits. Cephalalgia 2009;29(Suppl 3):15-21
74. Olesen J, Ashina M. Emerging migraine treatments and drug targets. Trends Pharmacol Sci 2011;32:352-9
75. Voglis G, Tavernarakis N. The role of synaptic ion channels in synaptic plasticity. EMBO Rep 2006;7:1104-10
76. Vikelis M, Mitsikostas DD. The role of glutamate and its receptors in migraine. CNS Neurol Disord Drug Targets 2007;6:251-7
77. D'Andrea G, Cananzi AR, Joseph R, et al. Platelet glycine, glutamate and aspartate in primary headache. Cephalalgia 1991;11:197-200
78. Kai-Kai MA, Howe R. Glutamate-immunoreactivity in the trigeminal and dorsal root ganglia, and intraspinal neurons and fibres in the dorsal horn of the rat. Histochem J 1991;23:171-9
79. Tallaksen-Greene SJ, Young AB, Penney JB, et al. Excitatory amino acid binding sites in the trigeminal principal sensory and spinal trigeminal nuclei of the rat. Neurosci Lett 1992;141:79-83
80. Andreou AP, Goadsby PJ. Therapeutic potential of novel glutamate receptor antagonists in migraine. Expert Opin Investig Drugs 2009;18:789-803
81. Cananzi AR, D'Andrea G, Perini F, et al. Platelet and plasma levels of glutamate and glutamine in migraine with and without aura. Cephalalgia 1995;15:132-5
82. Edvinsson L, Ekman R, Jansen I, et al. Calcitonin gene-related peptide and cerebral blood vessels: distribution and vasomotor effects. J Cereb Blood Flow Metab 1987;7:720-8
83. Lassen LH, Haderslev PA, Jacobsen VB, et al. CGRP may play a causative role in migraine. Cephalalgia 2002;22:54-61
84. Ho TW, Ferrari MD, Dodick DW, et al. Efficacy and tolerability of MK-0974 (telcagepant), a new oral antagonist of calcitonin gene-related peptide receptor, compared with zolmitriptan for acute migraine: a randomised, placebo-controlled, parallel-treatment trial. Lancet 2008;372:2115-23
85. Edvinsson L, Ho TW. CGRP receptor antagonism and migraine. Neurotherapeutics 2010;7:164-75
86. Goadsby PJ. Recent advances in understanding migraine mechanisms, molecules and therapeutics. Trends Mol Med 2007;13:39-44
87. Eftekhari S, Salvatore CA, Calamari A, et al. Differential distribution of calcitonin gene-related peptide and its receptor components in the human trigeminal ganglion. Neuroscience 2010;169:683-96
88. Liu Y, Broman J, Zhang M, et al. Brainstem and thalamic projections from a craniovascular sensory nervous centre in the rostral cervical spinal dorsal horn of rats. Cephalalgia 2009;29:935-48
89. Smith D, Hill RG, Edvinsson L, et al. An immunocytochemical investigation of human trigeminal nucleus caudalis: CGRP, substance P and 5-HT1D-receptor immunoreactivities are expressed by trigeminal sensory fibres. Cephalalgia 2002;22:424-31
90. Unger JW, Lange W. Immunohistochemical mapping of neurophysins and calcitonin gene-related peptide in the human brainstem and cervical spinal cord. J Chem Neuroanat 1991;4:299-309
91. Eftekhari S, Edvinsson L. Possible sites of action of the new calcitonin gene-related peptide receptor antagonists. Ther Adv Neurol Disord 2010;3:369-78
92. Chan KY, Gupta S, de Vries R, et al. Effects of ionotropic glutamate receptor antagonists on rat dural artery diameter in an intravital microscopy model. Br J Pharmacol 2010;160:1316-25
93. Xiao Y, Richter JA, Hurley JH. Release of glutamate and CGRP from trigeminal ganglion neurons: role of calcium channels and 5-HT1 receptor signaling. Mol Pain 2008;4:12
94. Gu XL, Yu LC. The colocalization of CGRP receptor and AMPA receptor in the spinal dorsal horn neuron of rat: a morphological and electrophysiological study. Neurosci Lett 2007;414:237-41
95. Ceruti S, Villa G, Fumagalli M, et al. Calcitonin gene-related peptide-mediated enhancement of purinergic neuron/glia communication by the algogenic factor bradykinin in mouse trigeminal ganglia from wild-type and R192Q Cav2.1 Knock-in mice: implications for basic mechanisms of migraine pain. J Neurosci 2011;31:3638-49
96. Ma QP. Co-localization of 5-HT(1B/1D/1F) receptors and glutamate in trigeminal ganglia in rats. Neuroreport 2001;12:1589-91
97. Choi IS, Cho JH, An CH, et al. 5-HT (1B) receptors inhibit glutamate release from primary afferent terminals in rat medullary dorsal horn neurons. Br J Pharmacol 2012;167:356-67
98. Guo JD, Rainnie DG. Presynaptic 5-HT (1B) receptor-mediated serotonergic inhibition of glutamate transmission in the bed nucleus of the stria terminalis. Neuroscience 2010;165:1390-401
99. Fink KB, Gothert M. 5-HT receptor regulation of neurotransmitter release. Pharmacol Rev 2007;59:360-417
100. McCall RB, Huff R, Chio CL, et al. Preclinical studies characterizing the anti-migraine and cardiovascular effects of the selective 5-HT1D receptor agonist PNU-142633. Cephalalgia 2002;22:799-806
101. Castro ME, Pascual J, Romon T, et al. Differential distribution of [3H] sumatriptan binding sites (5-HT1B, 5-HT1D and 5-HT1F receptors) in human brain: focus on brainstem and spinal cord. Neuropharmacology 1997;36:535-42
102. Pascual J, Del Arco C, Romon T, et al. [3H]Sumatriptan binding sites in human brain: regional-dependent labelling of 5-HT1D and 5-HT1F receptors. Eur J Pharmacol 1996;295:271-4
103. Phebus LA, Johnson KW, Zgombick JM, et al. Characterization of LY344864 as a pharmacological tool to study 5-HT1F receptors: binding affinities, brain penetration and activity in the neurogenic dural inflammation model of migraine. Life Sci 1997;61:2117-26
104. Gomez-Mancilla B, Cutler NR, Leibowitz MT, et al. Safety and efficacy of PNU-142633, a selective 5-HT1D agonist, in patients with acute migraine. Cephalalgia 2001;21:727-32
105. Ferrari MD. Re: gomez-Mancilla et al. Safety and efficacy of PNU-142633, a selective 5-HT(1D) agonist, in patients with acute migraine. Cephalalgia 2001;21:727-32. Cephalalgia 2001;21:711
106. Shepheard S, Edvinsson L, Cumberbatch M, et al. Possible antimigraine mechanisms of action of the 5HT1F receptor agonist LY334370. Cephalalgia 1999;19:851-8
107. Ferrari MD, Farkkila M, Reuter U, et al. Acute treatment of migraine with the selective 5-HT1F receptor agonist lasmiditan-a randomised proof-of-concept trial. Cephalalgia 2010;30:1170-8
108. Farkkila M, Diener HC, Geraud G, et al. Efficacy and tolerability of lasmiditan, an oral 5-HT(1F) receptor agonist, for the acute treatment of migraine: a phase 2 randomised, placebo-controlled, parallel-group, dose-ranging study. Lancet Neurol 2012;11:405-13
109. Vaughan D, Speed J, Medve R, et al. Safety and pharmacokinetics of NXN-188 after single and multiple doses in five phase I, randomized, double-blind, parallel studies in healthy adult volunteers. Clin Ther 2010;32:146-60
110. Bhatt DK, Gupta S, Jansen-Olesen I, et al. NXN-188, a selective nNOS inhibitor and a 5-HT1B/1D receptor agonist, inhibits CGRP release in preclinical migraine models. Cephalalgia 2013;33:87-100
111. Villalon CM, Centurion D, Lujan-Estrada M, et al. Mediation of 5-HT-induced external carotid vasodilatation in GR 127935-pretreated vagosympathectomized dogs by the putative 5-HT7 receptor. Br J Pharmacol 1997;120:1319-27
112. Cardenas CG, Mar LP, Vysokanov AV, et al. Serotonergic modulation of hyperpolarization-activated current in acutely isolated rat dorsal root ganglion neurons. J Physiol 1999;518(Pt 2):507-23
113. Pierce PA, Xie GX, Peroutka SJ, et al. Dual effect of the serotonin agonist, sumatriptan, on peripheral neurogenic inflammation. Reg Anesth 1996;21:219-25
114. Taiwo YO, Levine JD. Serotonin is a directly-acting hyperalgesic agent in the rat. Neuroscience 1992;48:485-90
115. Mahe C, Loetscher E, Dev KK, et al. Serotonin 5-HT7 receptors coupled to induction of interleukin-6 in human microglial MC-3 cells. Neuropharmacology 2005;49:40-7
116. Brenchat A, Romero L, Garcia M, et al. 5-HT7 receptor activation inhibits mechanical hypersensitivity secondary to capsaicin sensitization in mice. Pain 2009;141:239-47
117. Wang X, Fang Y, Liang J, et al. Selective inhibition of 5-HT7 receptor reduces CGRP release in an experimental model for migraine. Headache 2010;50:579-87
118. Agosti RM. 5HT1F-and 5HT7-receptor agonists for the treatment of migraines. CNS Neurol Disord Drug Targets 2007;6:235-7
119. Terron JA, Martinez-Garcia E. 5-HT7 receptor-mediated dilatation in the middle meningeal artery of anesthetized rats. Eur J Pharmacol 2007;560:56-60
120. Bigal ME, Lipton RB. Excessive acute migraine medication use and migraine progression. Neurology 2008;71:1821-8
121. Leysen JE, Gommeren W, Heylen L, et al. Alniditan, a new 5-hydroxytryptamine1D agonist and migraine-abortive agent: ligand-binding properties of human 5-hydroxytryptamine1D alpha, human 5-hydroxytryptamine1D beta, and calf 5-hydroxytryptamine1D receptors investigated with [3H]5-hydroxytryptamine and [3H]alniditan. Molecular pharmacology 1996;50:1567-80
122. Hoyer D. Functional correlates of serotonin 5-HT1 recognition sites. J Recept Res 1988;8:59-81
123. Beer MS, Heald MA, McAllister G, et al. Pharmacological characterisation of a cloned dog 5-HT1B receptor cell line. Eur J Pharmacol 1998;360:117-21
124. Parker EM, Izzarelli DG, Lewis-Higgins L, et al. Two amino acid differences in the sixth transmembrane domain are partially responsible for the pharmacological differences between the 5-HT1D beta and 5-HT1E 5-hydroxytryptamine receptors. J Neurochem 1996;67:2096-103
125. Adham N, Kao HT, Schecter LE, et al. Cloning of another human serotonin receptor (5-HT1F): a fifth 5-HT1 receptor subtype coupled to the inhibition of adenylate cyclase. Proc Natl Acad Sci USA 1993;90:408-12
126. Glusa E, Roos A. Endothelial 5-HT receptors mediate relaxation of porcine pulmonary arteries in response to ergotamine and dihydroergotamine. Br J Pharmacol 1996;119:330-4
127. Baxter GS, Murphy OE, Blackburn TP. Further characterization of 5-hydroxytryptamine receptors (putative 5-HT2B) in rat stomach fundus longitudinal muscle. Br J Pharmacol 1994;112:323-31
128. Leysen JE, Gommeren W. In vitro binding profile of drugs used in migraine. Pitman Publishing Ltd; London: 1984
129. Peroutka SJ, McCarthy BG. Sumatriptan (GR 43175) interacts selectively with 5-HT1B and 5-HT1D binding sites. Eur J Pharmacol 1989;163:133-6
130. Leysen JE. Serotonin Binding sites. Raven Press; New York: 1985
131. Gornemann T, Jahnichen S, Schurad B, et al. Pharmacological properties of a wide array of ergolines at functional alpha(1)-adrenoceptor subtypes. Naunyn Schmiedebergs Arch Pharmacol 2008;376:321-30
132. Newman-Tancredi A, Conte C, Chaput C, et al. Agonist activity of antimigraine drugs at recombinant human 5-HT1A receptors: potential implications for prophylactic and acute therapy. Naunyn Schmiedebergs Arch Pharmacol 1997;355:682-8
133. Napier C, Stewart M, Melrose H, et al. Characterisation of the 5-HT receptor binding profile of eletriptan and kinetics of [3H]eletriptan binding at human 5-HT1B and 5-HT1D receptors. Eur J Pharmacol 1999;368:259-68
134. Wainscott DB, Krushinski JH Jr, Audia JE, et al. [3H]LY334370, a novel radioligand for the 5-HT1F receptor. I. In vitro characterization of binding properties. Naunyn Schmiedebergs Arch Pharmacol 2005;371:169-77
135. Ruat M, Traiffort E, Leurs R, et al. Molecular cloning, characterization, and localization of a high-affinity serotonin receptor (5-HT7) activating cAMP formation. Proc Natl Acad Sci USA 1993;90:8547-51
136. Pregenzer JF, Alberts GL, Im WB, et al. Differential pharmacology between the guinea-pig and the gorilla 5-HT1D receptor as probed with isochromans (5-HT1D-selective ligands). Br J Pharmacol 1999;127:468-72
137. Lovell PJ, Bromidge SM, Dabbs S, et al. A novel, potent, and selective 5-HT(7) antagonist: (R)-3-(2-(2-(4-methylpiperidin-1-yl)ethyl)pyrrolidine-1- sulfonyl) phen ol (SB-269970). J Med Chem 2000;43:342-5