Possible site of action of CGRP antagonists in migraine

Cephalalgia

Volumn 31, Issue 6, 2011, Pages 748-750

  Tfelt Hansen, Peer ^a,b   Olesen, Jes ^a  

^a UNIVERSITY OF COPENHAGEN   (Denmark)

^b GLOSTRUP UNIVERSITY HOSPITAL   (Denmark)

Author keywords

CGRP receptor blockers; migraine; MK 3207; olcegepant; telcagepant

Indexed keywords

CALCITONIN GENE RELATED PEPTIDE RECEPTOR ANTAGONIST; CAPSAICIN; OLCEGEPANT; TELCAGEPANT;

ANTIMIGRAINE ACTIVITY; BLOOD BRAIN BARRIER; DRUG ACTIVITY; DRUG DOSE COMPARISON; DRUG EFFECT; DRUG INHIBITION; HAPLORHINI; HUMAN; IN VITRO STUDY; IN VIVO STUDY; MIGRAINE; NONHUMAN; REVIEW; SKIN BLOOD FLOW;

ANIMALS; AZEPINES; BICYCLO COMPOUNDS, HETEROCYCLIC; BLOOD-BRAIN BARRIER; CEREBROVASCULAR CIRCULATION; DIPEPTIDES; HUMANS; IMIDAZOLES; MIGRAINE DISORDERS; QUINAZOLINES; RECEPTORS, CALCITONIN GENE-RELATED PEPTIDE; SPIRO COMPOUNDS;

EID: 79954606149     PISSN: 03331024     EISSN: 14682982     Source Type: Journal    
DOI: 10.1177/0333102411398403     Document Type: Review

References (20)

1. Sixt ML, Messlinger K, Fischer MJM. Calcitonin gene-related peptide receptor antagonist olcegepant acts in the spinal trigeminal nucleus. Brain. 2009 ; 132: 3134-3141
2. Goadsby PJ, Charbill AR, Andreou AP, et al. Neurobiology of migraine. Neuroscience. 2009 ; 161: 327-341
3. Olesen J, Burstein R, Ashina M, et al. Origin of pain (nociception) in migraine. Lancet Neurol. 2009 ; 8: 679-690
4. Edvinsson L, Nilsson E, Jansen-Olesen I. Inhibitory effect of BIBN4096BS, CGRP8-37, a CGRP antibody and an RNA-Spiegelmer on CGRP induced vasodilatation in the perfused and non-perfused rat cerebral artery. Br J Pharmacol. 2007 ; 150: 633-640 (Pubitemid 46355559)
5. Edvinsson L. CGRP blockers in migraine therapy: where do they act?. Br J Pharmacol. 2008 ; 155: 967-969
6. Edvinsson L, Alm R, Shaw D, et al. Effect of the CGRP receptor antagonist BIBN4098BS in human cerebral, coronary and omental arteries and in SK.N.MC cells. Eur J Pharmacol. 2002 ; 434: 49-53 (Pubitemid 34033745)
7. Doods H, Hallermayer G, Wu D, et al. Pharmacological profile of BIBN4096BS, the first selective small molecule CGRP antagonist. Br J Pharmacol. 2000 ; 129: 420-433
8. Salvatore CA, Hershey JC, Corcoran HA, et al. Pharmacological characterization of MK-0974 [N-[(3R,6S)-6-(2,3-difluorophenyl)-2-oxo-1-(2,2,2- trifluoroethyl)asepan-3-yl]-4-(2-oxo-2,3-dihydro-1H-imidazol[4,5}pyridine-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: 416-421 (Pubitemid 351185864)
9. Moreno MJ, Abounader R, Hebert E, et al. Efficacy of the non-peptide receptor antagonist BIB4096BS in blocking CGRP-induced vasodilation in human and bovine cerebral arteries: potential implications in acute migraine management. Neuropharmacology. 2002 ; 42: 568-573
10. Verheggen R, Bumann K, Kaumann AJ. BIBN4096BS is a potent competitive antagonist of the relaxant effects of alpha-CGRP on human temporal artery: comparison with CGRP (8-37). Br J Pharmacol. 2002 ; 136: 120-126 (Pubitemid 34499324)
11. Verheggen R, Wotjas K, Webel H, et al. BIBN4096BS and CGRP(8-37) antagonize the relaxant effects of alpha-CGRP more than those of beta-CGRP in human extracranial arteries. Naunyn Schmiedeberg's Arch Pharmacol. 2005 ; 371: 383-392 (Pubitemid 41187510)
12. Olesen J, Diener HC, Husstedt IW, et al. Calcitonin gene-related peptide receptor antagonist BIBN 4096 BS for the acute treatment of migraine. N Eng J Med. 2004 ; 350: 1104-1110 (Pubitemid 38298990)
13. Storer RJ, Akerman S, Goadsby PJ. Calcitonin gene-related (CGRP) modulates nociceptive trigeminovascular transmission in the cat. Br J Pharmacol. 2004 ; 142: 1171-1181 (Pubitemid 39093014)
14. 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 (Pubitemid 351550355)
15. 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 randomized, placebo-controlled, parallel-treatment trial. Lancet. 2008 ; 372: 2115-2123
16. Connor KM, Shapiro RE, Diener H-C, et al. Randomized, controlled trial of telcagepant for the acute treatment of migraine. Neurology. 2009 ; 73: 970-977
17. 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 (Pubitemid 41552545)
18. Edvinsson L, Ho TW. CGRP receptor antagonism and migraine. Neurotherapeutics. 2010 ; 7: 164-175
19. Salvatore CA, Moore EL, Calamari A, et al. Phramacological properties of MK-3207, a potent and orally active calcitonin gene-related peptide receptor antagonist. J Pharmacol Exp Ther. 2010 ; 333: 152-160
20. Sinclair SR, Kane SA, Van der Schueren BJ, et al. 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