In-depth characterization of CGRP receptors in human intracranial arteries

Jansen‐Olesen, Inger; Jørgensen, Louise von Gersdorff; Engel, Uwe; Edvinsson, Lars

doi:10.1016/j.ejphar.2003.09.021

Cited by 61 publications

(61 citation statements)

References 33 publications

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“…On the basis of pharmacological criteria, it is known that CGRP may act mainly on CGRP 1 and CGRP 2 receptors (Arulmani et al 2004), with h-αCGRP 8-37 being a 10-fold more potent antagonist at CGRP 1 receptors than at CGRP 2 receptors (Quirion et al 1992 Gupta et al 2006a;Jansen-Olesen et al 2003;Oliver et al 2002). The results from our laboratory also advocate the presence of CGRP 1 receptors in human meningeal (Gupta et al 2006a) and coronary (Gupta et al 2006b) arteries, while in human distal coronary artery, there seems to be an additional population of CGRP receptors not complying with the current classification of CGRP 1 or CGRP 2 receptors (Gupta et al 2006b).…”

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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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%

Current and prospective pharmacological targets in relation to antimigraine action

Mehrotra

Gupta

Chan

et al. 2008

Naunyn-Schmied Arch Pharmacol

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“…The molecular components of CGRP 1 receptors that have been demonstrated in the human cerebral and meningeal artery include CLR and the RAMPs 1, 2 and 3 (Oliver et al, 2002;Jansen-Olesen et al, 2003); nevertheless, there is no report about RCP, which is required for the formation of a high-affinity G-protein-coupled receptor, thereby ensuring the signal transduction of CLR (Evans et al, 2000).…”

Section: Introductionmentioning

confidence: 97%

“…While CGRP 1 receptors are widely distributed, CGRP 2 receptors have only been described in rat vas deferens, and are more sensitive to the linear agonists 7 ]h-αCGRP ([Cys(Et) 2,7 ]h-αCGRP) and 7 ]h-αCGRP ([Cys(Acm) 2,7 ]h-αCGRP) (Dumont et al, 1997). Using these pharmacological tools, CGRP receptors have been characterised in human cerebral (Sams et al, 2000) and middle meningeal (Jansen- Olesen et al, 2003) arteries.…”

Section: Introductionmentioning

confidence: 99%

Characterisation of CGRP receptors in the human isolated middle meningeal artery

et al. 2006

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“…The CGRP receptor antagonist, BIBN4096BS appears to be a viable antimigraine drug as studied in human arteries [Edvinsson et al, 2002;Jansen-Olesen et al, 2003] and animals [Wu et al, , 2002Jansen-Olesen et al, 2001]. In clinical trials BIBN4096BS did not constrict coronary arteries [Edvinsson et al, 2002;Hasbak et al, 2003;Gupta et al, 2006a], making its use potentially advantageous over the triptans.…”

Section: Treatment Of Migraine Headachesmentioning

confidence: 98%

Role of neuropeptides in migraine: where do they stand in the latest expert recommendations in migraine treatment?

Samsam

Coveñas

Ahangari

et al. 2007

Drug Development Research

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Many factors have been implicated in the pathogenesis of migraine headache, including activation of the trigeminovascular system, dysfunction of: cerebral blood vessels, circulating vasoactive substances, mitochondrial energy metabolism, brain oxygenation and metabolism, platelet disorder, alterations in serotonin levels, low levels of brain tissue magnesium, altered transport of ions across the cell membrane, and inheritance and dysfunction of the brainstem periaqueductal gray matter. The headache phase of migraine is associated with cerebral vasodilation and inflammation, presumably mediated by the release of vasoactive substances and neuropeptides including CGRP (calcitonin gene-related peptide). Increased serum CGRP levels have been detected during migraine and cluster headache. One strategy to treat migraine is to inhibit the release of neuropeptides or to block their receptors. This article briefly reviews some experimental and clinical investigations focused on neuropeptide involvement in migraine. Drug Dev Res 68: 294-314, 2007.

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In-depth characterization of CGRP receptors in human intracranial arteries

Cited by 61 publications

References 33 publications

Current and prospective pharmacological targets in relation to antimigraine action

Current and prospective pharmacological targets in relation to antimigraine action

Characterisation of CGRP receptors in the human isolated middle meningeal artery

Role of neuropeptides in migraine: where do they stand in the latest expert recommendations in migraine treatment?

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