BIBN4096BS Antagonizes Human α-calcitonin Gene Related Peptide–induced Headache and Extracerebral Artery Dilatation*

Petersen, KA; Lassen, LH; Birk, Steffen; Lesko, Lynna M.; Olesen, Jes

doi:10.1016/j.clpt.2004.10.001

Cited by 162 publications

(197 citation statements)

References 46 publications

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“…Furthermore, in migraine patients, (a) a strong correlation was found between plasma CGRP concentrations and migraine headache as the changes in plasma CGRP levels during migraine attacks significantly correlated with the headache intensity (Durham 2004;Iovino et al 2004;Petersen et al 2005b); (b) infusion of CGRP produced a migraine-like headache (Olesen et al 2004); and (c) baseline CGRP levels were increased in migraineurs (Fusayasu et al 2007). …”

Section: Cgrp Receptorsmentioning

confidence: 99%

“…In in vivo animal models of migraine, olcegepant attenuated the vasodilation induced by trigeminal stimulation and capsaicin-induced carotid arteriovenous anastomotic dilatation Edvinsson 2004;Kapoor et al 2003;Petersen et al 2005b). In addition, olcegepant has been shown to prevent CGRP-induced headache and extracerebral vasodilatation (Petersen et al 2005b) but does not significantly affect the induced cerebral hemodynamic changes (Fig. 4).…”

Section: Cgrp Receptorsmentioning

confidence: 99%

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Current and prospective pharmacological targets in relation to antimigraine action

Mehrotra

Gupta

Chan

et al. 2008

Naunyn-Schmied Arch Pharmacol

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Migraine is a recurrent incapacitating neurovascular disorder characterized by unilateral and throbbing headaches associated with photophobia, phonophobia, nausea, and vomiting. Current specific drugs used in the acute treatment of migraine interact with vascular receptors, a fact that has raised concerns about their cardiovascular safety. In the past, α-adrenoceptor agonists (ergotamine, dihydroergotamine, isometheptene) were used. The last two decades have witnessed the advent of 5-HT 1B/1D receptor agonists (sumatriptan and second-generation triptans), which have a well-established efficacy in the acute treatment of migraine. Moreover, current prophylactic treatments of migraine include 5-HT 2 receptor antagonists, Ca 2+ channel blockers, and β-adrenoceptor antagonists. Despite the progress in migraine research and in view of its complex etiology, this disease still remains underdiagnosed, and available therapies are underused. In this review, we have discussed pharmacological targets in migraine, with special emphasis on compounds acting on 5-HT (5-HT 1-7 ), adrenergic (α 1 , α 2, and β), calcitonin gene-related peptide (CGRP 1 and CGRP 2 ), adenosine (A 1 , A 2 , and A 3 ), glutamate (NMDA, AMPA, kainate, and metabotropic), dopamine, endothelin, and female hormone (estrogen and progesterone) receptors. In addition, we have considered some other targets, including gamma-aminobutyric acid, angiotensin, bradykinin, histamine, and ionotropic receptors, in relation to antimigraine therapy. Finally, the cardiovascular safety of current and prospective antimigraine therapies is touched upon.

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Section: Cgrp Receptorsmentioning

confidence: 99%

Section: Cgrp Receptorsmentioning

confidence: 99%

Current and prospective pharmacological targets in relation to antimigraine action

Mehrotra

Gupta

Chan

et al. 2008

Naunyn-Schmied Arch Pharmacol

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“…[7][8][9][10][11][12][13][14][15][16][17][18][19] All measurements were performed using the same gamma camera and identical acquisition and processing protocols.…”

Section: Cerebral Blood Flow Measurementsmentioning

confidence: 99%

Sources of Variability of Resting Cerebral Blood Flow in Healthy Subjects: A Study Using¹³³Xe SPECT Measurements

Henriksen

Kruuse

Olesen

et al. 2013

J Cereb Blood Flow Metab

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Measurements of cerebral blood flow (CBF) show large variability among healthy subjects. The aim of the present study was to investigate the relative effect of established factors influencing CBF on the variability of resting CBF. We retrospectively analyzed spontaneous variability in 430 CBF measurements acquired in 152 healthy, young subjects using 133 Xe single-photon emission computed tomography. Cerebral blood flow was correlated positively with both end-tidal expiratory P CO 2 (P ET CO 2 ) and female gender and inversely with hematocrit (Hct). Between-and within-subject CO 2 reactivity was not significantly different. Including P ET CO 2 , Hct and gender in the model reduced between-subject and within-subject variance by 14% and 13.5%, respectively. Withinsubject variability was mainly influenced by P ET CO 2 and between-subject variability mostly by Hct, whereas gender appeared to be of little added value when Hct was also accounted for. The present study confirms large between-subject variability in CBF measurements and that gender, Hct, and P ET CO 2 explain only a small part of this variability. This implies that a large fraction of CBF variability may be due to unknown factors such as differences in neuron density or metabolism that could be subject for further studies.

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“…The ability of CGRP to trigger a delayed severe in headache, including some of the nonheadache symptoms, strongly suggests that CGRP plays a causal role in migraine. In addition, CGRP infusion in non-migraineurs caused a mild headache that was prevented by a CGRP receptor antagonist [28]. The effectiveness of this antagonist was a harbinger of its potential as an anti-migraine drug.…”

Section: Migraine and Cgrpmentioning

confidence: 96%

CGRP receptor antagonists: A new frontier of anti-migraine medications

Prado

Russo

2006

Drug Discovery Today: Therapeutic Strategies

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Migraine is a chronic pain condition that affects 12% of the population. Currently, the most effective treatments are the triptans, but they are limited in their efficacy and have potentially deleterious cardiovascular complications. Based on basic science studies over the past decade, a new generation of anti-migraine drugs is now being developed. At the forefront of these studies is a new calcitonin gene-related peptide (CGRP) receptor antagonist that is as effective as triptans in the acute treatment of migraines, without the cardiovascular effects. This review will address the likely mechanisms and therapeutic potential of CGRP receptor antagonists.

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BIBN4096BS Antagonizes Human α-calcitonin Gene Related Peptide–induced Headache and Extracerebral Artery Dilatation*

Abstract: These results show that BIBN4096BS effectively prevents CGRP-induced headache and extracerebral vasodilatation but does not significantly affect the induced cerebral hemodynamic changes.

Cited by 162 publications

References 46 publications

Current and prospective pharmacological targets in relation to antimigraine action

Current and prospective pharmacological targets in relation to antimigraine action

Sources of Variability of Resting Cerebral Blood Flow in Healthy Subjects: A Study Using¹³³Xe SPECT Measurements

CGRP receptor antagonists: A new frontier of anti-migraine medications

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BIBN4096BS Antagonizes Human α-calcitonin Gene Related Peptide–induced Headache and Extracerebral Artery Dilatation*

Abstract: These results show that BIBN4096BS effectively prevents CGRP-induced headache and extracerebral vasodilatation but does not significantly affect the induced cerebral hemodynamic changes.

Cited by 162 publications

References 46 publications

Current and prospective pharmacological targets in relation to antimigraine action

Current and prospective pharmacological targets in relation to antimigraine action

Sources of Variability of Resting Cerebral Blood Flow in Healthy Subjects: A Study Using133Xe SPECT Measurements

CGRP receptor antagonists: A new frontier of anti-migraine medications

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Product

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Sources of Variability of Resting Cerebral Blood Flow in Healthy Subjects: A Study Using¹³³Xe SPECT Measurements