5-HT7 receptor-mediated dilatation in the middle meningeal artery of anesthetized rats

Terrón, José A.; Martínez‐Garcia, Esther

doi:10.1016/j.ejphar.2007.01.019

Cited by 33 publications

(29 citation statements)

References 18 publications

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“…Among the various cranial vessels implicated in migraine headache, the middle meningeal artery has been considered as one of the most important for several reasons: It is the largest artery supplying the dura mater, its stimulation leads to activation of second-order trigeminal nociceptive pathways in the brain stem of mammals, and its stimulation is pain producing in humans. It is in this artery that Terron and Martinez-Garcia showed that 5-CT-induced hypotensive responses in anesthetized rats were strongly inhibited by specific blockade of the 5-HT7 receptor with SB-269970 [78]. This provides additional support to the notion that 5-HT promotes cranial dilatation and migraine via activation of 5-HT7 receptors.…”

Section: Migrainesupporting

confidence: 54%

“…However, the meningeal dilator responses produced by 5-CT were almost identical in vehicle-and 5,7-DHT-pretreated animals, suggesting that a reduction of 5-HT levels in the brain does not promote 5-HT7 receptor sensitization in the middle meningeal artery [79]. In support of a major role for 5-HT7 receptors in 5-CT-induced dilatation, SB-269970 strongly inhibited the hypotensive and meningeal dilator responses produced by this agonist in both vehicle-and 5,7-DHT-pretreated rats, which closely resembled the effect of the antagonist seen in intact anesthetized rats [78].…”

Section: Migrainementioning

confidence: 61%

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Role of the 5-HT7 Receptor in the Central Nervous System: from Current Status to Future Perspectives

et al. 2011

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Pharmacological and genetic tools targeting the 5-hydroxytryptamine (5-HT)7 receptor in preclinical animal models have implicated this receptor in diverse (patho)physiological processes of the central nervous system (CNS). Some data obtained with 5-HT7 receptor knockout mice, selective antagonists, and, to a lesser extent, agonists, however, are quite contradictory. In this review, we not only discuss in detail the role of the 5-HT7 receptor in the CNS but also propose some hypothetical models, which could explain the observed inconsistencies. These models are based on two novel concepts within the field of G protein-coupled receptors (GPCR), namely biphasic signaling and G protein-independent signaling, which both have been shown to be mediated by GPCR dimerization. This led us to suggest that the 5-HT7 receptor could reside in different dimeric contexts and initiate different signaling pathways, depending on the neuronal circuitry and/or brain region. In conclusion, we highlight GPCR dimerization and G protein-independent signaling as two promising future directions in 5-HT7 receptor research, which ultimately might lead to the development of more efficient dimer- and/or pathway-specific therapeutics.

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Section: Migrainesupporting

confidence: 54%

Section: Migrainementioning

confidence: 61%

Role of the 5-HT7 Receptor in the Central Nervous System: from Current Status to Future Perspectives

et al. 2011

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“…Studies using 5-HT 7 receptor-selective antagonists suggested that the 5-HT 7 receptor modulates neuronal function also in a number of brain areas along the pathway of the trigeminovascular system, dorsal raphe nucleus, periaqueductal grey, and thalamus [76]. Other lines of evidence indicated that 5-HT 7 receptors are involved in the dilatation of meningeal arteries, neuroinflammatory processes, central sensitization, and the activation of pain pathways [77,78]. A recent study showed that the selective 5-HT 7 receptor antagonist SB269970 partly inhibited the release of calcitonin gene-related peptide after electrical stimulation of the trigeminal ganglion in animals [76].…”

Section: Discussionmentioning

confidence: 99%

Serotonergic Agents in the Management of Cluster Headache

Lambru

Matharu

2011

Curr Pain Headache Rep

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Cluster headache is a highly disabling primary headache disorder, characterized by unilateral headache attacks occurring in association with cranial autonomic symptoms. Serotonergic agents, such as the ergot alkaloids, have traditionally been used for the acute and preventive treatment of cluster headache and other primary headaches. Although it initially was thought that their efficacy was due solely to the vasoconstriction of extracranial cerebral vessels, new mechanisms of action of these drugs have been ascertained as a consequence of advances in elucidation of the pathogenesis of primary headaches and the development of triptans. This article reviews the current knowledge about serotonergic agonists and antagonists used in the management of cluster headache, focusing on their mechanisms of action and on the possible role of serotonin system dysfunction in this complex disorder.

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“…Before the availability of selective 5-HT 7 receptor antagonists, pharmacological profiling was used to implicate the 5-HT 7 receptor as the most likely mediator of 5-HT induced vasodilation in preparations of the basilar and middle cerebral arteries (Terrón & Falcón-Neri, 1999). Later involvement of the 5-HT 7 receptor was confirmed since such vasodilation could be blocked in vivo by SB-269970 (Terrón & Martínez-García, 2007). This has been shown to also be true after 5-HT depletion, suggesting that the 5-HT 7 receptors involved are not sensitized by reduced availability of 5-HT (Martínez-García et al, 2009).…”

Section: 5-ht7 Receptor Function In Normal and Pathological Processesmentioning

confidence: 92%

Serotonin 5-HT7 receptor agents: Structure-activity relationships and potential therapeutic applications in central nervous system disorders

Leopoldo

Lacivita

Berardi

et al. 2011

Pharmacology & Therapeutics

164

145

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Since its discovery in the 1940s in serum, the mammalian intestinal mucosa, and in the central nervous system, serotonin (5-HT) has been shown to be involved in virtually all cognitive and behavioral human functions, and alterations in its neurochemistry have been implicated in the etiology of a plethora of neuropsychiatric disorders. The cloning of 5-HT receptor subtypes has been of importance in enabling them to be classified as specific protein molecules encoded by specific genes. The 5-HT7 receptor is the most recently classified member of the serotonin receptor family. Since its identification, it has been the subject of intense research efforts driven by its presence in functionally relevant regions of the brain. The availability of some selective antagonists and agonists, in combination with genetically modified mice lacking the 5-HT7 receptor, has allowed for a better understanding of the pathophysiological role of this receptor. This paper reviews data on localization and pharmacological properties of the 5-HT7 receptor, and summarizes the results of structure-activity relationship studies aimed at the discovery of selective 5-HT7 receptor ligands. Additionally, an overview of the potential therapeutic applications of 5-HT7 receptor agonists and antagonists in central nervous system disorders is presented.

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5-HT7 receptor-mediated dilatation in the middle meningeal artery of anesthetized rats

Abstract: Topical administration of 5-carboxamidotryptamine (5-CT; 0.01-1000 μM) to the exposed dura mater encephali of anesthetized rats produced decreases in blood pressure and dilatation in the middle meningeal artery. Pretreatment with the 5-HT 1B/1D receptor antagonist,

Cited by 33 publications

References 18 publications

Role of the 5-HT7 Receptor in the Central Nervous System: from Current Status to Future Perspectives

Role of the 5-HT7 Receptor in the Central Nervous System: from Current Status to Future Perspectives

Serotonergic Agents in the Management of Cluster Headache

Serotonin 5-HT7 receptor agents: Structure-activity relationships and potential therapeutic applications in central nervous system disorders

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