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BIBN4096BS antagonizes human alpha-calcitonin gene related peptide-induced headache and extracerebral artery dilatation
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Calcitonin gene-related peptide does not cause the familial hemiplegic migraine phenotype
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This study shows that CGRP does not cause an aura or delayed headache in individuals with familial hemiplegic migraine
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Hansen, J.M.1
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Familial hemiplegic migraine type 1 shows no hypersensitivity to nitric oxide
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Familial hemiplegic migraine type 2 does not share hypersensitivity to nitric oxide with common types of migraine
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Hansen JM, Thomsen LL, Marconi R, et al. Familial hemiplegic migraine type 2 does not share hypersensitivity to nitric oxide with common types of migraine. Cephalalgia 2008; 28:367-375.
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55149086558
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The role of nitric oxide (NO) in migraine, tension-type headache and cluster headache
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Comprehensive review of the role of nitric oxide in primary headaches with references to interactions of the CGRP and nitric oxide pathways in headache pathophysiology
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Olesen J. The role of nitric oxide (NO) in migraine, tension-type headache and cluster headache. Pharmacol Ther 2008; 120:157-171. Comprehensive review of the role of nitric oxide in primary headaches with references to interactions of the CGRP and nitric oxide pathways in headache pathophysiology.
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Olesen, J.1
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19
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Comparison of CGRP and NO responses in the human peripheral microcirculation of migraine and control subjects
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This study shows that peripheral microcirculation in migraineurs is not hypersensitive to CGRP and nitric oxide, suggesting that central effects of CGRP may be more relevant in migraine
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Edvinsson ML, Edvinsson L Comparison of CGRP and NO responses in the human peripheral microcirculation of migraine and control subjects. Cephalalgia 2008; 28:563-566. This study shows that peripheral microcirculation in migraineurs is not hypersensitive to CGRP and nitric oxide, suggesting that central effects of CGRP may be more relevant in migraine.
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Phase II clinical trial of the oral CGRP antagonist telcagepant showing effectiveness and tolerability in comparison with a triptan
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Ho TW, Mannix LK, Fan X, et al. Randomized controlled trial of an oral CGRP receptor antagonist, MK-0974, in acute treatment of migraine. Neurology 2008; 70:1304-1312. Phase II clinical trial of the oral CGRP antagonist telcagepant showing effectiveness and tolerability in comparison with a triptan.
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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
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Phase III clinical trial of the oral CGRP antagonist telcagepant showing effectiveness and tolerability in comparison with a triptan
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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; 372:2115-2123. Phase III clinical trial of the oral CGRP antagonist telcagepant showing effectiveness and tolerability in comparison with a triptan.
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Ho, T.W.1
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Molecular mechanisms of sensitization of pain-transducing P2X3 receptors by the migraine mediators CGRP and NGF
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Review of P2X3 receptors in chronic pain and possible role in migraine
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Giniatullin R, Nistri A, Fabbretti E. Molecular mechanisms of sensitization of pain-transducing P2X3 receptors by the migraine mediators CGRP and NGF. Mol Neurobiol 2008; 37:83-90. Review of P2X3 receptors in chronic pain and possible role in migraine.
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23
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49649113201
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Mechanisms mediating the en-hanced gene transcription of P2X3 receptor by calcitonin gene-related peptide in trigeminal sensory neurons
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This study describes the effect of CGRP on two target genes relevant to migraine, which may help explain the mechanism underlying the delayed onset of headache following CGRP injection
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Simonetti M, Giniatullin R, Fabbretti E. Mechanisms mediating the en-hanced gene transcription of P2X3 receptor by calcitonin gene-related peptide in trigeminal sensory neurons. J Biol Chem 2008; 283:18743-18752. This study describes the effect of CGRP on two target genes relevant to migraine, which may help explain the mechanism underlying the delayed onset of headache following CGRP injection.
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Recober A, Russo AF. Olcegepant, a nonpeptide CGRP1 antagonist for migraine treatment. IDrugs 2007; 10:566-574.
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Recober A, Russo AF. Olcegepant, a nonpeptide CGRP1 antagonist for migraine treatment. IDrugs 2007; 10:566-574.
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CGRP-receptor antagonism in migraine treatment
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Comment discussing CGRP antagonists in migraine therapy
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Edvinsson L. CGRP-receptor antagonism in migraine treatment. Lancet 2008; 372:2089-2090. Comment discussing CGRP antagonists in migraine therapy.
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Salvatore CA, Hershey JC, Corcoran HA, et al. Pharmacological character-ization 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-carbox amide], a potent and orally active calcitonin gene-related peptide receptor antagonist for the treatment of migraine. J Pharmacol Exp Ther 2008; 324:416-421. This is a detailed description of the pharmacological characteristics of telcagepant.
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Salvatore CA, Hershey JC, Corcoran HA, et al. Pharmacological character-ization 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-carbox amide], a potent and orally active calcitonin gene-related peptide receptor antagonist for the treatment of migraine. J Pharmacol Exp Ther 2008; 324:416-421. This is a detailed description of the pharmacological characteristics of telcagepant.
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30
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0037134498
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Receptor activity-modifying protein 1 determines the species selectivity of nonpeptide CGRP receptor antagonists
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Mallee JJ, Salvatore CA, LeBourdelles B, et al. Receptor activity-modifying protein 1 determines the species selectivity of nonpeptide CGRP receptor antagonists. J Biol Chem 2002; 277:14294-14298.
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Mallee, J.J.1
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31
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Sensitization of calcitonin gene-related peptide receptors by receptor activity-modifying protein-1 in the trigeminal ganglion
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Zhang Z, Winborn CS, Marquez de Prado B, et al. Sensitization of calcitonin gene-related peptide receptors by receptor activity-modifying protein-1 in the trigeminal ganglion. J Neurosci 2007; 27:2693-2703.
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32
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61849148972
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Calcitonin gene-related peptide receptor inhibition reduces neuronal activity induced by prolonged increase in nitric oxide in the rat spinal trigeminal nucleus
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This study demonstrates how a CGRP receptor antagonist can prevent nitric oxide-induced activation of the spinal trigeminal nucleus and suggests possible shared mechanisms between nitric oxide and CGRP
-
Koulchitsky S, Fischer M, 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; 29:408-417. This study demonstrates how a CGRP receptor antagonist can prevent nitric oxide-induced activation of the spinal trigeminal nucleus and suggests possible shared mechanisms between nitric oxide and CGRP.
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Koulchitsky, S.1
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50249096199
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Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1 H-in dazol-5-yl)-1 -oxo-1 -(4-(piperidin-1 -yljpiperidin-1 -yl)propan-2-yl) piperidine-1 -carboxamide (BMS-694153): A potent antagonist of the human calcitonin gene-related peptide receptor for migraine with rapid and efficient intranasal exposure
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Degnan AP, Chaturvedula PV, Conway CM, ef al. Discovery of (R)-4-(8-fluoro-2-oxo-1,2-dihydroquinazolin-3(4H)-yl)-N-(3-(7-methyl-1 H-in dazol-5-yl)-1 -oxo-1 -(4-(piperidin-1 -yljpiperidin-1 -yl)propan-2-yl) piperidine-1 -carboxamide (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; 51:4858-4861.
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Degnan, A.P.1
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Calcitonin gene-related peptide (CGRP) receptor antagonists: Investigations of a pyridinone template
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Nguyen DN, Paone DV, Shaw AW, et al. Calcitonin gene-related peptide (CGRP) receptor antagonists: investigations of a pyridinone template. Bioorg Med Chem Lett 2008; 18:755-758.
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Nguyen, D.N.1
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39549094684
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Treatment of migraine attacks based on the interaction with the trigemino-cerebrovascular system
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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.
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Link, A.S.1
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Clinical and preclinical rationale for CGRP-receptor antagonists in the treatment of migraine
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Tepper SJ, Stillman MJ. Clinical and preclinical rationale for CGRP-receptor antagonists in the treatment of migraine. Headache 2008; 48:1259-1268.
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Tepper, S.J.1
Stillman, M.J.2
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51149090168
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Proinflammatory mediators and migraine pathogenesis: Moving towards CGRP as a target for a novel therapeutic class
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Farinelli I, Missori S, Martelletti P. Proinflammatory mediators and migraine pathogenesis: moving towards CGRP as a target for a novel therapeutic class. Expert Rev Neurother 2008; 8:1347-1354.
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Farinelli, I.1
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Martelletti, P.3
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34548834456
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Novel migraine therapy with calcitonin gene-regulated peptide receptor antagonists
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Comprehensive review of CGRP antagonists in migraine therapy
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Edvinsson L. Novel migraine therapy with calcitonin gene-regulated peptide receptor antagonists. Expert Opin Ther Targets 2007; 11:1179-1188. Comprehensive review of CGRP antagonists in migraine therapy.
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Expert Opin Ther Targets
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Edvinsson, L.1
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40
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56749157338
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CGRP blockers in migraine therapy: Where do they act?
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This review discusses the controversy regarding the site of action of CGRP receptor antagonists
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Edvinsson L. CGRP blockers in migraine therapy: where do they act? Br J Pharmacol 2008; 155:967-969. This review discusses the controversy regarding the site of action of CGRP receptor antagonists.
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Br J Pharmacol
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Edvinsson, L.1
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41
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40949083906
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Calcitonin receptor-like receptor (CLR), receptor activity-modifying protein 1 (RAMP1), and calcitonin gene-related peptide (CGRP) immunoreactivity in the rat trigeminovascular system: Differences between peripheral and central CGRP receptor distribution
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This study is the first detailed analysis of the distribution of CGRP receptor components throughout the rat trigeminovascular system
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Lennerz JK, Ruhle V, Ceppa EP, et al. Calcitonin receptor-like receptor (CLR), receptor activity-modifying protein 1 (RAMP1), and calcitonin gene-related peptide (CGRP) immunoreactivity in the rat trigeminovascular system: differences between peripheral and central CGRP receptor distribution. J Comp Neural 2008; 507:1277-1299. This study is the first detailed analysis of the distribution of CGRP receptor components throughout the rat trigeminovascular system.
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J Comp Neural
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, pp. 1277-1299
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Lennerz, J.K.1
Ruhle, V.2
Ceppa, E.P.3
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42
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34547787129
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Calcitonin receptor-like receptor and receptor activity modifying protein 1 in the rat dorsal horn: Localization in glutamatergic presynaptic terminals containing opioids and adrenergic alpha2C receptors
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This study shows the distribution of the CGRP receptor in the rat dorsal horn
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Marvizon JC, Perez OA, Song B, et al. Calcitonin receptor-like receptor and receptor activity modifying protein 1 in the rat dorsal horn: localization in glutamatergic presynaptic terminals containing opioids and adrenergic alpha2C receptors. Neuroscience 2007; 148:250-265. This study shows the distribution of the CGRP receptor in the rat dorsal horn.
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Neuroscience
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, pp. 250-265
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Marvizon, J.C.1
Perez, O.A.2
Song, B.3
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43
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23744494704
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Localization of calcitonin receptor-like receptor and receptor activity modifying protein 1 in enteric neurons, dorsal root ganglia, and the spinal cord of the rat
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Cottrell GS, Roosterman D, Marvizon JC, et al. Localization of calcitonin receptor-like receptor and receptor activity modifying protein 1 in enteric neurons, dorsal root ganglia, and the spinal cord of the rat. J Comp Neural 2005; 490:239-255.
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J Comp Neural
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Cottrell, G.S.1
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Marvizon, J.C.3
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44
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10644231738
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Calcitonin gene-related peptide regulates gene transcription in primary afferent neurons
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Anderson LE, Seybold VS. Calcitonin gene-related peptide regulates gene transcription in primary afferent neurons. J Neurochem 2004; 91:1417-1429.
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J Neurochem
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Anderson, L.E.1
Seybold, V.S.2
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45
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49649110601
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Serotonin type 1D receptors (5HTR) are differentially distributed in nerve fibres innervating craniofacial tissues
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This study addresses the distribution of serotonin type 1D receptors as a potential explanation for the specificity of triptans for headache versus other pain syndromes
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Harriott AM, Gold MS. Serotonin type 1D receptors (5HTR) are differentially distributed in nerve fibres innervating craniofacial tissues. Cephalalgia 2008; 28:933-944. This study addresses the distribution of serotonin type 1D receptors as a potential explanation for the specificity of triptans for headache versus other pain syndromes.
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Cephalalgia
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Harriott, A.M.1
Gold, M.S.2
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46
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56749176453
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CGRP function-blocking antibodies inhibit neurogenic vasodilatation without affecting heart rate or arterial blood pressure in the rat
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This study describes a complementary, but alternative strategy to CGRP receptor antagonists
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Zeller J, Poulsen KT, Sutton JE, et al. CGRP function-blocking antibodies inhibit neurogenic vasodilatation without affecting heart rate or arterial blood pressure in the rat. Br J Pharmacol 2008; 155:1093-1103. This study describes a complementary, but alternative strategy to CGRP receptor antagonists.
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Br J Pharmacol
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Zeller, J.1
Poulsen, K.T.2
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47
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33745107264
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Inhibition of stimulated meningeal blood flow by a calcitonin gene-related peptide binding mirror-image RNA oligonu-cleotide
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Denekas T, Troltzsch M, Vater A, et al. Inhibition of stimulated meningeal blood flow by a calcitonin gene-related peptide binding mirror-image RNA oligonu-cleotide. Br J Pharmacol 2006; 148:536-543.
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Denekas, T.1
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48
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33847671313
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Inhibitory effect of BIBN4096BS, CGRP(8-37), a CGRP antibody and an RNA-Spiegelmer on CGRP induced vasodilatation in the perfused and nonperfused rat middle cerebral artery
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This study looks at the site of action of CGRP receptor antagonists, CGRP antibody and RNA-Spiegelmer on the vasculature
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This review discusses the role of RAMPs as potential drug targets
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This study identifies important residues of the RAMPs that may affect the CGRP receptor function
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This editorial discusses the potential roles of RAMP1 in migraine
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