GABAA receptor modulation: Potential to deliver novel pain medicines?

Munro, Gordon; Hansen, René Rydhof; Mirza, Naheed

doi:10.1016/j.ejphar.2013.01.070

Cited by 45 publications

(36 citation statements)

References 67 publications

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“…Numerous articles have reviewed ongoing efforts and prospects for therapies targeting different aspects of synaptic inhibition: restoring normal chloride regulation, [136][137][138] enhancing GABAergic transmission [139][140][141][142] or enhancing glycinergic transmission 143,144 not to mention related issues such as microglia and inflammation. Rather than repeat the details here, a few simple observations will be made to highlight the practical utility of the information conveyed earlier in this chapter.…”

Section: Implications For Therapeutic Interventionsmentioning

confidence: 99%

Synaptic Inhibition and Disinhibition in the Spinal Dorsal Horn

Prescott

2015

Progress in Molecular Biology and Translational Science

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Section: Implications For Therapeutic Interventionsmentioning

confidence: 99%

Synaptic Inhibition and Disinhibition in the Spinal Dorsal Horn

Prescott

2015

Progress in Molecular Biology and Translational Science

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“…Because sedation is primarily produced by activation of GABAa-α1 receptors, it follows that work related to subunit selective GABA agonists with different pharmacologic profiles would attract significant attention [59]. The potential for GABAergic analgesic development is bolstered by the identification of distinct GABAa subunit populations in the dorsal horn of the spinal cord and on primary afferent neurons [60].…”

Section: How Do Pharmacological Interventions Take Advantage Of Pamentioning

confidence: 99%

“…Agents that selectively inhibit TNF-α in the substantia gelatinosa could theoretically prevent the development of GABA- or glutamate-rooted causes of chronic pain. Similarly, GABA-acting drugs, which are not currently designed for providing pain relief, could theoretically be used to alleviate chronic pain or balance imbalanced pain neurotransmitters [59]. …”

Section: Five-year Viewmentioning

confidence: 99%

Transmission pathways and mediators as the basis for clinical pharmacology of pain

Kirkpatrick

McEntire

Smith

et al. 2016

Expert Review of Clinical Pharmacology

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Introduction Mediators in pain transmission are the targets of a multitude of different analgesic pharmaceuticals. This review explores the most significant mediators of pain transmission as well as the pharmaceuticals that act on them. Areas Covered The review explores many of the key mediators of pain transmission. In doing so, this review uncovers important areas for further research. It also highlights agents with potential for producing novel analgesics, probes important interactions between pain transmission pathways that could contribute to synergistic analgesia, and emphasizes transmission factors that participate in transforming acute injury into chronic pain. Expert Commentary This review examines current pain research, particularly in the context of identifying novel analgesics, highlighting interactions between analgesic transmission pathways, and discussing factors that may contribute to the development of chronic pain after an acute injury.

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“…GABA A receptors have been widely reported to be involved in several models of somatic pain and are actively pursued as potential targets for novel analgesic drugs. [28][29][30] In contrast, their role in visceral pain condition was confirmed only recently. Sengupta et al 31 reported that down regulation of microRNA-mediated GABA A1 receptor subunit in adult spinal cord following neonatal cystitis was responsible for the development of chronic visceral pain in rats.…”

Section: Gamma Aminobutyric Acid Receptorsmentioning

confidence: 99%

Role of Principal Ionotropic and Metabotropic Receptors in Visceral Pain

Kannampalli

Sengupta

2015

J Neurogastroenterol Motil

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Visceral pain is the most common form of pain caused by varied diseases and a major reason for patients to seek medical consultation. It also leads to a significant economic burden due to workdays lost and reduced productivity. Further, long-term use of non-specific medications is also associated with side effects affecting the quality of life. Despite years of extensive research and the availability of several therapeutic options, management of patients with chronic visceral pain is often inadequate, resulting in frustration for both patients and physicians. This is, most likely, because the mechanisms associated with chronic visceral pain are different from those of acute pain. Accumulating evidence from years of research implicates several receptors and ion channels in the induction and maintenance of central and peripheral sensitization during chronic pain states. Understanding the specific role of these receptors will facilitate to capitalize on their unique properties to augment the therapeutic efficacy while at the same time minimizing unwanted side effects. The aim of this review is to provide a concise review of the recent literature that reports on the role of principal ionotropic receptors and metabotropic receptors in the modulation visceral pain. We also include an overview of the possibility of these receptors as potential new targets for the treatment of chronic visceral pain conditions. (J Neurogastroenterol Motil 2015;21:147-158)

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GABAA receptor modulation: Potential to deliver novel pain medicines?

Cited by 45 publications

References 67 publications

Synaptic Inhibition and Disinhibition in the Spinal Dorsal Horn

Synaptic Inhibition and Disinhibition in the Spinal Dorsal Horn

Transmission pathways and mediators as the basis for clinical pharmacology of pain

Role of Principal Ionotropic and Metabotropic Receptors in Visceral Pain

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