3,173 results match your criteria channel trpv1


TRPV1 activation and internalization is part of the LPS-induced inflammation in human iPSC-derived cardiomyocytes.

Sci Rep 2021 Jul 19;11(1):14689. Epub 2021 Jul 19.

First Department of Medicine, Faculty of Medicine, University Medical Center Mannheim (UMM), University of Heidelberg, Theodor-Kutzer-Ufer 1-3, 68167, Mannheim, Germany.

The non-selective cation channel transient receptor potential vanilloid 1 (TRPV1) is expressed throughout the cardiovascular system. Recent evidence shows a role for TRPV1 in inflammatory processes. The role of TRPV1 for myocardial inflammation has not been established yet. Read More

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Plasticity in Intrinsic Excitability of Hypothalamic Magnocellular Neurosecretory Neurons in Late-Pregnant and Lactating Rats.

Int J Mol Sci 2021 Jul 1;22(13). Epub 2021 Jul 1.

Brain Health Research Centre, University of Otago, Dunedin 9054, New Zealand.

Oxytocin and vasopressin secretion from the posterior pituitary gland are required for normal pregnancy and lactation. Oxytocin secretion is relatively low and constant under basal conditions but becomes pulsatile during birth and lactation to stimulate episodic contraction of the uterus for delivery of the fetus and milk ejection during suckling. Vasopressin secretion is maintained in pregnancy and lactation despite reduced osmolality (the principal stimulus for vasopressin secretion) to increase water retention to cope with the cardiovascular demands of pregnancy and lactation. Read More

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Th2 Modulation of Transient Receptor Potential Channels: An Unmet Therapeutic Intervention for Atopic Dermatitis.

Front Immunol 2021 30;12:696784. Epub 2021 Jun 30.

School of Life Sciences, Henan University, Kaifeng, China.

Atopic dermatitis (AD) is a multifaceted, chronic relapsing inflammatory skin disease that affects people of all ages. It is characterized by chronic eczema, constant pruritus, and severe discomfort. AD often progresses from mild annoyance to intractable pruritic inflammatory lesions associated with exacerbated skin sensitivity. Read More

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The effects of neuronal cell differentiation on TRPM7, TRPM8 and TRPV1 channels in the model of Parkinson's disease.

Neurol Res 2021 Jul 14:1-14. Epub 2021 Jul 14.

Department of Biophysics, School of Medicine, Süleyman Demirel University, Isparta, Turkey.

Transient Receptor Potential Melastatin-like 7 (TRPM7), Transient Receptor Potential Melastatin-like 8 (TRPM8) and Transient Receptor Potential Vanilloid-like 1 (TRPV1) channels are expressed in neurological tissues such as brain cortex, dorsal root ganglion and hippocampal neurons and involved in several neurological diseases. The SH-SY5Y neuronal cell line is frequently used as a cellular model of neurodegenerative diseases including Parkinson's disease. The differentiated SH-SY5Y cells have much neuronal structure, function and exaggerated neuronal marker expression. Read More

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α2δ-1 Upregulation in Primary Sensory Neurons Promotes NMDA Receptor-Mediated Glutamatergic Input in Resiniferatoxin-Induced Neuropathy.

J Neurosci 2021 Jul 17;41(27):5963-5978. Epub 2021 Jun 17.

Center for Neuroscience and Pain Research, Department of Anesthesiology and Perioperative Medicine, University of Texas MD Anderson Cancer Center, Houston, Texas 77030

Systemic treatment with resiniferatoxin (RTX) induces small-fiber sensory neuropathy by damaging TRPV1-expressing primary sensory neurons and causes distinct thermal sensory impairment and tactile allodynia, which resemble the unique clinical features of postherpetic neuralgia. However, the synaptic plasticity associated with RTX-induced tactile allodynia remains unknown. In this study, we found that RTX-induced neuropathy is associated with α2δ-1 upregulation in the dorsal root ganglion (DRG) and increased physical interaction between α2δ-1 and GluN1 in the spinal cord synaptosomes. Read More

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TRP Channel Agonists Activate Different Afferent Neuromodulatory Mechanisms in Guinea Pig Urinary Bladder.

Front Physiol 2021 24;12:692719. Epub 2021 Jun 24.

Department of Urology, The Second Hospital, Cheeloo College of Medicine, Shandong University, Jinan, China.

Activation of TRP channels expressed in urinary bladder afferent nerves and urothelium releases neurotransmitters that influence bladder function. Experiments were undertaken to examine the mechanisms underlying effects of TRPA1 (allyl isothiocyanate, AITC), TRPV1 (capsaicin, CAPS), and TRPC (oleoyl-2-acetyl-sn-glycerol, OAG) agonists on guinea pig bladder activity. Effects of these agonists were compared with effects of nitro-oleic acid (OA-NO), an electrophilic nitro-fatty acid, known to activate TRPV1, TRPA1 or TRPC channels in sensory neurons. Read More

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De Novo Design of Peptidic Positive Allosteric Modulators Targeting TRPV1 with Analgesic Effects.

Adv Sci (Weinh) 2021 Jul 11:e2101716. Epub 2021 Jul 11.

Kidney Disease Center, First Affiliated Hospital and Department of Biophysics, Zhejiang University School of Medicine, Hangzhou, Zhejiang, 310058, China.

Transient receptor potential vanilloid 1 (TRPV1) ion channel is a nociceptor critically involved in pain sensation. Direct blockade of TRPV1 exhibits significant analgesic effects but also incurs severe side effects such as hyperthermia, causing failures of TRPV1 inhibitors in clinical trials. In order to selectively target TRPV1 channels that are actively involved in pain-sensing, peptidic positive allosteric modulators (PAMs) based on the high-resolution structure of the TRPV1 intracellular ankyrin-repeat like domain are de novo designed. Read More

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Population Coding of Capsaicin Concentration by Sensory Neurons Revealed Using Ca Imaging of Dorsal Root Ganglia Explants from Adult pirt-GCaMP3 Mouse.

Cell Physiol Biochem 2021 Jul;55(4):428-448

International Centre for Neurotherapeutics, Dublin City University, Glasnevin, Dublin, Ireland.

Background/aims: Nociceptors detect noxious capsaicin (CAPS) via the transient receptor potential vanilloid 1 (TRPV1) ion channel, but coding mechanisms for relaying CAPS concentration [CAPS] remain obscure. Prolonged (up to 1h.) exposure to CAPS is used clinically to desensitise sensory fibres for treatment of neuropathic pain, but its signalling has typically been studied in cultures of dissociated sensory neurons employing low cell numbers and very short exposure times. Read More

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Noopept Attenuates Diabetes-Mediated Neuropathic Pain and Oxidative Hippocampal Neurotoxicity via Inhibition of TRPV1 Channel in Rats.

Mol Neurobiol 2021 Jul 9. Epub 2021 Jul 9.

Department of Pathology, Faculty of Medicine, Inonu University, Malatya, Turkey.

Neuropathic pain and oxidative neurotoxicity are two adverse main actions of diabetes mellitus (DM). The expression levels of calcium ion (Ca) permeable TRPV1 channels are high in the dorsal root ganglion (DRGs) and hippocampus (HIPPO). TRPV1 is activated by capsaicin and reactive free oxygen radicals (fROS) to mediate peripheral neuropathy and neurotoxicity. Read More

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Heat-dependent opening of TRPV1 in the presence of capsaicin.

Nat Struct Mol Biol 2021 Jul 8;28(7):554-563. Epub 2021 Jul 8.

Department of Biochemistry, Duke University School of Medicine, Durham, NC, USA.

Transient receptor potential vanilloid member 1 (TRPV1) is a Ca-permeable cation channel that serves as the primary heat and capsaicin sensor in humans. Using cryo-EM, we have determined the structures of apo and capsaicin-bound full-length rat TRPV1 reconstituted into lipid nanodiscs over a range of temperatures. This has allowed us to visualize the noxious heat-induced opening of TRPV1 in the presence of capsaicin. Read More

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Distribution of Corneal TRPV1 and Its Association With Immune Cells During Homeostasis and Injury.

Invest Ophthalmol Vis Sci 2021 Jul;62(9)

Department of Optometry and Vision Sciences, University of Melbourne, Parkville, Australia.

Purpose: Given the role of corneal sensory nerves during epithelial wound repair, we sought to examine the relationship between immune cells and polymodal nociceptors following corneal injury.

Methods: Young C57BL/6J mice received a 2 mm corneal epithelial injury. One week later, corneal wholemounts were immunostained using β-tubulin-488, TRPV1 (transient receptor potential ion channel subfamily V member-1, a nonselective cation channel) and immune cell (MHC-II, CD45 and CD68) antibodies. Read More

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Molecular signaling of synthetic cannabinoids: Comparison of CB1 receptor and TRPV1 channel activation.

Eur J Pharmacol 2021 Jul 2;907:174301. Epub 2021 Jul 2.

Department of Pharmacology, Physiology, & Neuroscience, University of South Carolina, School of Medicine, Columbia, SC, USA. Electronic address:

Recreational use of synthetic cannabinoids (SCs) is associated with desirable euphoric and relaxation effects as well as adverse effects including anxiety, agitation and psychosis. These SC-mediated actions represent a combination of potentiated cannabinoid receptor signaling and "off-target" receptor activity. The goal of this study was to compare the efficacy of various classes of SCs in stimulating CB receptors and activating "off-target" transient receptor potential (TRP) channels. Read More

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Electroacupuncture Attenuates Chronic Inflammatory Pain and Depression Comorbidity through Transient Receptor Potential V1 in the Brain.

Am J Chin Med 2021 Jul 3:1-19. Epub 2021 Jul 3.

College of Chinese Medicine, Graduate Institute of Acupuncture Science, Taiwan.

Chronic pain is one of the highest costs in clinical therapy, often appearing comorbid with depression. They present with overlapping clinical conditions and common pathological pathways especially in neuroinflammation, both of which can be reversed by electroacupuncture (EA). Transient receptor potential V1 receptor (TRPV1) is a Ca[Formula: see text] permeable ion channel that responds to brain inflammation and has a known role in the development of chronic pain and depression. Read More

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Riboflavin Inhibits Histamine-Dependent Itch by Modulating Transient Receptor Potential Vanilloid 1 (TRPV1).

Front Mol Neurosci 2021 18;14:643483. Epub 2021 Jun 18.

Gachon Pain Center and Department of Physiology, College of Medicine, Gachon University, Incheon, South Korea.

Riboflavin, also known as vitamin B, isfound in foods and is used as a dietary supplement. Its deficiency (also called ariboflavinosis) results in some skin lesions and inflammations, such as stomatitis, cheilosis, oily scaly skin rashes, and itchy, watery eyes. Various therapeutic effects of riboflavin, such as anticancer, antioxidant, anti-inflammatory, and anti-nociceptive effects, are well known. Read More

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ASIC2 Synergizes with TRPV1 in the Mechano-Electrical Transduction of Arterial Baroreceptors.

Neurosci Bull 2021 Jul 2. Epub 2021 Jul 2.

Department of Neurobiology, School of Basic Medical Sciences, Beijing Key Laboratory of Neural Regeneration and Repair, Advanced Innovation Center for Human Brain Protection, Capital Medical University, Beijing, 100069, China.

Mechanosensitive ion channels (MSCs) are key molecules in the mechano-electrical transduction of arterial baroreceptors. Among them, acid-sensing ion channel 2 (ASIC2) and transient receptor potential vanilloid subfamily member 1 (TRPV1) have been studied extensively and documented to play important roles. In this study, experiments using aortic arch-aortic nerve preparations isolated from rats revealed that both ASIC2 and TRPV1 are functionally necessary, as blocking either abrogated nearly all pressure-dependent neural discharge. Read More

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TRPV1 Activation by Capsaicin Mediates Glucose Oxidation and ATP Production Independent of Insulin Signalling in Mouse Skeletal Muscle Cells.

Cells 2021 Jun 21;10(6). Epub 2021 Jun 21.

School of Health Sciences, College of Health and Medicine, University of Tasmania, Newnham Drive, Launceston, TAS 7248, Australia.

Background: Insulin resistance (IR), a key characteristic of type 2 diabetes (T2DM), is manifested by decreased insulin-stimulated glucose transport in target tissues. Emerging research has highlighted transient receptor potential cation channel subfamily V member (TRPV1) activation by capsaicin as a potential therapeutic target for these conditions. However, there are limited data on the effects of capsaicin on cell signalling molecules involved in glucose uptake. Read More

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TRPV1 Blocker HCRG21 Suppresses TNF-α Production and Prevents the Development of Edema and Hypersensitivity in Carrageenan-Induced Acute Local Inflammation.

Biomedicines 2021 Jun 23;9(7). Epub 2021 Jun 23.

G.B. Elyakov Pacific Institute of Bioorganic Chemistry, Far Eastern Branch, Russian Academy of Sciences, 159, Pr. 100 let Vladivostoku, 690022 Vladivostok, Russia.

Currently the TRPV1 (transient receptor potential vanilloid type 1) channel is considered to be one of the main targets for pro-inflammatory mediators including TNF-α. Similarly, the inhibition of TRPV1 activity in the peripheral nervous system affects pro-inflammatory mediator production and enhances analgesia in total. In this study, the analgesic and anti-inflammatory effects of HCRG21, the first peptide blocker of TRPV1, were demonstrated in a mice model of carrageenan-induced paw edema. Read More

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TRPV1 Hyperfunction Contributes to Renal Inflammation in Oxalate Nephropathy.

Int J Mol Sci 2021 Jun 8;22(12). Epub 2021 Jun 8.

School of Medicine, Fu Jen Catholic University, New Taipei 242062, Taiwan.

Inflammation worsens oxalate nephropathy by exacerbating tubular damage. The transient receptor potential vanilloid 1 (TRPV1) channel is present in kidney and has a polymodal sensing ability. Here, we tested whether TRPV1 plays a role in hyperoxaluria-induced renal inflammation. Read More

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TRPV1: Role in Skin and Skin Diseases and Potential Target for Improving Wound Healing.

Int J Mol Sci 2021 Jun 7;22(11). Epub 2021 Jun 7.

Department of Dermatology, School of Medicine, UC Davis, Sacramento, CA 95816, USA.

Skin is innervated by a multitude of sensory nerves that are important to the function of this barrier tissue in homeostasis and injury. The role of innervation and neuromediators has been previously reviewed so here we focus on the role of the transient receptor potential cation channel, subfamily V member 1 (TRPV1) in wound healing, with the intent of targeting it in treatment of non-healing wounds. TRPV1 structure and function as well as the outcomes of TRPV1-targeted therapies utilized in several diseases and tissues are summarized. Read More

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Advancement in research on the role of the transient receptor potential vanilloid channel in cerebral ischemic injury (Review).

Exp Ther Med 2021 Aug 15;22(2):881. Epub 2021 Jun 15.

School of Pharmacy and State Key Laboratory of Characteristic Chinese Medicine Resources in Southwest China, Chengdu University of Traditional Chinese Medicine, Chengdu, Sichuan 611137, P.R. China.

Stroke is a common critical disease occurring in middle-aged and elderly individuals, and is characterized by high morbidity, lethality and mortality. As such, it is of great concern to medical professionals. The aim of the present review was to investigate the effects of transient receptor potential vanilloid (TRPV) subtypes during cerebral ischemia in ischemia-reperfusion animal models, oxygen glucose deprivation and in other administration cell models to explore new avenues for stroke research and clinical treatments. Read More

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alleviated capsaicin-induced mechanical allodynia in a rat model through transient receptor potential vanilloid 1 modulation.

Korean J Pain 2021 Jul;34(3):262-270

Pharmacological and Diagnostic Research Center, Al-Ahliyya Amman University, Amman, Jordan.

Background: Transient receptor potential vanilloid 1 (TRPV1) is a non-selective cation channel implicated in pain sensation in response to heat, protons, and capsaicin (CAPS). It is well established that TRPV1 is involved in mechanical allodynia. This study investigates the effect of (Fabaceae) in CAPS-induced mechanical allodynia and its mechanism of action. Read More

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The design and synthesis of transient receptor potential vanilloid 3 inhibitors with novel skeleton.

Bioorg Chem 2021 Jun 21;114:105115. Epub 2021 Jun 21.

Department of Medicinal Chemistry, School of Pharmacy, Qingdao University Medical College, Qingdao University, Qingdao, Shandong, China. Electronic address:

Transient receptor potential vanilloid 3 (TRPV3) channel as a member of thermo TRPV subfamily is primarily expressed in the keratinocytes of the skin and sensory neurons, and plays critical roles in various physiological and pathological processes such as inflammation, pain sensation and skin disorders. However, TRPV3 studies have been challenging, in part due to a lack of research tools such as selective antagonists. Recently, we synthesized a series of cinnamate ester derivatives and evaluated their inhibitory activities on human TRPV3 channels expressed in HEK293 cells using whole-cell patch clamp recordings. Read More

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Alloxan as a better option than streptozotocin for studies involving painful diabetic neuropathy.

J Pharmacol Toxicol Methods 2021 Jun 25;112:107090. Epub 2021 Jun 25.

Departamento de Fisiologia, Instituto de Ciências Biomédicas, Universidade Federal de Uberlândia, Av. Pará, 1720, Uberlândia Zip Code 38405-320, Minas Gerais, Brazil. Electronic address:

Previous data indicate that the diabetogenic substance streptozotocin might act in nociceptive neurons changing the sensory signal, regardless of hyperglycemia. In the present article the effects of streptozotocin were compared with another diabetogenic drug, alloxan, for diabetes induction in rats. A possible direct effect of these drugs was tested by means of in vivo experiments and in vitro assays using cultured primary nociceptive neurons. Read More

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Screen of anti-migraine active compounds from Duijinsan by spectrum-effect relationship analysis and molecular docking.

J Ethnopharmacol 2021 Jun 20;279:114352. Epub 2021 Jun 20.

Tang Center of Herbal Medicine Research and Department of Anesthesia & Critical Care, University of Chicago, Chicago, IL, 60637, USA. Electronic address:

Ethnopharmacological Relevance: Duijinsan (DJS) is a famous Chinese medicine prescription composed of Radix scutellariae (RS) and Rhei Radix (RRR), which has been mainly used for treating migraine.

Aim Of The Study: This study aimed to uncover the anti-migraine active compounds from DJS and preliminary predicted the pharmacological mechanism by evaluating the spectrum-effect relationship between high-performance liquid chromatography (HPLC) fingerprints and anti-migraine effects of Duijinsan (DJS) extract combined with molecular docking.

Materials And Methods: HPLC and LC-MS were applied for chemical analyses of DJS extracts in different proportions. Read More

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Melatonin antagonizes ozone-exacerbated asthma by inhibiting the TRPV1 channel and stabilizing the Nrf2 pathway.

Environ Sci Pollut Res Int 2021 Jun 19. Epub 2021 Jun 19.

Brain Science and Advanced Technology Institute, School of Medicine, Wuhan University of Science and Technology, Wuhan, 430065, China.

Over the past few years, ozone has been identified as a potential risk factor for exacerbating asthma. However, few attempts have been made to prevent the progression of ozone-exacerbated asthma. This study investigated the attenuating effects of melatonin on ozone-aggravated allergic asthma, and explored the changes to the transient receptor potential vanilloid 1 (TRPV1)-nuclear factor erythroid-derived 2-related factor 2 (Nrf2) pathway associated with melatonin treatment. Read More

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The Impact of TRPV1 on Cancer Pathogenesis and Therapy: A Systematic Review.

Int J Biol Sci 2021 11;17(8):2034-2049. Epub 2021 May 11.

Guangdong Provincial Key Laboratory of Regional Immunity and Diseases, Shenzhen University International Cancer Center, Department of Cell Biology and Genetics, School of Medicine, College of Life Sciences and Oceanography, Shenzhen University, Shenzhen 518055, China.

The transient receptor potential cation channel subfamily V member 1 (TRPV1) is a transmembrane protein that can be activated by various physical and chemical stimuli and is associated with pain transduction. In recent years, TRPV1 was discovered to play essential roles in cancer tumorigenesis and development, as TRPV1 expression levels are altered in numerous cancer cell types. Several investigations have discovered direct associations between TRPV1 and cancer cell proliferation, cell death, and metastasis. Read More

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High-throughput screening of TRPV1 ligands in the light of the Bioluminescence Resonance Energy Transfer technique.

Mol Pharmacol 2021 Jun 14. Epub 2021 Jun 14.

IMS laboratory / CNRS UMR 5218, Bordeaux University, France

Ion channels are attractive drug targets for many therapeutic applications. However, high-throughput screening (HTS) of drug candidates is difficult and remains very expensive. We thus assessed the suitability of the Bioluminescence Resonance Energy Transfer (BRET) technique as a new HTS method for ion-channel studies by taking advantage of our recently characterized intra- and intermolecular BRET probes targeting the TRPV1 ion channel. Read More

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Activation of Transient Receptor Potential Ankyrin 1 and Vanilloid 1 Channels Promotes Odontogenic Differentiation of Human Dental Pulp Cells.

J Endod 2021 Jun 12. Epub 2021 Jun 12.

Department of Endodontics, College of Stomatology, Tianjin Medical University, Tianjin, China. Electronic address:

Introduction: Transient receptor potential ankyrin 1 (TRPA1) and vanilloid 1 (TRPV1) are thermosensitive channels that play an important role in thermal sensation or tooth pain by regulating intracellular Ca concentration that is essential for pulp tissue repair. The aim of this study was to evaluate the role of TRPA1 and TRPV1 channels in the odontogenic differentiation of human dental pulp cells (HDPCs).

Methods: HDPCs were isolated from healthy human intact third molars and cultured in odontogenic differentiation medium. Read More

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Capsaicin and Proton Differently Modulate Activation Kinetics of Mouse Transient Receptor Potential Vanilloid-1 Channel Induced by Depolarization.

Front Pharmacol 2021 20;12:672157. Epub 2021 May 20.

Division of Molecular Pharmacology and Cell Biophysics, Department of Disease Management Dentistry, Graduate School of Dentistry, Tohoku University, Sendai, Japan.

The transient receptor potential vanilloid type 1 (TRPV1) channel is a non-selective cation channel expressed with transient receptor potential ankyrin type 1 (TRPA1) in small and medial size neurons of the dorsal root ganglions and trigeminal ganglions. TRPV1 is activated by capsaicin, thermal stimuli higher than 43°C, mechanical stress, and protons (H). Although the TRPV1 channel does not have positively charged residues at regular intervals on its transmembrane segments, alterations in membrane potential also affect the state of TRPV1 channel. Read More

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Electroacupuncture reduces cold stress-induced pain through microglial inactivation and transient receptor potential V1 in mice.

Chin Med 2021 Jun 3;16(1):43. Epub 2021 Jun 3.

College of Chinese Medicine, Graduate Institute of Acupuncture Science, China Medical University, 91 Hsueh-Shih Road, Taichung, 40402, Taiwan.

Background: The treatment, and efficacy thereof, is considered to be inadequate with specificity to alleviation of Fibromyalgia and its associated pain. Fibromyalgia patients suffer from chronic and persistent widespread pain and generalized tenderness. Transient receptor potential V1 (TRPV1), which is reported as a Ca permeable ion channel that can be activated by inflammation, is reported to be involved in the development of fibromyalgia pain. Read More

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