Literature DB >> 25186006

[Pain-relieving effect of CGRP antagonism on inflammatory pain].

S Hirsch1, F Birklein.   

Abstract

The neuropeptide calcitonin gene-related peptide (CGRP) is known to play a major role in the pathogenesis of pain syndromes, in particular migraine pain; however, its implication in inflammatory processes is not well known. The CGRP receptor antagonist BIBN4096BS was shown to reduce migraine pain and trigeminal neuronal activity. An analgesic action of this compound can also be found in rats with induced acute inflammation by injection of complete Freund's adjuvant (CFA) in one hindpaw. In this model the compound reduced inflammatory pain and spinal neuronal activity. Behavioral experiments (Randall-Selitto test) revealed a reversal of the CFA-induced mechanical hyperalgesia in rats after systemic drug administration. In vivo electrophysiological studies performed in rats injected with CFA using recordings of wide dynamic range neurons in deep dorsal horn layers of the lumbar spinal cord, confirmed a reduction of neuronal activity after systemic drug administration. The same considerable amount of reduction occurred after topical administration onto the paw with resulting systemic plasma concentrations in the low nanomolar range. Spinal administration of BIBN4096BS did not modify the neuronal activity in the CFA model which suggests that peripheral blockade of CGRP receptors by BIBN4096BS significantly alleviates inflammatory pain.

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Year:  2014        PMID: 25186006     DOI: 10.1007/s00482-014-1460-0

Source DB:  PubMed          Journal:  Schmerz        ISSN: 0932-433X            Impact factor:   1.107


  29 in total

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Authors:  H Doods
Journal:  Curr Opin Investig Drugs       Date:  2001-09

3.  Pharmacological profile of BIBN4096BS, the first selective small molecule CGRP antagonist.

Authors:  H Doods; G Hallermayer; D Wu; M Entzeroth; K Rudolf; W Engel; W Eberlein
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4.  Sustained pain freedom and no adverse events as an endpoint in clinical trials of acute migraine treatments: application to patient-level data from a trial of the CGRP receptor antagonist, telcagepant, and zolmitriptan.

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Journal:  Cephalalgia       Date:  2010-10-11       Impact factor: 6.292

5.  Spinal CGRP1 receptors contribute to supraspinally organized pain behavior and pain-related sensitization of amygdala neurons.

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Journal:  Pain       Date:  2007-03-01       Impact factor: 6.961

6.  Calcitonin gene-related peptide receptor inhibition reduces neuronal activity induced by prolonged increase in nitric oxide in the rat spinal trigeminal nucleus.

Authors:  S Koulchitsky; M J M Fischer; K Messlinger
Journal:  Cephalalgia       Date:  2008-11-25       Impact factor: 6.292

7.  Population pharmacokinetic modelling of BIBN 4096 BS, the first compound of the new class of calcitonin gene-related peptide receptor antagonists.

Authors:  Iñaki F Trocóniz; Jan-Markus Wolters; Hans Guenter Schaefer; Willy Roth
Journal:  Eur J Pharm Sci       Date:  2004-07       Impact factor: 4.384

8.  The CGRP receptor antagonist BIBN4096BS peripherally alleviates inflammatory pain in rats.

Authors:  Silke Hirsch; Laura Corradini; Stefan Just; Kirsten Arndt; Henri Doods
Journal:  Pain       Date:  2013-01-11       Impact factor: 6.961

Review 9.  Development and potential of non-peptide antagonists for calcitonin-gene-related peptide (CGRP) receptors: evidence for CGRP receptor heterogeneity.

Authors:  D Wu; H Doods; K Arndt; M Schindler
Journal:  Biochem Soc Trans       Date:  2002-08       Impact factor: 5.407

10.  Acute migraine therapy: new drugs and new approaches.

Authors:  Teshamae S Monteith; Peter J Goadsby
Journal:  Curr Treat Options Neurol       Date:  2011-02       Impact factor: 3.598

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2.  Bioinformatic Analysis of Potential Biomarkers for Spinal Cord-injured Patients with Intractable Neuropathic Pain.

Authors:  Yimin Wang; Fang Ye; Chanyan Huang; Faling Xue; Yingyuan Li; Shaowei Gao; Zeting Qiu; Si Li; Qinchang Chen; Huaqiang Zhou; Yiyan Song; Wenqi Huang; Wulin Tan; Zhongxing Wang
Journal:  Clin J Pain       Date:  2018-09       Impact factor: 3.442

  2 in total

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