CGRP receptors in the control of pain and inflammation

被引:149
作者
Benemei, Silvia [1 ]
Nicoletti, Paola [1 ]
Capone, Jay G. [2 ]
Geppetti, Pierangelo [1 ,2 ]
机构
[1] Univ Florence, Ctr Study Headache, Florence, Italy
[2] S Anna Univ Hosp, Headache Ctr, Ferrara, Italy
关键词
GENE-RELATED-PEPTIDE; ISOLATED RAT HEARTS; TRIGEMINOVASCULAR SYSTEM; EXTRACEREBRAL CIRCULATION; NEUROPEPTIDE CHANGES; MYOCARDIAL-ISCHEMIA; CAPSAICIN RECEPTOR; MIGRAINE HEADACHE; BLOOD-VESSELS; SUBSTANCE-P;
D O I
10.1016/j.coph.2008.12.007
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
Calcitonin gene related peptide (CGRP) has been proposed to contribute to pain transmission and inflammation and for these reasons to the mechanism of migraine. CGRP is, in fact, expressed in and released from a subset of polymodal primary sensory neurons of the trigeminal ganglion. Release of CGRP in the dorsal spinal cord has been associated to nociceptive transmission, and release from perivascular nerve endings causes neurogenic vasodilatation. CGRP levels increase in the cranial circulation during migraine attacks, and GRP injection in migraineurs results in migraine-like attacks. Most importantly, two chemically unrelated CGRP-receptor antagonists, the parenteral agent, olcegepant, and the orally available telcagepant demonstrated efficacy in the treatment of migraine attacks, thus supporting CGRP as an important mediator in migraine.
引用
收藏
页码:9 / 14
页数:6
相关论文
共 56 条
[1]   Vascular actions of calcitonin gene-related peptide and adrenomedullin [J].
Brain, SD ;
Grant, AD .
PHYSIOLOGICAL REVIEWS, 2004, 84 (03) :903-934
[2]   A receptor activity modifying protein (RAMP)2-dependent adrenomedullin receptor is a calcitonin gene-related peptide receptor when coexpressed with human RAMP1 [J].
Bühlmann, N ;
Leuthäuser, K ;
Muff, R ;
Fischer, JA ;
Born, W .
ENDOCRINOLOGY, 1999, 140 (06) :2883-2890
[3]   The capsaicin receptor: a heat-activated ion channel in the pain pathway [J].
Caterina, MJ ;
Schumacher, MA ;
Tominaga, M ;
Rosen, TA ;
Levine, JD ;
Julius, D .
NATURE, 1997, 389 (6653) :816-824
[4]   The role of calcitonin gene-related peptide (CGRP) in ischemic preconditioning in isolated rat hearts [J].
Chai, WX ;
Mehrotra, S ;
Danser, AHJ ;
Schoemaker, RG .
EUROPEAN JOURNAL OF PHARMACOLOGY, 2006, 531 (1-3) :246-253
[5]   CALCITONIN GENE-RELATED PEPTIDE RECEPTOR ANTAGONIST HUMAN CGRP-(8-37) [J].
CHIBA, T ;
YAMAGUCHI, A ;
YAMATANI, T ;
NAKAMURA, A ;
MORISHITA, T ;
INUI, T ;
FUKASE, M ;
NODA, T ;
FUJITA, T .
AMERICAN JOURNAL OF PHYSIOLOGY, 1989, 256 (02) :E331-E335
[6]   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].
Degnan, Andrew P. ;
Chaturvedula, Prasad V. ;
Conway, Charles M. ;
Cook, Deborah A. ;
Davis, Carl D. ;
Denton, Rex ;
Han, Xiaojun ;
Macci, Robert ;
Mathias, Neil R. ;
Moench, Paul ;
Pin, Sokhoin S. ;
Ren, Shelly X. ;
Schartman, Richard ;
Signor, Laura J. ;
Thalody, George ;
Widmann, Kimberly A. ;
Xu, Cen ;
Macor, John E. ;
Dubowchik, Gene M. .
JOURNAL OF MEDICINAL CHEMISTRY, 2008, 51 (16) :4858-4861
[7]   RPR100893, a substance-P antagonist, is not effective in the treatment of migraine attacks [J].
Diener, HC .
CEPHALALGIA, 2003, 23 (03) :183-185
[8]   Pharmacological profile of BIBN4096BS, the first selective small molecule CGRP antagonist [J].
Doods, H ;
Hallermayer, G ;
Wu, DM ;
Entzeroth, M ;
Rudolf, K ;
Engel, W ;
Eberlein, W .
BRITISH JOURNAL OF PHARMACOLOGY, 2000, 129 (03) :420-423
[9]   CGRP antagonists: unravelling the role of CGRP in migraine [J].
Doods, Henri ;
Arndt, Kirsten ;
Rudolf, Klaus ;
Just, Stefan .
TRENDS IN PHARMACOLOGICAL SCIENCES, 2007, 28 (11) :580-587
[10]   Inhibitory effect of BIBN4096BS, CGRP8-37, a CGRP antibody and an RNA-Spiegelmer on CGRP induced vasodilatation in the perfused and non-perfused rat middle cerebral artery [J].
Edvinsson, L. ;
Nilsson, E. ;
Jansen-Olesen, I. .
BRITISH JOURNAL OF PHARMACOLOGY, 2007, 150 (05) :633-640