CGRP receptors in the control of pain and inflammation

Current Opinion in Pharmacology

Volumn 9, Issue 1, 2009, Pages 9-14

  Benemei, Silvia ^a   Nicoletti, Paola ^a   Capone, Jay G ^b   Geppetti, Pierangelo ^a,b  

^a UNIVERSITY OF FLORENCE   (Italy)

^b UNIVERSITY HOSPITAL OF FERRARA   (Italy)

Author keywords

[No Author keywords available]

Indexed keywords

ANTIMIGRAINE AGENT; BMS 694153; CALCITONIN GENE RELATED PEPTIDE RECEPTOR; CALCITONIN GENE RELATED PEPTIDE RECEPTOR ANTAGONIST; CAPSAICIN; ERGOT DERIVATIVE; MK 0974; OLCEGEPANT; OPIATE ANTAGONIST; TACHYKININ RECEPTOR ANTAGONIST; TELCAGEPANT; TRIPTAN DERIVATIVE; UNCLASSIFIED DRUG;

BRAIN CIRCULATION; CLINICAL TRIAL; DRUG BIOAVAILABILITY; DRUG EFFICACY; HUMAN; INFLAMMATION; MIGRAINE; NERVE ENDING; NOCICEPTION; NONHUMAN; PAIN; PRIORITY JOURNAL; PROTEIN EXPRESSION; PROTEIN SECRETION; REVIEW; SENSORY NERVE CELL; TRIGEMINUS GANGLION; VASODILATATION;

ANIMALS; AZEPINES; CALCITONIN GENE-RELATED PEPTIDE; DIPEPTIDES; HUMANS; IMIDAZOLES; MIGRAINE DISORDERS; NEUROGENIC INFLAMMATION; QUINAZOLINES; RECEPTORS, CALCITONIN GENE-RELATED PEPTIDE;

EID: 59349095975     PISSN: 14714892     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.coph.2008.12.007     Document Type: Review

References (56)

1. Markowitz S., Saito K., and Moskowitz M.A. Neurogenically mediated leakage of plasma protein occurs from blood vessels in dura mater but not brain. J Neurosci 7 (1987) 4129-4136
2. Geppetti P., and Holzer P. Neurogenic Inflammation (1996), CRC Press, Boca Raton
3. Caterina M.J., Schumacher M.A., Tominaga M., Rosen T.A., Levine J.D., and Julius D. The capsaicin receptor: a heat-activated ion channel in the pain pathway. Nature 389 (1997) 816-824
4. Szallasi A., and Blumberg P.M. Vanilloid (capsaicin) receptors and mechanisms. Pharmacol Rev 51 (1999) 159-212
5. Szolcsanyi J. A pharmacological approach to elucidation of the role of different nerve fibres and receptor endings in mediation of pain. J Physiol Paris 73 (1977) 251-259
6. Moskowitz M.A., and Buzzi M.G. Neuroeffector functions of sensory fibres: implications for headache mechanisms and drug actions. J Neurol 238 (1991) S18-22
7. Goldstein D.J., Wang O., Saper J.R., Stoltz R., Silberstein S.D., and Mathew N.T. Ineffectiveness of neurokinin-1 antagonist in acute migraine: a crossover study. Cephalalgia 17 (1997) 785-790
8. Diener H.C. RPR100893, a substance-P antagonist, is not effective in the treatment of migraine attacks. Cephalalgia 23 (2003) 183-185
9. Salvatore C.A., Hershey J.C., Corcoran H.A., Fay J.F., Johnston V.K., Moore E.L., Mosser S.D., Burgey C.S., Paone D.V., Shaw A.W., et al. 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 324 (2008) 416-421. The authors report the pharmacological characterization of MK-0974 (telcagepant), an orally available CGRP-receptor antagonist, which abates the capsaicin-evoked skin vasodilatation.
10. Salvatore C., Sinclair S., Kane S., Xiao A., Willson K., Xu Y., Hickey L., Palcza J., deLepeleire I., Vanmolkot F., et al. MK-0974 oral CGRP antagonist inhibits capsaicin-induced increase in dermal microvascular blood flow. Neurology 68 (2007) A307
11. Trang T., Quirion R., and Jhamandas K. The spinal basis of opioid tolerance and physical dependence: involvement of calcitonin gene-related peptide, substance P, and arachidonic acid-derived metabolites. Peptides 26 (2005) 1346-1355
12. King T., Ossipov M.H., Vanderah T.W., Porreca F., and Lai J. Is paradoxical pain induced by sustained opioid exposure an underlying mechanism of opioid antinociceptive tolerance?. Neurosignals 14 (2005) 194-205
13. Brain S.D., and Grant A.D. Vascular actions of calcitonin gene-related peptide and adrenomedullin. Physiol Rev 84 (2004) 903-934
14. Njuki F., Nicholl C.G., Howard A., Mak J.C., Barnes P.J., Girgis S.I., and Legon S. A new calcitonin-receptor-like sequence in rat pulmonary blood vessels. Clin Sci (Lond) 85 (1993) 385-388
15. Fluhmann B., Muff R., Hunziker W., Fischer J.A., and Born W. A human orphan calcitonin receptor-like structure. Biochem Biophys Res Commun 206 (1995) 341-347
16. McLatchie L.M., Fraser N.J., Main M.J., Wise A., Brown J., Thompson N., Solari R., Lee M.G., and Foord S.M. RAMPs regulate the transport and ligand specificity of the calcitonin-receptor-like receptor. Nature 393 (1998) 333-339
17. Buhlmann N., Leuthauser K., Muff R., Fischer J., and Born W. A receptor activity modifying protein (RAMP)2-dependent adrenomedullin receptor is a calcitonin gene-related peptide receptor when coexpressed with human RAMP1. Endocrinology 140 (1999) 2883-2890
18. Gray D.W., and Marshall I. Nitric oxide synthesis inhibitors attenuate calcitonin gene-related peptide endothelium-dependent vasorelaxation in rat aorta. Eur J Pharmacol 212 (1992) 37-42
19. Raddino R., Pela G., Manca C., Barbagallo M., D'Aloia A., Passeri M., and Visioli O. Mechanism of action of human calcitonin gene-related peptide in rabbit heart and in human mammary arteries. J Cardiovasc Pharmacol 29 (1997) 463-470
20. Lennerz J.K., Ruhle V., Ceppa E.P., Neuhuber W.L., Bunnett N.W., Grady E.F., and Messlinger K. 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 Neurol 507 (2008) 1277-1299. The authors show by immunohistochemistry that colocalization of the two components of the functional receptor (the calcitonin like receptor and RAMP1) is confined to the arterial smooth muscle and some inflammatory cells, but not to neurons of the trigeminal system.
21. Graham J., and Wolff H. Mechanism of migraine headache and action of ergotamine tartrate. Arch Neurol Psychiatry 39 (1938) 737-763
22. Lance J. Mechanism and Management of Headache (1969), Butterworths, New York
23. Goadsby P.J., Lipton R.B., and Ferrari M.D. Migraine - current understanding and treatment. N Eng J Med 346 (2002) 257-270
24. Goadsby P.J., Edvinsson L., and Ekman R. Release of vasoactive peptides in the extracerebral circulation of humans and the cat during activation of the trigeminovascular system. Ann Neurol 23 (1988) 193-196
25. Nicoletti P., Trevisani M., Manconi M., Gatti R., De Siena G., Zagli G., Benemei S., Capone J.A., Geppetti P., and Pini L.A. Ethanol causes neurogenic vasodilation by TRPV1 activation and CGRP release in the trigeminovascular system of the guinea pig. Cephalalgia 28 (2008) 9-17. The study demonstrates that ethanol, at doses commonly used in alcoholic beverages, dilates meningeal blood vessels via TRPV1 activation and CGRP release.
26. Goadsby P.J., Edvinsson L., and Ekman R. Vasoactive peptide release in the extracerebral circulation of humans during migraine headache. Ann Neurol 28 (1990) 183-187
27. Juhasz G., Zsombok T., Modos E.A., Olajos S., Jakab B., Nemeth J., Szolcsanyi J., Vitrai J., and Bagdy G. NO-induced migraine attack: strong increase in plasma calcitonin gene-related peptide (CGRP) concentration and negative correlation with platelet serotonin release. Pain 106 (2003) 461-470
28. Gallai V., Sarchielli P., Floridi A., Franceschini M., Codini M., Glioti G., Trequattrini A., and Palumbo R. Vasoactive peptide levels in the plasma of young migraine patients with and without aura assessed both interictally and ictally. Cephalalgia 15 (1995) 384-390
29. Fanciullacci M., Alessandri M., Figini M., Geppetti P., and Michelacci S. Increase in plasma calcitonin gene-related peptide from the extracerebral circulation during nitroglycerin-induced cluster headache attack. Pain 60 (1995) 119-123
30. Goadsby P.J., and Edvinsson L. The trigeminovascular system and migraine: studies characterizing cerebrovascular and neuropeptide changes seen in humans and cats. Ann Neurol 33 (1993) 48-56
31. Wei E.P., Moskowitz M.A., Boccalini P., and Kontos H.A. Calcitonin gene-related peptide mediates nitroglycerin and sodium nitroprusside-induced vasodilation in feline cerebral arterioles. Circ Res 70 (1992) 1313-1319
32. Lassen L.H., Haderslev P.A., Jacobsen V.B., Iversen H.K., Sperling B., and Olesen J. CGRP may play a causative role in migraine. Cephalalgia 22 (2002) 54-61
33. Hansen J.M., Thomsen L.L., Olesen J., and Ashina M. Calcitonin gene-related peptide does not cause the familial hemiplegic migraine phenotype. Neurology 71 (2008) 841-847
34. Olesen J., Diener H.C., Husstedt I.W., Goadsby P.J., Hall D., Meier U., Pollentier S., and Lesko L.M. Calcitonin gene-related peptide receptor antagonist BIBN 4096 BS for the acute treatment of migraine. N Engl J Med 350 (2004) 1104-1110
35. Ho T.W., Mannix L.K., Fan X., Assaid C., Furtek C., Jones C.J., Lines C.R., and Rapoport A.M. Randomized controlled trial of an oral CGRP antagonist, MK-0974, in acute treatment of migraine. Neurology (2007). The study reports the positive results of a phase II study with telcagepant (MK-0974) in the acute treatment of the migraine attack.
36. Chiba T., Yamaguchi A., Yamatani T., Nakamura A., Morishita T., Inui T., Fukase M., Noda T., and Fujita T. Calcitonin gene-related peptide receptor antagonist human CGRP-(8-37). Am J Physiol Endocrinol Metab 256 (1989) E331-335
37. Doods H., Hallermayer G., Wu D., Entzeroth M., Rudolf K., Engel W., and Eberlein W. Pharmacological profile of BIBN4096BS, the first selective small molecule CGRP antagonist. Br J Pharmacol 129 (2000) 420-423
38. Doods H., Arndt K., Rudolf K., and Just S. CGRP antagonists: unravelling the role of CGRP in migraine. Trends Pharmacol Sci 28 (2007) 580-587. The authors review preclinical and clinical data on the two CGRP-receptor antagonists which have been proven to ameliorate the migraine attack as well as the theoretical basis of the mechanism of action of these drugs.
39. Paone D.V., Shaw A.W., Nguyen D.N., Burgey C.S., Deng J.Z., Kane S.A., Koblan K.S., Salvatore C.A., Mosser S.D., Johnston V.K., et al. 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 50 (2007) 5564-5567
40. Geppetti P., Del Bianco E., Patacchini R., Santicioli P., Maggi C.A., and Tramontana M. Low pH-induced release of calcitonin gene-related peptide from capsaicin-sensitive sensory nerves: mechanism of action and biological response. Neuroscience 41 (1991) 295-301
41. Tominaga M., Caterina M.J., Malmberg A.B., Rosen T.A., Gilbert H., Skinner K., Raumann B.E., Basbaum A.I., and Julius D. The cloned capsaicin receptor integrates multiple pain-producing stimuli. Neuron 21 (1998) 531-543
42. Li Y.J., Xiao Z.S., Peng C.F., and Deng H.W. Calcitonin gene-related peptide-induced preconditioning protects against ischemia-reperfusion injury in isolated rat hearts. Eur J Pharmacol 311 (1996) 163-167
43. Lu R., Li Y.J., and Deng H.W. Evidence for calcitonin gene-related peptide-mediated ischemic preconditioning in the rat heart. Regul Pept 82 (1999) 53-57
44. Chai W., Mehrotra S., Jan Danser A.H., and Schoemaker R.G. The role of calcitonin gene-related peptide (CGRP) in ischemic preconditioning in isolated rat hearts. Eur J Pharmacol 531 (2006) 246-253
45. Kallner G., Gonon A., and Franco-Cereceda A. Calcitonin gene-related peptide in myocardial ischaemia and reperfusion in the pig. Cardiovasc Res 38 (1998) 493-499
46. Wu D.M., van Zwieten P.A., and Doods H.N. Effects of calcitonin gene-related peptide and BIBN4096BS on myocardial ischemia in anesthetized rats. Acta Pharmacol Sin 22 (2001) 588-594
47. Wang L., and Wang D.H. TRPV1 gene knockout impairs postischemic recovery in isolated perfused heart in mice. Circulation 112 (2005) 3617-3623
48. Zhong B., and Wang D.H. TRPV1 gene knockout impairs preconditioning protection against myocardial injury in isolated perfused hearts in mice. Am J Physiol Heart Circ Physiol 293 (2007) H1791-1798
49. Petersen K.A., Birk S., Doods H., Edvinsson L., and Olesen J. Inhibitory effect of BIBN4096BS on cephalic vasodilatation induced by CGRP or transcranial electrical stimulation in the rat. Br J Pharmacol 143 (2004) 697-704
50. Petersen K., Birk S., Lassen L., Kruuse C., Jonassen O., Lesko L., and Olesen J. The CGRP-antagonist, BIBN4096BS does not affect cerebral or systemic haemodynamics in healthy volunteers. Cephalalgia 25 (2005) 139-147
51. Lassen L.H., Jacobsen V.B., Haderslev P.A., Sperling B., Iversen H.K., Olesen J., and Tfelt-Hansen P. Involvement of calcitonin gene-related peptide in migraine: regional cerebral blood flow and blood flow velocity in migraine patients. J Headache Pain 9 (2008) 151-157
52. Zeller J., Poulsen K.T., Sutton J.E., Abdiche Y.N., Collier S., Chopra R., Garcia C.A., Pons J., Rosenthal A., and Shelton D.L. CGRP function-blocking antibodies inhibit neurogenic vasodilatation without affecting heart rate or arterial blood pressure in the rat. Br J Pharmacol 155 (2008) 1093-1103
53. Edvinsson L., Nilsson E., and Jansen-Olesen I. Inhibitory effect of BIBN4096BS, CGRP(8-37), a CGRP antibody and an RNA-Spiegelmer on CGRP induced vasodilatation in the perfused and non-perfused rat middle cerebral artery. Br J Pharmacol 150 (2007) 633-640
54. Degnan A.P., Chaturvedula P.V., Conway C.M., Cook D.A., Davis C.D., Denton R., Han X., Macci R., Mathias N.R., Moench P., et al. 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-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 51 (2008) 4858-4861
55. Goadsby P.J., and Edvinsson L. Neuropeptide changes in a case of chronic paroxysmal hemicrania - evidence for trigemino-parasympathetic activation. Cephalalgia 16 (1996) 448-450
56. Ho T.W., Ferrari M.D., Dodick D.W., Galet V., Kost J., Fan X., Leibensperger H., Froman S., Assaid C., Lines C., Koppen H., and Winner P.K. 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 372 (2009) 2115-2123