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Transient Receptor Potential (TRP) Channels as Novel Therapeutic Targets

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A special issue of Pharmaceuticals (ISSN 1424-8247). This special issue belongs to the section "Pharmacology".

Deadline for manuscript submissions: 20 February 2025 | Viewed by 18240

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Special Issue Editor

Dr. Dana Cucu

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Faculty of Biology, University of Bucharest, 050095 Bucharest, Romania
Interests: TRP channels; signalling pathways; tumoral process

Special Issue Information

Dear Colleagues,

The discovery of a transient receptor potential (TRP) channel in 1969 as a sensor for phototransduction in Drosophila melanogaster began an era of intensive research, leading to the identification of the TRP superfamily comprising 28 cation-permeable channels. The work culminated with the 2021 Nobel Prize in Physiology that was received by Dr. David Julius and Dr. Ardem Patapoutian for the discovery of the roles of these channels (TRP and Piezo) in temperature and touch sensation. The expression of these proteins was found in tissues as diverse as their function. Some of the family members (e.g., TRPV1 and TRPM8) were studied with electrophysiological and imaging methods in sensory neurons, where they were found to transduce thermal stimuli, neuropathic pain or taste. Others (e.g., TRPM8, TRPM7 and TRPV6) were analysed in cancer cells via molecular methods, and were found to participate in migration, apoptosis or proliferation, while others (e.g., TRPV1, TRPA1 and TRMP2) were determined to be sensors for reactive oxygen species and Ph variations.

Altogether, these knowledge and technical developments have brought us to the point where we can identify TRP channels as chemical and cellular sensors. It may be the moment that we propose some ways to use these poly-modal channels, as well as their agonists and antagonists, for therapy. However, before our knowledge in the field breaks the barrier from bench to bedside, we still need to answer some questions. We do not know, for instance, the signalling pathways in which TRP channels stimulate or inhibit cell migration, cell proliferation or other tumoral processes. Is this related only to the transport of Ca²⁺, as we are tempted to believe? Or are there other features independent of the channel conductance? How come TRPM8 are stimulators of migration in some tumoral cells and inhibitors in others? Which are the protein actors involved in the fine tuning all these functions? For these and many other questions, we want to search for answers in this Special Issue, "Transient Receptor Potential Channels as Novel Therapeutic Targets". Therefore, this is an invitation to all participants in this fascinating field to propose their models based on precise scientific methods, to decipher signalling pathways and to explain the dual role of these proteins in various tissues.

Dr. Dana Cucu
Guest Editor

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Keywords

TRP channels
signalling pathways
tumoral process
pain
migration
apoptosis
inflammation
oxidative stress

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Published Papers (12 papers)

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18 pages, 2966 KiB

Open AccessArticle

Lubiprostone Improves Distal Segment-Specific Colonic Contractions through TRPC4 Activation Stimulated by EP3 Prostanoid Receptor

by Byeongseok Jeong, Jun Hyung Lee, Jin-A Lee, Seong Jung Kim, Junhyung Lee, Insuk So, Jae Yeoul Jun and Chansik Hong

Pharmaceuticals 2024, 17(10), 1327; https://doi.org/10.3390/ph17101327 - 4 Oct 2024

Viewed by 584

Abstract

Background: Prokinetic agents are effective in increasing gastrointestinal (GI) contractility and alleviating constipation, often caused by slow intestinal motility. Lubiprostone (LUB), known for activating CLC-2 chloride channels, increases the chloride ion concentration in the GI tract, supporting water retention and stool movement. Despite its therapeutic efficacy, the exact mechanisms underlying its pharmacological action are poorly understood. Here, we investigated whether LUB activates the canonical transient receptor potential cation channel type 4 (TRPC4) through stimulation with E-type prostaglandin receptor (EP) type 3. Methods: Using isotonic tension recordings on mouse colon strips, we examined LUB-induced contractility in both proximal and distal colon segments. Quantitative real-time polymerase chain reaction (qRT-PCR) was conducted to determine mRNA levels of EP1-4 receptor subtypes in distal colonic muscular strips and isolated myocytes. The effects of a TRPC4 blocker and EP3 antagonist on LUB-stimulated contractions were also evaluated. Results: LUB showed significant contraction in the distal segment compared to the proximal segment. EP3 receptor mRNA levels were highly expressed in the distal colon tissue, which correlated with the observed enhanced contraction. Furthermore, LUB-induced spontaneous contractions in distal colon muscles were reduced by a TRPC4 blocker or EP3 antagonist, indicating that LUB-stimulated EP3 receptor activation may lead to TRPC4 activation and increased intracellular calcium in colonic smooth muscle. Conclusions: These findings suggest that LUB improves mass movement through indirect activation of the TRPC4 channel in the distal colon. The segment-specific action of prokinetic agents like LUB provides compelling evidence for a personalized approach to symptom management, supporting the defecation reflex. Full article

(This article belongs to the Special Issue Transient Receptor Potential (TRP) Channels as Novel Therapeutic Targets)

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16 pages, 4396 KiB

Open AccessArticle

Study on the Therapeutic Effects and Mechanisms of Gintonin in Irritable Bowel Syndrome and Its Relationship with TRPV1, TRPV4, and NaV1.5

by Na-Ri Choi, Seok-Jae Ko, Joo-Hyun Nam, Woo-Gyun Choi, Jong-Hwan Lee, Seung-Yeol Nah, Jae-Woo Park and Byung-Joo Kim

Pharmaceuticals 2024, 17(9), 1170; https://doi.org/10.3390/ph17091170 - 4 Sep 2024

Viewed by 872

Abstract

Irritable bowel syndrome (IBS) is a gastrointestinal (GI) disease accompanied by changes in bowel habits without any specific cause. Gintonin is a newly isolated glycoprotein from ginseng that is a lysophosphatidic acid (LPA) receptor ligand. To investigate the efficacy and mechanisms of action of gintonin in IBS, we developed a zymosan-induced IBS murine model. In addition, electrophysiological experiments were conducted to confirm the relevance of various ion channels. In mice, gintonin restored colon length and weight to normal and decreased stool scores, whilst food intake remained constant. Colon mucosal thickness and inflammation-related tumor necrosis factor-α levels were decreased by gintonin, along with a reduction in pain-related behaviors. In addition, the fecal microbiota from gintonin-treated mice had relatively more Lactobacillaceae and Lachnospiraceae and less Bacteroidaceae than microbiota from the control mice. Moreover, gintonin inhibited transient receptor potential vanilloid (TRPV) 1 and TRPV4 associated with visceral hypersensitivity and voltage-gated Na⁺ 1.5 channels associated with GI function. These results suggest that gintonin may be one of the effective components in the treatment of IBS. Full article

(This article belongs to the Special Issue Transient Receptor Potential (TRP) Channels as Novel Therapeutic Targets)

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16 pages, 5679 KiB

Open AccessArticle

TRPV1 Activation Antagonizes High-Fat Diet-Induced Obesity at Thermoneutrality and Enhances UCP-1 Transcription via PRDM-16

by Padmamalini Baskaran, Noah Gustafson and Nicolas Chavez

Pharmaceuticals 2024, 17(8), 1098; https://doi.org/10.3390/ph17081098 - 21 Aug 2024

Viewed by 1267

Abstract

Body weight is a balance between energy intake and energy expenditure. Energy expenditure is mainly governed by physical activity and adaptive thermogenesis. Adaptive dietary thermogenesis in brown and beige adipose tissue occurs through mitochondrial uncoupling protein (UCP-1). Laboratory mice, when housed at an ambient temperature of 22–24 °C, maintain their body temperature by dietary thermogenesis, eating more food compared to thermoneutrality. Humans remain in the thermoneutral zone (TNZ) without expending extra energy to maintain normal body temperature. TRPV1 activation by capsaicin (CAP) inhibited weight gain in mice housed at ambient temperature by activating UCP-1-dependent adaptive thermogenesis. Hence, we evaluated the effect of CAP feeding on WT and UCP-1^−/− mice maintained under thermoneutral conditions. Our research presents novel findings that TRPV1 activation by CAP at thermoneutrality counters obesity in WT mice and promotes PRDM-16-dependent UCP-1 transcription. CAP fails to inhibit weight gain in UCP-1^−/− mice housed at thermoneutrality and in adipose tissue-specific PRDM-16^−/− mice. In vitro, capsaicin treatment increases UCP-1 transcription in PRDM-16 overexpressing cells. Our data indicate for the first time that TRPV1 activation counters obesity at thermoneutrality permissive for UCP-1 and the enhancement of PRDM-16 is not beneficial in the absence of UCP-1. Full article

(This article belongs to the Special Issue Transient Receptor Potential (TRP) Channels as Novel Therapeutic Targets)

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16 pages, 8817 KiB

Open AccessArticle

Transient Receptor Potential Ankyrin 1 (TRPA1) Modulation by 4-Hydroxynonenal (4-HNE) in Pancreatic Adenocarcinoma Cell Lines: Putative Roles for Therapies

by Florentina Piciu, Dan Domocos, Gabriela Chiritoiu, Marioara Chiritoiu-Butnaru, Maria Mernea, Cezar Gabriel Popescu, Dragos Paul Mihai, Bianca Galateanu, Ariana Hudita, Alexandru Babes and Dana Cucu

Pharmaceuticals 2024, 17(3), 344; https://doi.org/10.3390/ph17030344 - 6 Mar 2024

Viewed by 1460

Abstract

Background: Transient receptor potential channels (TRP) are overexpressed in some pancreatic adenocarcinoma (PDAC) patients and cell lines, settling them as putative therapeutic targets in this disease. Reactive oxygen species (ROS), with levels increased in PDAC, modulate some members of the TRP family renamed “redox channels”. Here, we investigate the direct effects of 4-hydroxinonenal (4-HNE) on TRPA1, natively expressed in PDAC cell lines and in association with cell migration and cell cycle progression. Methods: We performed microfluorimetry experiments, while the activation of resident membrane channels was investigated using confocal microscopy. We applied a prospective molecular docking of 4-HNE using Autodock and AutoDock Tools4. Also, we simulated the diffusion of 4-HNE through the membrane from the extracellular space with the Permeability of Molecules across Membranes (PerMM) web server. The analysis of cell migration was performed using the wound healing assay, and cell cycle progression was acquired using a Beckman Coulter CytoFlex flow cytometer. Results: Our results show, for the first time in PDAC, that 4-HNE diffuses through the cell membrane and rapidly activates Ca²⁺ uptake in PDAC cells. This process depends on TRPA1 activation, as 4-HNE forms a covalent binding with a pocket-like region within the intracellular N-terminal of the channel, shaped by the cysteine residues 621, 641, and 665. The activation of TRPA1 by 4-HNE inhibits cell migration and induces cell cycle arrest in the G2/M phase. Conclusions: Our study brings new insights into the effects of 4-HNE, highlighting the activation of the TRPA1 channel, a druggable, putative target for PDAC-expressing tumors. Full article

(This article belongs to the Special Issue Transient Receptor Potential (TRP) Channels as Novel Therapeutic Targets)

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23 pages, 3619 KiB

Open AccessArticle

TRPV4 Activation during Guinea Pig Airway Smooth Muscle Contraction Promotes Ca²⁺ and Na⁺ Influx

by Luis M. Montaño, Abril Carbajal-García, María F. Casas-Hernández, David Arredondo-Zamarripa and Jorge Reyes-García

Pharmaceuticals 2024, 17(3), 293; https://doi.org/10.3390/ph17030293 - 24 Feb 2024

Cited by 1 | Viewed by 1352

Abstract

Airway smooth muscle (ASM) contraction is determined by the increase in intracellular Ca²⁺ concentration ([Ca²⁺]_i) caused by its release from the sarcoplasmic reticulum (SR) or by extracellular Ca²⁺ influx. Major channels involved in Ca²⁺ influx in ASM cells are L-type voltage-dependent Ca²⁺ channels (L-VDCCs) and nonselective cation channels (NSCCs). Transient receptor potential vanilloid 4 (TRPV4) is an NSCC recently studied in ASM. Mechanical stimuli, such as contraction, can activate TRPV4. We investigated the possible activation of TRPV4 by histamine (His)- or carbachol (CCh)-induced contraction in guinea pig ASM. In single myocytes, the TRPV4 agonist (GSK101) evoked an increase in [Ca²⁺]_i, characterized by a slow onset and a plateau phase. The TRPV4 antagonist (GSK219) decreased channel activity by 94%, whereas the Ca²⁺-free medium abolished the Ca²⁺ response induced by GSK101. Moreover, GSK101 caused Na⁺ influx in tracheal myocytes. GSK219 reduced the Ca²⁺ peak and the Ca²⁺ plateau triggered by His or CCh. TRPV4 blockade shifted the concentration–response curve relating to His and CCh to the right in tracheal rings and reduced the maximal contraction. Finally, the activation of TRPV4 in single myocytes increased the Ca²⁺ refilling of the SR. We conclude that contraction of ASM cells after stimulation with His or CCh promotes TRPV4 activation, the subsequent influx of Ca²⁺ and Na⁺, and the opening of L-VDCCs. The entry of Ca²⁺ into ASM cells via TRPV4 and L-VDCCs contributes to optimal smooth muscle contraction. Full article

(This article belongs to the Special Issue Transient Receptor Potential (TRP) Channels as Novel Therapeutic Targets)

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14 pages, 4892 KiB

Open AccessArticle

Functional Analysis of TRPA1, TRPM3, and TRPV1 Channels in Human Dermal Arteries and Their Role in Vascular Modulation

by Eduardo Rivera-Mancilla, Linda Al-Hassany, Heleen Marynissen, Dorien Bamps, Ingrid M. Garrelds, Jérôme Cornette, A. H. Jan Danser, Carlos M. Villalón, Jan N. de Hoon and Antoinette MaassenVanDenBrink

Pharmaceuticals 2024, 17(2), 156; https://doi.org/10.3390/ph17020156 - 25 Jan 2024

Cited by 1 | Viewed by 1637

Abstract

Transient receptor potential (TRP) channels are pivotal in modulating vascular functions. In fact, topical application of cinnamaldehyde or capsaicin (TRPA1 and TRPV1 channel agonists, respectively) induces “local” changes in blood flow by releasing vasodilator neuropeptides. We investigated TRP channels’ contributions and the pharmacological mechanisms driving vasodilation in human isolated dermal arteries. Ex vivo studies assessed the vascular function of artery segments and analyzed the effects of different compounds. Concentration–response curves to cinnamaldehyde, pregnenolone sulfate (PregS, TRPM3 agonist), and capsaicin were constructed to evaluate the effect of the antagonists HC030031 (TRPA1); isosakuranetin (TRPM3); and capsazepine (TRPV1). Additionally, the antagonists/inhibitors olcegepant (CGRP receptor); L-NAME (nitric oxide synthase); indomethacin (cyclooxygenase); TRAM-34 plus apamin (K⁺ channels); and MK-801 (NMDA receptors, only for PregS) were used. Moreover, CGRP release was assessed in the organ bath fluid post-agonist-exposure. In dermal arteries, cinnamaldehyde- and capsaicin-induced relaxation remained unchanged after the aforementioned antagonists, while PregS-induced relaxation was significantly inhibited by isosakuranetin, L-NAME and MK-801. Furthermore, there was a significant increase in CGRP levels post-agonist-exposure. In our experimental model, TRPA1 and TRPV1 channels seem not to be involved in cinnamaldehyde- or capsaicin-induced relaxation, respectively, whereas TRPM3 channels contribute to PregS-induced relaxation, possibly via CGRP-independent mechanisms. Full article

(This article belongs to the Special Issue Transient Receptor Potential (TRP) Channels as Novel Therapeutic Targets)

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11 pages, 2352 KiB

Open AccessArticle

Pharmacological Differences between Native Homomeric Transient Receptor Potential Canonical Type 4 Channels and Heteromeric Transient Receptor Potential Canonical Type 1/4 Channels in Lateral Septal Neurons

by Kevin D. Phelan, U Thaung Shwe and Fang Zheng

Pharmaceuticals 2023, 16(9), 1291; https://doi.org/10.3390/ph16091291 - 13 Sep 2023

Cited by 3 | Viewed by 972

Abstract

Given the unique expression patterns and revelations of its critical involvement in a host of neurological disorders, the TRPC1/4/5 subgroup has become an intense target of drug development, and some compounds are now in clinical trials. However, little is known about the exact subunit composition of this subfamily of TRPC channels in various native tissues, and whether it has functional and pharmacological implications. In this study, we investigated the effects of two TRPC4 modulators located in the lateral septum, in which a metabotropic glutamate receptor (mGluR) agonist-induced plateau potential is mediated by TRPC channels composed of TRPC1 and TRPC4. Lateral septal neurons were recorded intracellularly in brain slices using sharp electrodes. Drugs were applied via bath superfusion. We showed that the plateau potential in mice lacking TRPC1 is modulated by ML204 and La³⁺ in a manner that is like homomeric TRPC4 channels in artificial expression systems. However, the plateau potential that is primarily mediated by heteromeric TRPC1/4 channels in lateral septal neurons in wildtype mice was modulated differently by ML204 and La³⁺. Our data suggest that native homomeric TRPC4 channels and heteromeric TRPC1/4 channels are pharmacologically distinct, and the current drug development strategy regarding TRPC1/4/5 may need to be reevaluated. Full article

(This article belongs to the Special Issue Transient Receptor Potential (TRP) Channels as Novel Therapeutic Targets)

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16 pages, 4670 KiB

Open AccessArticle

Electrophilic Agonists Modulate the Transient Receptor Potential Ankyrin-1 Channels Mediated by Insulin and Glucagon-like Peptide-1 Secretion for Glucose Homeostasis

by Marisa Jadna Silva Frederico, Andreza Cipriani, Jocelyn Brice Alexandre Heim, Ana Karla Bittencourt Mendes, Marcela Aragón, Joana Margarida Gaspar, Nylane Maria Nunes De Alencar and Fátima Regina Mena Barreto Silva

Pharmaceuticals 2023, 16(8), 1167; https://doi.org/10.3390/ph16081167 - 16 Aug 2023

Cited by 3 | Viewed by 1149

Abstract

This pre-clinical study investigated the transient receptor potential ankyrin-1 (TRPA1) channels on modulating targets for glucose homeostasis using agonists: the electrophilic agonists, cinnamaldehyde (CIN) and allyl isothiocyanate (AITC), and the non-electrophilic agonist, carvacrol (CRV). A glucose tolerance test was performed on rats. CIN and AITC (5, 10 and 20 mg/kg) or CRV (25, 100, 300, and 600 mg/kg) were administered intraperitoneally (i.p.), and glycemia was measured. In the intestine, Glucagon-like peptide-1 (GLP-1) and disaccharidase activity were evaluated (in vivo and in vitro, respectively). Furthermore, in vivo and in vitro insulin secretion was determined. Islets were used to measure insulin secretion and calcium influx. CIN and AITC improved glucose tolerance and increased insulin secretion in vivo and in vitro. CRV was unable to reduce glycemia. Electrophilic agonists, CIN and AITC, inhibited disaccharidases and acted as secretagogues in the intestine by inducing GLP-1 release in vivo and in vitro and contributed to insulin secretion and glycemia. The effect of CIN on calcium influx in pancreatic islets (insulin secretion) involves voltage-dependent calcium channels and calcium from stores. TRPA1 triggers calcium influx and potentiates intracellular calcium release to induce insulin secretion, suggesting that electrophilic agonists mediate this signaling transduction for the control of glycemia. Full article

(This article belongs to the Special Issue Transient Receptor Potential (TRP) Channels as Novel Therapeutic Targets)

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13 pages, 3018 KiB

Open AccessArticle

Analysis of the Effect of the TRPC4/TRPC5 Blocker, ML204, in Sucrose-Induced Metabolic Imbalance

by Mizael C. Araújo, Suzany H. S. Soczek, Jaqueline P. Pontes, Bruno A. S. Pinto, Lucas M. França, Bruna da Silva Soley, Gabriela S. Santos, Warlison F. de Silva Saminez, Fernanda K. M. Fernandes, João L. do Carmo Lima, Daniele Maria-Ferreira, João F. S. Rodrigues, Nara L. M. Quintão, Valério Monteiro-Neto, Antônio M. A. Paes and Elizabeth S. Fernandes

Pharmaceuticals 2023, 16(8), 1100; https://doi.org/10.3390/ph16081100 - 3 Aug 2023

Cited by 5 | Viewed by 1457

Abstract

Sugar-induced metabolic imbalances are a major health problem since an excessive consumption of saccharides has been linked to greater obesity rates at a global level. Sucrose, a disaccharide composed of 50% glucose and 50% fructose, is commonly used in the food industry and found in a range of fast, restaurant, and processed foods. Herein, we investigated the effects of a TRPC4/TRPC5 blocker, ML204, in the metabolic imbalances triggered by early exposure to sucrose-enriched diet in mice. TRPC4 and TRPC5 belong to the family of non-selective Ca⁺² channels known as transient receptor potential channels. High-sucrose (HS)-fed animals with hyperglycaemia and dyslipidaemia, were accompanied by increased body mass index. mesenteric adipose tissue accumulation with larger diameter cells and hepatic steatosis in comparison to those fed normal diet. HS mice also exhibited enhanced adipose, liver, and pancreas TNFα and VEGF levels. ML204 exacerbated hyperglycaemia, dyslipidaemia, fat tissue deposition, hepatic steatosis, and adipose tissue and liver TNFα in HS-fed mice. Normal mice treated with the blocker had greater hepatic steatosis and adipose tissue cell numbers/diameter than those receiving vehicle, but showed no significant changes in tissue inflammation, glucose, and lipid levels. The results indicate that TRPC4/TRPC5 protect against the metabolic imbalances caused by HS ingestion. Full article

(This article belongs to the Special Issue Transient Receptor Potential (TRP) Channels as Novel Therapeutic Targets)

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Review

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13 pages, 281 KiB

Open AccessReview

TRPV1 Channels in the Central Nervous System as Drug Targets

by Loris A. Chahl

Pharmaceuticals 2024, 17(6), 756; https://doi.org/10.3390/ph17060756 - 7 Jun 2024

Cited by 1 | Viewed by 1406

Abstract

TRPV1 channels are polymodal cation channels located predominantly on primary afferent neurons that are activated by inflammatory mediators, capsaicin (the active component in chili peppers), and noxious heat. TRPV1 channel antagonists are potential new analgesic agents, but their development has been hindered by the finding that they also produce loss of thermal homeostasis and response to noxious heat. Results from recent studies of the TRPV1 channel indicate that it might be possible to develop TRPV1 channel antagonists that inhibit pain without affecting noxious heat sensation. TRPV1 channels are also present in the central nervous system (CNS) and have been implicated in learning, memory, and behaviour. TRPV1 channel modulators have been proposed to have possible therapeutic potential in the treatment of neurological and psychiatric conditions. However, further understanding of the role of TRPV1 channels in the CNS is required before therapeutic advances in the treatment of neuropsychiatric conditions with TRPV1 channel modulators can be made. Full article

(This article belongs to the Special Issue Transient Receptor Potential (TRP) Channels as Novel Therapeutic Targets)

18 pages, 1424 KiB

Open AccessReview

Targeting Transient Receptor Potential (TRP) Channels, Mas-Related G-Protein-Coupled Receptors (Mrgprs), and Protease-Activated Receptors (PARs) to Relieve Itch

by Merab G. Tsagareli, Taylor Follansbee, Mirela Iodi Carstens and Earl Carstens

Pharmaceuticals 2023, 16(12), 1707; https://doi.org/10.3390/ph16121707 - 8 Dec 2023

Cited by 3 | Viewed by 2490

Abstract

Itch (pruritus) is a sensation in the skin that provokes the desire to scratch. The sensation of itch is mediated through a subclass of primary afferent sensory neurons, termed pruriceptors, which express molecular receptors that are activated by itch-evoking ligands. Also expressed in pruriceptors are several types of Transient Receptor Potential (TRP) channels. TRP channels are a diverse class of cation channels that are responsive to various somatosensory stimuli like touch, pain, itch, and temperature. In pruriceptors, TRP channels can be activated through intracellular signaling cascades initiated by pruritogen receptors and underly neuronal activation. In this review, we discuss the role of TRP channels TRPA1, TRPV1, TRPV2, TRPV3, TRPV4, TRPM8, and TRPC3/4 in acute and chronic pruritus. Since these channels often mediate itch in association with pruritogen receptors, we also discuss Mas-related G-protein-coupled receptors (Mrgprs) and protease-activated receptors (PARs). Additionally, we cover the exciting therapeutic targets amongst the TRP family, as well as Mrgprs and PARs for the treatment of pruritus. Full article

(This article belongs to the Special Issue Transient Receptor Potential (TRP) Channels as Novel Therapeutic Targets)

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16 pages, 918 KiB

Open AccessReview

Role of Resolvins in Inflammatory and Neuropathic Pain

by Jaeik Park, Jueun Roh, Jingying Pan, Yong Ho Kim, Chul-Kyu Park and Youn Yi Jo

Pharmaceuticals 2023, 16(10), 1366; https://doi.org/10.3390/ph16101366 - 27 Sep 2023

Cited by 2 | Viewed by 1911

Abstract

Chronic pain is an unpleasant experience associated with actual or potential tissue damage. Inflammatory pain alerts the body to inflammation and promotes healing; however, unresolved inflammation can lead to chronic pain. Conversely, neuropathic pain, due to somatosensory damage, can be a disease in itself. However, inflammation plays a considerable role in the progression of both types of pain. Resolvins, derived from omega-3 fatty acids, actively suppress pro-inflammatory mediators and aid in the resolution of inflammation. Resolvins alleviate various inflammatory and neuropathic pain models by reducing hypersensitivity and regulating inflammatory cytokines and glial activation in the spinal cord and dorsal root ganglia. Thus, resolvins are a promising alternative for pain management with the potential to reduce the side effects associated with conventional medications. Continued research is crucial to unlock the therapeutic potential of resolvins and integrate them into effective clinical pain management strategies. This review aimed to evaluate the literature surrounding the resolvins in inflammatory and neuropathic pain. Full article

(This article belongs to the Special Issue Transient Receptor Potential (TRP) Channels as Novel Therapeutic Targets)

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