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Pharmaceuticals
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Emerging Pain Targets and Therapy
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Emerging Pain Targets and Therapy

A special issue of Pharmaceuticals (ISSN 1424-8247).

Deadline for manuscript submissions: closed (31 July 2012) | Viewed by 66764

Special Issue Editor

Dr. Kim Lawson

E-Mail Website
Guest Editor
Department of Biosciences and Chemistry, Biomolecular Sciences Research Centre, Faculty of Health and Wellbeing, Sheffield Hallam University, Sheffield, UK
Interests: fibromyalgia; pain; potassium channels; drug design/discovery
Special Issues, Collections and Topics in MDPI journals

Special Issue Information

Dear Colleagues,

Pain remains a major clinical challenge with the management of pain the most frequent issue encountered by clinicians. Many current analgesics are limited by serious unwanted effects, while for some pain conditions there are no effective analgesics. Advances in molecular biological techniques that have enabled the discovery of specific molecules involved in pain production have contributed to a better understanding of pain and the mechanisms of different types of pain and are providing clues for the development of novel pharmacotherapies for specific pain types. This increased understanding of pain physiology has offered a number of potential targets (e.g. TRPV1, voltage-gated sodium channels, calcium channels, glutamate receptors, cannabinoids) for future treatments, in particular for neuropathic and chronic pain. This special issue is intended to provide the reader with an insight into the progress made in this field through novel contributions of original papers and critical reviews.

Dr. Kim Lawson
Guest Editor

Keywords

  • pain
  • pain pathways
  • emerging targets
  • molecular biology
  • novel therapies
  • ion channels

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Related Special Issue

Published Papers (6 papers)

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Research

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1086 KiB  
Article
Real-Time Translocation and Function of PKCβII Isoform in Response to Nociceptive Signaling via the TRPV1 Pain Receptor
by Sravan Mandadi, Patricia J. Armati and Basil D. Roufogalis
Pharmaceuticals 2011, 4(11), 1503-1517; https://doi.org/10.3390/ph4111503 - 11 Nov 2011
Cited by 3 | Viewed by 6994
Abstract
Serine/threonine protein kinase C βII isoform (PKCβII) or the pain receptor transient receptor potential vanilloid 1 (TRPV1) have been separately implicated in mediating heat hyperalgesia during inflammation or diabetic neuropathy. However, detailed information on the role of PKC βII in nociceptive signaling mediated [...] Read more.
Serine/threonine protein kinase C βII isoform (PKCβII) or the pain receptor transient receptor potential vanilloid 1 (TRPV1) have been separately implicated in mediating heat hyperalgesia during inflammation or diabetic neuropathy. However, detailed information on the role of PKC βII in nociceptive signaling mediated by TRPV1 is lacking. This study presents evidence for activation and translocation of the PKC βII isoform as a signaling event in nociception mediated by activation of TRPV1 by capsaicin. We show that capsaicin induces translocation of cytosolic PKCβII isoform fused with enhanced green fluorescence protein (PKCβII-EGFP) in dorsal root ganglion (DRG) neurons. We also show capsaicin-induced translocation in Chinese Hamster Ovarian (CHO) cells co-transfected with TRPV1 and PKCβII-EGFP, but not in CHO cells expressing PKCβII-EGFP alone. By contrast, the PKC activator phorbol-12-myristate-13-acetate (PMA) induced translocation of PKCβII-EGFP which was sustained and independent of calcium or TRPV1. In addition PMA-induced sensitization of TRPV1 to capsaicin response in DRG neurons was attenuated by PKCβII blocker CGP 53353. Capsaicin response via TRPV1 in the DRG neurons was confirmed by TRPV1 antagonist AMG 9810. These results suggested a novel and potential signaling link between PKCβII and TRPV1. These cell culture models provide a platform for investigating mechanisms of painful neuropathies mediated by nociceptors expressing the pain sensing gene TRPV1, and its regulation by the PKC isoform PKCβII. Full article
(This article belongs to the Special Issue Emerging Pain Targets and Therapy)
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Review

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209 KiB  
Review
The Use of California Sagebrush (Artemisia californica) Liniment to Control Pain
by James D. Adams, Jr.
Pharmaceuticals 2012, 5(10), 1045-1053; https://doi.org/10.3390/ph5101045 - 27 Sep 2012
Cited by 13 | Viewed by 15709
Abstract
The incidence of arthritis is increasing every year, as does the need for pain medication. The current work reviews an American Indian liniment that is traditionally used for pain therapy. The chemistry, therapeutic use and safety of the liniment are reviewed. The liniment [...] Read more.
The incidence of arthritis is increasing every year, as does the need for pain medication. The current work reviews an American Indian liniment that is traditionally used for pain therapy. The chemistry, therapeutic use and safety of the liniment are reviewed. The liniment contains monoterpenoids, sesquiterpenes, flavonoids, alkaloids and other compounds. Full article
(This article belongs to the Special Issue Emerging Pain Targets and Therapy)
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140 KiB  
Review
Role of Transient Receptor Potential Vanilloid 1 in Inflammation and Autoimmune Diseases
by Fumio Tsuji and Hiroyuki Aono
Pharmaceuticals 2012, 5(8), 837-852; https://doi.org/10.3390/ph5080837 - 17 Aug 2012
Cited by 48 | Viewed by 10142
Abstract
Transient receptor potential vanilloid 1 (TRPV1), a non-selective cation channel, is a receptor activated by high temperatures and chemical agonists such as the vanilloids and protons. Because of these properties, TRPV1 has emerged as a polymodal nocisensor of nociceptive afferent neurons. TRPV1 is [...] Read more.
Transient receptor potential vanilloid 1 (TRPV1), a non-selective cation channel, is a receptor activated by high temperatures and chemical agonists such as the vanilloids and protons. Because of these properties, TRPV1 has emerged as a polymodal nocisensor of nociceptive afferent neurons. TRPV1 is thought to be a central transducer of hyperalgesia and a prime target for controlling pain pharmacologically because it is a point where many proalgesic pathways converge and it is upregulated and sensitized by inflammation and injury. However, whether TRPV1 agonists promote or inhibit inflammation remains unclear. We recently demonstrated that SA13353 (1-[2-(1-adamantyl)ethyl]-1-pentyl-3-[3-(4-pyridyl)propyl]urea), a novel TRPV1 agonist, inhibits tumor necrosis factor-a production by the activation of capsaicin-sensitive afferent neurons and reduces the severity of symptoms in kidney injury, lung inflammation, arthritis, and encephalomyelitis. These results suggest that TRPV1 agonists may act as anti-inflammatories in certain inflammatory and autoimmune conditions in vivo. Given the potential deleterious effects of inhibiting the population of channels with a protective function, caution should be taken in the use of potent TRPV1 antagonists as a general strategy to treat inflammation. Further studies are required to clarify the role of TRPV1 and neuropeptides, which are released because of TRPV1 activation in inflammation and autoimmune diseases. Full article
(This article belongs to the Special Issue Emerging Pain Targets and Therapy)
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287 KiB  
Review
Receptor and Channel Heteromers as Pain Targets
by Kelly A. Berg, Amol M. Patwardhan and Armen N. Akopian
Pharmaceuticals 2012, 5(3), 249-278; https://doi.org/10.3390/ph5030249 - 23 Feb 2012
Cited by 8 | Viewed by 7822
Abstract
Recent discoveries indicate that many G-protein coupled receptors (GPCRs) and channels involved in pain modulation are able to form receptor heteromers. Receptor and channel heteromers often display distinct signaling characteristics, pharmacological properties and physiological function in comparison to monomer/homomer receptor or ion channel [...] Read more.
Recent discoveries indicate that many G-protein coupled receptors (GPCRs) and channels involved in pain modulation are able to form receptor heteromers. Receptor and channel heteromers often display distinct signaling characteristics, pharmacological properties and physiological function in comparison to monomer/homomer receptor or ion channel counterparts. It may be possible to capitalize on such unique properties to augment therapeutic efficacy while minimizing side effects. For example, drugs specifically targeting heteromers may have greater tissue specificity and analgesic efficacy. This review will focus on current progress in our understanding of roles of heteromeric GPCRs and channels in pain pathways as well as strategies for controlling pain pathways via targeting heteromeric receptors and channels. This approach may be instrumental in the discovery of novel classes of drugs and expand our repertoire of targets for pain pharmacotherapy. Full article
(This article belongs to the Special Issue Emerging Pain Targets and Therapy)
473 KiB  
Review
TRPV1 Antagonists and Chronic Pain: Beyond Thermal Perception
by Michael R. Brandt, Chad E. Beyer and Stephen M. Stahl
Pharmaceuticals 2012, 5(2), 114-132; https://doi.org/10.3390/ph5020114 - 2 Feb 2012
Cited by 38 | Viewed by 10250
Abstract
In the last decade, considerable evidence as accumulated to support the development of Transient Receptor Potential Vanilloid 1 (TRPV1) antagonists for the treatment of various chronic pain conditions. Whereas there is a widely accepted rationale for the development of TRPV1 antagonists for the [...] Read more.
In the last decade, considerable evidence as accumulated to support the development of Transient Receptor Potential Vanilloid 1 (TRPV1) antagonists for the treatment of various chronic pain conditions. Whereas there is a widely accepted rationale for the development of TRPV1 antagonists for the treatment of various inflammatory pain conditions, their development for indications of chronic pain, where conditions of tactical, mechanical and spontaneous pain predominate, is less clear. Preclinical localization and expression studies provide a firm foundation for the use of molecules targeting TRPV1 for conditions of bone pain, osteoarthritis and neuropathic pain. Selective TRPV1 antagonists weakly attenuate tactile and mechanical hypersensivity and are partially effective for behavioral and electrophysiological endpoints that incorporate aspects of spontaneous pain. While initial studies with TRPV1 antagonist in normal human subjects indicate a loss of warm thermal perception, clinical studies assessing allelic variants suggests that TRPV1 may mediate other sensory modalities under certain conditions. The focus of this review is to summarize the current perspectives of TRPV1 for the treatment of conditions beyond those with a primary thermal sensitivity. Full article
(This article belongs to the Special Issue Emerging Pain Targets and Therapy)
1565 KiB  
Review
New Strategies to Develop Novel Pain Therapies: Addressing Thermoreceptors from Different Points of View
by Asia Fernández-Carvajal, Gregorio Fernández-Ballester, Isabel Devesa, José Manuel González-Ros and Antonio Ferrer-Montiel
Pharmaceuticals 2012, 5(1), 16-48; https://doi.org/10.3390/ph5010016 - 27 Dec 2011
Cited by 21 | Viewed by 14945
Abstract
One approach to develop successful pain therapies is the modulation of dysfunctional ion channels that contribute to the detection of thermal, mechanical and chemical painful stimuli. These ion channels, known as thermoTRPs, promote the sensitization and activation of primary sensory neurons known as [...] Read more.
One approach to develop successful pain therapies is the modulation of dysfunctional ion channels that contribute to the detection of thermal, mechanical and chemical painful stimuli. These ion channels, known as thermoTRPs, promote the sensitization and activation of primary sensory neurons known as nociceptors. Pharmacological blockade and genetic deletion of thermoTRP have validated these channels as therapeutic targets for pain intervention. Several thermoTRP modulators have progressed towards clinical development, although most failed because of the appearance of unpredicted side effects. Thus, there is yet a need to develop novel channel modulators with improved therapeutic index. Here, we review the current state-of-the art and illustrate new pharmacological paradigms based on TRPV1 that include: (i) the identification of activity-dependent modulators of this thermoTRP channel; (ii) the design of allosteric modulators that interfere with protein-protein interaction involved in the functional coupling of stimulus sensing and gate opening; and (iii) the development of compounds that abrogate the inflammation-mediated increase of receptor expression in the neuronal surface. These new sites of action represent novel strategies to modulate pathologically active TRPV1, while minimizing an effect on the TRPV1 subpopulation involved in physiological and protective roles, thus increasing their potential therapeutic use. Full article
(This article belongs to the Special Issue Emerging Pain Targets and Therapy)
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