Migraine: Current concepts and emerging therapies

Arulmozhi, D. K.; Addepalli, Veeranjaneyulu; Bodhankar, S.L.

doi:10.1016/j.vph.2005.07.001

Cited by 73 publications

(51 citation statements)

References 87 publications

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“…[17] Drugs targeting both 5-HT 2B and 5-HT 2C receptors can be used to treat migraines. [42,55] Drugs modulating 5-HT 2C activity are applicable in the treatment of obesity, erectile dysfunction and anxiety disorders. [17,32] …”

Section: Receptorsmentioning

confidence: 99%

Structure–Activity Relationships of Phenylalkylamines as Agonist Ligands for 5‐HT_2A Receptors

2008

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Agonist activation of central 5-HT(2A) receptors results in diverse effects, such as hallucinations and changes of consciousness. Recent findings indicate that activation of the 5-HT(2A) receptor also leads to interesting physiological responses, possibly holding therapeutic value. Selective agonists are needed to study the full therapeutic potential of this receptor. 5-HT(2A) ligands with agonist profiles are primarily derived from phenylalkylamines, indolealkylamines, and certain piperazines. Of these, phenylalkylamines, most notably substituted phenylisopropylamines, are considered the most selective agonists for 5-HT(2) receptors. This review summarizes the structure-activity relationships (SAR) of phenylalkylamines as agonist ligands for 5-HT(2A) receptors. Selectivity is a central theme, as is selectivity for the 5-HT(2A) receptor and for its specific signaling pathways. SAR data from receptor affinity studies, functional assays, behavioral drug discrimination as well as human studies are discussed.

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Section: Receptorsmentioning

confidence: 99%

Structure–Activity Relationships of Phenylalkylamines as Agonist Ligands for 5‐HT_2A Receptors

2008

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“…It has been demonstrated that obesity is a pro-inflammatory state; adipocytes can secrete a variety of cytokines, including IL-6 and tumor necrosis factor, which are cytokines that promote inflammation [2,3]. On the other hand, migraine is associated with neurovascular inflammation involving the same cytokines [4]. …”

Section: Introductionmentioning

confidence: 99%

Association between Body Mass Index and Migraine

et al. 2010

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Objective: To explore the prevalence of overweight and obesity in patients with migraine. Background: Previous studies support the concept that obesity is an exacerbating factor for migraine. Also, some studies have found an increased frequency of obesity and overweight in migraine patients compared to the normal population. Methods: We studied 1,371 patients with migraine and 612 controls. The migraine population was matched by gender with a healthy control group. Results: Mean age of patients with migraine was 38.0 ± 13.3 years and in the controls it was 34.8 ± 12.1 years. The percentage of females in both groups was similar (migraine 81.6% vs. control 83.3%, p = 0.40). The distribution of body mass index (BMI) in migraine patients and controls was as follows: underweight patients (BMI <18.5) 3.1% migraine versus controls 1.5%; normal (BMI 18.5–24.9) 44.8% migraine versus controls 47.1%; overweight (BMI 25–29.9) 38.3% migraine versus controls 33.7%; obese (BMI 30–34.5) 10.3% migraine versus controls 13.6%; morbidly obese (BMI 35) 3.4% migraine versus controls 4.2%. Overweight and obesity in migraine patients versus controls were statistically significant. No association was found between the disability and severity of migraine and BMI. Conclusions: This study did not find associations between severity or disability of migraine and BMI.

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“…While cortical spreading depression (CSD) has not yet been demonstrated in the human cerebral cortex, characteristics of CSD in humans have certainly been shown [Hadjikhani et al, 2001]. This inflammation reaction may also lower the nociceptive threshold required to stimulate meningial sensory fibers [Moskowitz, 1990] and act on vascular tissues to cause vasodilatation, plasma protein extravasation in the surrounding area, endothelial changes, platelet aggregation and subsequent release of more serotonin, white cell adhesion, and further inflammation [Arulmozhi et al, 2005;Dimitriadou et al, 1991Dimitriadou et al, , 1992. These stimulations are transmitted to brain rostral structures involved in pain processing such as several thalamic nuclei, hypothalamic nuclei, and the caudal periaqueductal gray region [May, 2006].…”

Section: Introductionmentioning

confidence: 99%

Migraine genetics and prospects for pharmacotherapy

Colson

Fernandez

Griffiths

2007

Drug Development Research

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Migraine is a common complex neurological disorder with a well-known but poorly characterized genetic liability. The search for migraine susceptibility genes has been the focus of intense research. It is now believed that common migraine is not a single gene disorder, but attributable to several potentially interacting genetic variants. These variants may differ in each sufferer and interact with environmental factors to set the individual migraine threshold. This genetic liability may play an important role in the clinical heterogeneity seen in migraine and also in the variability of treatment response. This review will look at genetic loci implicated in migraine to date and consider their current or prospective role in migraine therapy. To elucidate the complex nature of migraine genetic liability, approaches that consider detailed endophenotypic profiles that encompass treatment response may provide much more relevant information than simple end diagnosis. Drug Dev Res 68: 282-293, 2007. r 2007 Wiley-Liss, Inc.

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Migraine: Current concepts and emerging therapies

Cited by 73 publications

References 87 publications

Structure–Activity Relationships of Phenylalkylamines as Agonist Ligands for 5‐HT_2A Receptors

Structure–Activity Relationships of Phenylalkylamines as Agonist Ligands for 5‐HT_2A Receptors

Association between Body Mass Index and Migraine

Migraine genetics and prospects for pharmacotherapy

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Migraine: Current concepts and emerging therapies

Cited by 73 publications

References 87 publications

Structure–Activity Relationships of Phenylalkylamines as Agonist Ligands for 5‐HT2A Receptors

Structure–Activity Relationships of Phenylalkylamines as Agonist Ligands for 5‐HT2A Receptors

Association between Body Mass Index and Migraine

Migraine genetics and prospects for pharmacotherapy

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Product

Resources

About

Structure–Activity Relationships of Phenylalkylamines as Agonist Ligands for 5‐HT_2A Receptors

Structure–Activity Relationships of Phenylalkylamines as Agonist Ligands for 5‐HT_2A Receptors