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Calcitonin gene-related peptide receptor antagonists for migraine

Pages 815-823 | Published online: 19 May 2010

Bibliography

  • Cerbo R, Pesare M, Aurilia C, Socio-economic costs of migraine. J Headache Pain 2004;2:s15-19
  • Amara SG, Jonas V, Rosenfeld MG, Alternative RNA processing in calcitonin gene expression generates mRNAs encoding different polypeptide products. Nature 1982;298:240-4
  • Wimalawansa SJ. Calcitonin gene-related peptide and its receptors: molecular genetics, physiology, pathophysiology, and therapeutic potentials. Endocr Rev 1996;17:533-85
  • Hanko J, Hardebo JE, Kahrstrom J, Calcitonin gene-related peptide is present in mammalian cerebrovascular nerve fibres and dilates pial and peripheral arteries. Neurosci Lett 1985;57:91-5
  • Vega AV, Avila G. CGRP, a vasodilator neuropeptide that stimulates neuromuscular transmission and EC coupling. Curr Vasc Pharmacol 2010;8:394-403
  • Lu JT, Son YJ, Lee J, Mice lacking alpha-calcitonin gene-related peptide exhibit normal cardiovascular regulation and neuromuscular development. Mol Cell Neurosci 1999;14:99-120
  • Kraenzlin ME, Ch'ng JL, Mulderry PK, Infusion of a novel peptide, calcitonin gene-related peptide (CGRP) in man. Pharmacokinetics and effects on gastric acid secretion and on gastrointestinal hormones. Regul Pept 1985;10:189-97
  • Aiyar N, Rand K, Elshourbagy NA, A cDNA encoding the calcitonin gene-related peptide type 1 receptor. J Biol Chem 1996;271:11325-9
  • McLatchie LM, Fraser NJ, Main MJ, RAMPs regulate the transport and ligand specificity of the calcitonin-receptor-like receptor. Nature 1998;393:333-9
  • Ma W, Chabot JG, Powell KJ, Localization and modulation of calcitonin gene-related peptide-receptor component protein-immunoreactive cells in the rat central and peripheral nervous systems. Neuroscience 2003;120:677-94
  • Sams A, Jansen-Olesen I. Expression of calcitonin receptor-like receptor and receptor-activity-modifying proteins in human cranial arteries. Neurosci Lett 1998;258:41-4
  • Koth CM, Abdul-Manan N, Lepre CA, Refolding and characterization of a soluble ectodomain complex of the calcitonin gene-related peptide receptor. Biochemistry 2010;49:1862-72
  • Barwell J, Miller PS, Donnelly D, Poyner DR. Mapping interaction sites within the N-terminus of the calcitonin gene-related peptide receptor; the role of residues 23-60 of the calcitonin receptor-like receptor. Peptides 2010;31:170-6
  • Hay DL, Poyner DR, Smith DM. Desensitisation of adrenomedullin and CGRP receptors. Regul Pept 2003;112:139-45
  • Feindel W, Penfield W, McNaughton FL. The tentorial nerves and localization of intracranial pain in man. Neurology 1960;10:555-63
  • Penfield W. A contribution to the mechanism of intracranial pain. Proc Assoc Res Nerv Mental Dis 1934;15:399-415
  • Ray BS, Wolff HG. Experimental studies on headache: pain-sensitive structures of the head and their significance in headache. Arch Surg 1940;41:813-56
  • Tajti J, Uddman R, Moller S, Messenger molecules and receptor mRNA in the human trigeminal ganglion. J Auton Nerv Syst 1999;76:176-83
  • Skofitsch G, Jacobowitz DM. Calcitonin gene-related peptide coexists with substance P in capsaicin sensitive neurons and sensory ganglia of the rat. Peptides 1985;6:747-54
  • Lee Y, Kawai Y, Shiosaka S, Coexistence of calcitonin gene-related peptide and substance P-like peptide in single cells of the trigeminal ganglion of the rat: immunohistochemical analysis. Brain Res 1985;330:194-6
  • Messlinger K, Hanesch U, Baumgartel M, Innervation of the dura mater encephali of cat and rat: ultrastructure and calcitonin gene-related peptide-like and substance P-like immunoreactivity. Anat Embryol (Berl) 1993;188:219-37
  • Liu Y, Broman J, Edvinsson L. Central projections of the sensory innervation of the rat middle meningeal artery. Brain Res 2008;1208:103-10
  • Mason RT, Peterfreund RA, Sawchenko PE, Release of the predicted calcitonin gene-related peptide from cultured rat trigeminal ganglion cells. Nature 1984;308:653-5
  • Eberhardt M, Hoffmann T, Sauer SK, Calcitonin gene-related peptide release from intact isolated dorsal root and trigeminal ganglia. Neuropeptides 2008;42:311-17
  • Jenkins DW, Langmead CJ, Parsons AA, Strijbos PJ. Regulation of calcitonin gene-related peptide release from rat trigeminal nucleus caudalis slices in vitro. Neurosci Lett 2004;366:241-4
  • Ebersberger A, Averbeck B, Messlinger K, Reeh PW. Release of substance P, calcitonin gene-related peptide and prostaglandin E2 from rat dura mater encephali following electrical and chemical stimulation in vitro. Neuroscience 1999;89:901-7
  • Strecker T, Dux M, Messlinger K. Nitric oxide releases calcitonin-gene-related peptide from rat dura mater encephali promoting increases in meningeal blood flow. J Vasc Res 2002;39:489-96
  • Zimmermann K, Reeh PW, Averbeck B. ATP can enhance the proton-induced CGRP release through P2Y receptors and secondary PGE(2) release in isolated rat dura mater. Pain 2002;97:259-65
  • Fischer MJ, Messlinger K. Cannabinoid and vanilloid effects of R(+)-methanandamide in the hemisected meningeal preparation. Cephalalgia 2007;27:422-8
  • Goadsby PJ, Edvinsson L, Ekman R. Release of vasoactive peptides in the extracerebral circulation of humans and the cat during activation of the trigeminovascular system. Ann Neurol 1988;23:193-6
  • Tfelt-Hansen P, Le H. Calcitonin gene-related peptide in blood: is it increased in the external jugular vein during migraine and cluster headache? A review. J Headache Pain 2009;10:137-43
  • Jansen-Olesen I, Mortensen A, Edvinsson L. Calcitonin gene-related peptide is released from capsaicin-sensitive nerve fibres and induces vasodilatation of human cerebral arteries concomitant with activation of adenylyl cyclase. Cephalalgia 1996;16:310-16
  • Juhasz G, Zsombok T, Modos EA, NO-induced migraine attack: strong increase in plasma calcitonin gene-related peptide (CGRP) concentration and negative correlation with platelet serotonin release. Pain 2003;106:461-70
  • Eberhardt M, Neeb L, Vogel EM, Glyceroltrinitrate facilitates stimulated CGRP release but not gene expression of CGRP or its receptor components in rat trigeminal ganglia. Neuropeptides 2009;43:483-9
  • Price TJ, Flores CM. Critical evaluation of the colocalization between calcitonin gene-related peptide, substance P, transient receptor potential vanilloid subfamily type 1 immunoreactivities, and isolectin B4 binding in primary afferent neurons of the rat and mouse. J Pain 2007;8:263-72
  • Fusco BM, Fiore G, Gallo F, ‘Capsaicin-sensitive’ sensory neurons in cluster headache: pathophysiological aspects and therapeutic indication. Headache 1994;34:132-7
  • Petersen KA, Birk S, Doods H, Inhibitory effect of BIBN4096BS on cephalic vasodilatation induced by CGRP or transcranial electrical stimulation in the rat. Br J Pharmacol 2004;143:697-704
  • Bolay H, Reuter U, Dunn AK, Intrinsic brain activity triggers trigeminal meningeal afferents in a migraine model. Nat Med 2002;8:136-42
  • Le Greves P, Nyberg F, Terenius L, Hokfelt T. Calcitonin gene-related peptide is a potent inhibitor of substance P degradation. Eur J Pharmacol 1985;115:309-11
  • Oku R, Satoh M, Fujii N, Calcitonin gene-related peptide promotes mechanical nociception by potentiating release of substance P from the spinal dorsal horn in rats. Brain Res 1987;403:350-4
  • Mao J, Coghill RC, Kellstein DE, Calcitonin gene-related peptide enhances substance P-induced behaviors via metabolic inhibition: in vivo evidence for a new mechanism of neuromodulation. Brain Res 1992;574:157-63
  • Storer RJ, Akerman S, Goadsby PJ. Calcitonin gene-related peptide (CGRP) modulates nociceptive trigeminovascular transmission in the cat. Br J Pharmacol 2004;142:1171-81
  • Kangrga I, Randic M. Tachykinins and calcitonin gene-related peptide enhance release of endogenous glutamate and aspartate from the rat spinal dorsal horn slice. J Neurosci 1990;10:2026-38
  • Shekhar YC, Anand IS, Sarma R, Effects of prolonged infusion of human alpha calcitonin gene-related peptide on hemodynamics, renal blood flow and hormone levels in congestive heart failure. Am J Cardiol 1991;67:732-6
  • Lassen LH, Haderslev PA, Jacobsen VB, CGRP may play a causative role in migraine. Cephalalgia 2002;22:54-61
  • Recober A, Kuburas A, Zhang Z, Role of calcitonin gene-related peptide in light-aversive behavior: implications for migraine. J Neurosci 2009;29:8798-804
  • Chiba T, Yamaguchi A, Yamatani T, Calcitonin gene-related peptide receptor antagonist human CGRP-(8-37). Am J Physiol 1989;256:E331-3
  • Carpenter KA, Schmidt R, von Mentzer B, Turn structures in CGRP C-terminal analogues promote stable arrangements of key residue side chains. Biochemistry 2001;40:8317-25
  • Vanmolkot FH, Van der Schueren BJ, de Hoon JN. Calcitonin gene-related peptide-induced vasodilation in the human forearm is antagonized by CGRP8-37: evaluation of a human in vivo pharmacodynamic model. Clin Pharmacol Ther 2006;79:263-73
  • Miranda LP, Holder JR, Shi L, Identification of potent, selective, and metabolically stable peptide antagonists to the calcitonin gene-related peptide (CGRP) receptor. J Med Chem 2008;51:7889-97
  • Daines RA, Sham KKC, Taggert JJ, Quinine analogs as non-peptide calcitonin gene-related peptide (CGRP) receptor antagonists. Bioorg Med Chem Lett 1997;7:2673-6
  • Doods H, Hallermayer G, Wu D, Pharmacological profile of BIBN4096BS, the first selective small molecule CGRP antagonist. Br J Pharmacol 2000;129:420-3
  • Aiyar N, Daines RA, Disa J, Pharmacology of SB-273779, a nonpeptide calcitonin gene-related peptide 1 receptor antagonist. J Pharmacol Exp Ther 2001;296:768-75
  • Nichols PL, Brand J, Briggs M, Potent oxadiazole CGRP receptor antagonists for the potential treatment of migraine. Bioorg Med Chem Lett 2010;20:1368-72
  • Mallee JJ, Salvatore CA, LeBourdelles B, Receptor activity-modifying protein 1 determines the species selectivity of non-peptide CGRP receptor antagonists. J Biol Chem 2002;277:14294-8
  • Hasbak P, Saetrum OO, Eskesen K, Investigation of CGRP receptors and peptide pharmacology in human coronary arteries. Characterization with a nonpeptide antagonist. J Pharmacol Exp Ther 2003;304:326-33
  • Vater A, Jarosch F, Buchner K, Klussmann S. Short bioactive Spiegelmers to migraine-associated calcitonin gene-related peptide rapidly identified by a novel approach: tailored-SELEX. Nucleic Acids Res 2003;31:e130
  • Denekas T, Troltzsch M, Vater A, Inhibition of stimulated meningeal blood flow by a calcitonin gene-related peptide binding mirror-image RNA oligonucleotide. Br J Pharmacol 2006;148:536-43
  • Juhl L, Edvinsson L, Olesen J, Jansen-Olesen I. Effect of two novel CGRP-binding compounds in a closed cranial window rat model. Eur J Pharmacol 2007;567:117-24
  • Paone DV, Shaw AW, Nguyen DN, Potent, orally bioavailable calcitonin gene-related peptide receptor antagonists for the treatment of migraine: discovery of N-[(3R,6S)-6-(2,3-difluorophenyl)-2-oxo-1- (2,2,2-trifluoroethyl)azepan-3-yl]-4- (2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin- 1-yl)piperidine-1-carboxamide (MK-0974). J Med Chem 2007;50:5564-7
  • Salvatore CA, Hershey JC, Corcoran HA, Pharmacological characterization of MK-0974 [N-[(3R,6S)-6-(2,3-difluorophenyl)-2-oxo-1-(2,2,2-trifluoroethyl)azepan-3-yl]-4-( 2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxamide], a potent and orally active calcitonin gene-related peptide receptor antagonist for the treatment of migraine. J Pharmacol Exp Ther 2008;324:416-21
  • Bell IM, Bednar RA, Corcoran HA, The identification of potent, orally bioavailable tricyclic CGRP receptor antagonists. Bioorg Med Chem Lett 2009;19:4740-2
  • Wood MR, Schirripa KM, Kim JJ, Novel CGRP receptor antagonists through a design strategy of target simplification with addition of molecular flexibility. Bioorg Med Chem Lett 2009;19:5787-90
  • Stump CA, Bell IM, Bednar RA, The discovery of highly potent CGRP receptor antagonists. Bioorg Med Chem Lett 2009;19:214-17
  • Bell IM, Galliccio SN, Wood MR, Discovery of MK-3207: a highly potent, orally bioavailable CGRP receptor antagonist. ACS Med Chem Lett 2010;1:24-9
  • Salvatore CA, Moore EL, Calamari A, Pharmacological properties of MK-3207 [2-[(8R)-8-(3,-difluorophenyl)-10-oxo-6,9-diazaspiro[4.5]dec-9-yl]-N-[(2R)-2'-ox o-1,1',2',3-tetrahydrospiro[indene-2,3'-pyrrolo[2,3-b]pyridin]-5-yl]acetamide], a potent and orally active CGRP receptor antagonist. J Pharmacol Exp Ther 2010;333:152-60
  • Degnan AP, Chaturvedula PV, Conway CM, Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1H-indazol-5 -yl)-1-oxo-1-(4-(piperidin-1-yl)piperidin-1-yl)propan-2-yl)piperidine-1-carboxami de (BMS-694153): a potent antagonist of the human calcitonin gene-related peptide receptor for migraine with rapid and efficient intranasal exposure. J Med Chem 2008;51:4858-61
  • Peterlin BL, Rapoport AM. Clinical pharmacology of the serotonin receptor agonist, zolmitriptan. Expert Opin Drug Metab Toxicol 2007;3:899-911
  • Diener HC, Evers S. Effectiveness and satisfaction with zolmitriptan 5 mg nasal spray for treatment of migraine in real-life practice: results of a postmarketing surveillance study. Clin Drug Investig 2007;27:59-66
  • Degnan AP, Conway CM, Dalterio RA, Carbamates as potent calcitonin gene-related peptide antagonists with improved solution stability. Bioorg Med Chem Lett 2009;19:3555-8
  • Leniger T, Pageler L, Stude P, Comparison of intravenous valproate with intravenous lysine-acetylsalicylic acid in acute migraine attacks. Headache 2005;45:42-6
  • Williamson DJ, Hargreaves RJ. Neurogenic inflammation in the context of migraine. Microsc Res Tech 2001;53:167-78
  • Fischer MJ, Koulchitsky S, Messlinger K. The nonpeptide calcitonin gene-related peptide receptor antagonist BIBN4096BS lowers the activity of neurons with meningeal input in the rat spinal trigeminal nucleus. J Neurosci 2005;25:5877-83
  • Koulchitsky S, Fischer MJ, Messlinger K. Calcitonin gene-related peptide receptor inhibition reduces neuronal activity induced by prolonged increase in nitric oxide in the rat spinal trigeminal nucleus. Cephalalgia 2009;29:408-17
  • Edvinsson L. CGRP blockers in migraine therapy: where do they act? Br J Pharmacol 2008;155:967-9
  • Levy D, Burstein R, Strassman AM. Calcitonin gene-related peptide does not excite or sensitize meningeal nociceptors: implications for the pathophysiology of migraine. Ann Neurol 2005;58:698-705
  • Sixt ML, Messlinger K, Fischer MJ. Calcitonin gene-related peptide receptor antagonist olcegepant acts in the spinal trigeminal nucleus. Brain 2009;132:3134-41
  • Sur C, Hargreaves R, Bell I, CSF levels and binding pattern of novel CGRP receptor antagonists in rhesus monkey and human central nervous system: toward the development of a PET tracer. Cephalagia 2009;29:136-7
  • Moore EL, Gingell JJ, Kane SA, Mapping the CGRP receptor ligand binding domain. tryptophan-84 of RAMP1 is critical for agonist and antagonist binding. Biochem Biophys Res Commun 2010;394:141-5
  • Miller PS, Barwell J, Poyner DR, Non-peptidic antagonists of the CGRP receptor, BIBN4096BS and MK-0974, interact with the calcitonin receptor-like receptor via methionine-42 and RAMP1 via tryptophan-74. Biochem Biophys Res Commun 2010;391:437-42
  • Poyner DR, Hay DL, Connor AC. CGRP receptor antagonists: design and screening. Exp Opin Drug Discov 2009;4:1253-65
  • Iovino M, Feifel U, Yong CL, Safety, tolerability and pharmacokinetics of BIBN 4096 BS, the first selective small molecule calcitonin gene-related peptide receptor antagonist, following single intravenous administration in healthy volunteers. Cephalalgia 2004;24:645-56
  • Petersen KA, Birk S, Lassen LH, The CGRP-antagonist, BIBN4096BS does not affect cerebral or systemic haemodynamics in healthy volunteers. Cephalalgia 2005;25:139-47
  • Van der Schueren BJ, Rogiers A, Vanmolkot FH, Calcitonin gene-related peptide8-37 antagonizes capsaicin-induced vasodilation in the skin: evaluation of a human in vivo pharmacodynamic model. J Pharmacol Exp Ther 2008;325:248-55
  • Sinclair SR, Kane SA, Van der Schueren BJ, Inhibition of capsaicin-induced increase in dermal blood flow by the oral CGRP receptor antagonist, telcagepant (MK-0974). Br J Clin Pharmacol 2010;69:15-22
  • Petersen KA, Lassen LH, Birk S, BIBN4096BS antagonizes human alpha-calcitonin gene related peptide-induced headache and extracerebral artery dilatation. Clin Pharmacol Ther 2005;77:202-13
  • Olesen J, Diener HC, Husstedt IW, Calcitonin gene-related peptide receptor antagonist BIBN 4096 BS for the acute treatment of migraine. N Engl J Med 2004;350:1104-10
  • Ho TW, Mannix LK, Fan X, Randomized controlled trial of an oral CGRP receptor antagonist, MK-0974, in acute treatment of migraine. Neurology 2008;70:1304-12
  • Ho TW, Ferrari MD, Dodick DW, 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
  • Connor KM, Shapiro RE, Diener HC, Randomized, controlled trial of telcagepant for the acute treatment of migraine. Neurology 2009;73:970-7
  • Han TH, Blanchard RL, Palcza J, Single- and multiple-dose pharmacokinetics and tolerability of telcagepant, an oral calcitonin gene\-related peptide receptor antagonist, in adults. J Clin Pharmacol 2010. [Epub ahead of print]
  • Roller S, Cui D, Laspina C, Preclinical pharmacokinetics of MK-0974, an orally active calcitonin-gene related peptide (CGRP)-receptor antagonist, mechanism of dose dependency and species differences. Xenobiotica 2009;39:33-45
  • Kroeger I, Erhardt A, Abt D, The neuropeptide calcitonin gene-related peptide (CGRP) prevents inflammatory liver injury in mice. J Hepatol 2009;51:342-53
  • Dodick D, Lipton RB, Martin V, Consensus statement: cardiovascular safety profile of triptans (5-HT agonists) in the acute treatment of migraine. Headache 2004;44:414-25
  • Regan CP, Stump GL, Kane SA, Lynch JJ Jr. Calcitonin gene-related peptide receptor antagonism does not affect the severity of myocardial ischemia during atrial pacing in dogs with coronary artery stenosis. J Pharmacol Exp Ther 2009;328:571-8
  • Edvinsson L, Alm R, Shaw D, Effect of the CGRP receptor antagonist BIBN4096BS in human cerebral, coronary and omental arteries and in SK-N-MC cells. Eur J Pharmacol 2002;434:49-53
  • Lynch JJ Jr, Regan CP, Md LE, Comparison of the vasoconstrictor effects of the calcitonin gene-related peptide (CGRP) receptor antagonist telcagepant (MK-0974) and zolmitriptan in human isolated coronary arteries. J Cardiovasc Pharmacol 2010. [Epub ahead of print]
  • Hou JF, Yu LC. Blockade effects of BIBN4096BS on CGRP-induced inhibition on whole-cell K+ currents in spinal dorsal horn neuron of rats. Neurosci Lett 2010;469:15-8
  • Ferrari MD, Roon KI, Lipton RB, Goadsby PJ. Oral triptans (serotonin 5-HT(1B/1D) agonists) in acute migraine treatment: a meta-analysis of 53 trials. Lancet 2001;358:1668-75
  • Tfelt-Hansen PC. Is there an inherent limit to the efficacy of calcitonin gene-related peptide receptor antagonists in the acute treatment of migraine? A comment. J Headache Pain 2009;10:389-91

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