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https://www.readbyqxmd.com/read/28740604/identification-of-a-novel-trpm8-agonist-from-nutmeg-a-promising-cooling-compound
#1
Tomohiro Shirai, Kentaro Kumihashi, Mitsuyoshi Sakasai, Hiroshi Kusuoku, Yusuke Shibuya, Atsushi Ohuchi
The transient receptor potential melastatin 8 (TRPM8) ion channel is the primary receptor for innocuous cold stimuli (<28 °C) in humans. TRPM8 agonists such as l-(-)-menthol are widely used as flavors and additives to impart briskness, in addition to medicinal uses for inflammation and pain. Though various natural and synthetic agonists have been explored, only few natural compounds are known. We report herein the identification and characterization of the novel neolignan agonist erythro- and threo-Δ(8')-7-ethoxy-4-hydroxy-3,3',5'-trimethoxy-8-O-4'-neolignan (1) with an EC50 of 0...
July 13, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28732812/extracts-and-compounds-active-on-trp-ion-channels-from-waldheimia-glabra-a-ritual-medicinal-plant-from-himalaya
#2
Annamaria Giorgi, Angela Bassoli, Gigliola Borgonovo, Sara Panseri, Alessandra Manzo, Daniela Pentimalli, Aniello Schiano Moriello, Luciano De Petrocellis
BACKGROUND: Waldheimia glabra (Decne.) Regel is a wild plant from the Himalayan Mountains, commonly known as Smooth Ground Daisy. This plant is traditionally used by local populations in religious rituals (incense) or in traditional herbal medicine to treat skin diseases, headache, joint pain and fever. In literature few data are available on the investigation of this aromatic plant. PURPOSE: The present work aims at deepening knowledge about the chemical composition of W...
August 15, 2017: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
https://www.readbyqxmd.com/read/28713241/cold-temperature-encoding-by-cutaneous-trpa1-and-trpm8-carrying-fibers-in-the-mouse
#3
Zoltan Winter, Philipp Gruschwitz, Stephanie Eger, Filip Touska, Katharina Zimmermann
Previous research identified TRPM8 and TRPA1 cold transducers with separate functions, one being functional in the non-noxious range and the second one being a nociceptive transducer. TRPM8-deficient mice present overt deficits in the detection of environmental cool, but not a lack of cold avoidance and TRPA1-deficient mice show clear deficits in some cold nocifensive assays. The extent of TRPA1's contribution to cold sensing in vivo is still unclear, because mice lacking both TRPM8 and TRPA1 (DKO) were described with unchanged cold avoidance from TRPM8(-/-) based on a two-temperature-choice assay and by c-fos measurement...
2017: Frontiers in Molecular Neuroscience
https://www.readbyqxmd.com/read/28693898/nanosecond-pulsed-electric-fields-depolarize-transmembrane-potential-via-voltage-gated-k-ca-2-and-trpm8-channels-in-u87-glioblastoma-cells
#4
Ryan C Burke, Sylvia M Bardet, Lynn Carr, Sergii Romanenko, Delia Arnaud-Cormos, Philippe Leveque, Rodney P O'Connor
Nanosecond pulsed electric fields (nsPEFs) have a variety of applications in the biomedical and biotechnology industries. Cancer treatment has been at the forefront of investigations thus far as nsPEFs permeabilize cellular and intracellular membranes leading to apoptosis and necrosis. nsPEFs may also influence ion channel gating and have the potential to modulate cell physiology without poration of the membrane. This phenomenon was explored using live cell imaging and a sensitive fluorescent probe of transmembrane voltage in the human glioblastoma cell line, U87 MG, known to express a number of voltage-gated ion channels...
July 7, 2017: Biochimica et Biophysica Acta
https://www.readbyqxmd.com/read/28674258/roles-of-transient-receptor-potential-ankyrin-1-in-oxaliplatin-induced-peripheral-neuropathy
#5
Takayuki Nakagawa, Shuji Kaneko
Chemotherapy-induced peripheral neuropathy (CIPN), characterized by symptoms of paresthesia, dysesthesia, numbness, and pain, is a common adverse effect of several chemotherapeutic agents, including platinum-based agents, taxanes, and vinca alkaloids. However, no effective prevention or treatment strategies exist for CIPN because the mechanisms underpinning this neuropathy are poorly understood. Recent accumulating evidence suggests that some transient receptor potential (TRP) channels functioning as nociceptors in primary sensory neurons are responsible for CIPN...
2017: Biological & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28669932/cough-and-airway-disease-the-role-of-ion-channels
#6
REVIEW
Sara J Bonvini, Maria G Belvisi
Cough is the most common reason for patients to visit a primary care physician, yet it remains an unmet medical need. It can be idiopathic in nature but can also be a troublesome symptom across chronic lung diseases such as asthma, COPD and idiopathic pulmonary fibrosis (IPF). Chronic cough affects up to 12% of the population and yet there are no safe and effective therapies. The cough reflex is regulated by vagal, sensory afferent nerves which innervate the airway. The Transient Receptor Potential (TRP) family of ion channels are expressed on sensory nerve terminals, and when activated can evoke cough...
June 29, 2017: Pulmonary Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/28662813/discovery-and-development-of-a-novel-class-of-phenoxyacetyl-amides-as-highly-potent-trpm8-agonists-for-use-as-cooling-agents
#7
Alain Noncovich, Chad Priest, Jane Ung, Andrew P Patron, Guy Servant, Paul Brust, Nicole Servant, Nathan Faber, Hanghui Liu, Nicole S Gonsalves, Tanya L Ditschun
The paper presents the activity trends for a novel series of phenoxyacetyl amides as human TRPM8 receptor agonists. This series encompasses in vitro activity values ranging from the micromolar to the picomolar levels. Sensory evaluation of these molecules highlights their relevance as cooling agents for oral applications. The positive outcome of the complete evaluation of N-(1H-pyrazol-3-yl)-N-(thiophen-2-ylmethyl)-2-(p-tolyloxy)acetamide resulted in its approval for Generally Recognized As Safe (GRAS) status by the Flavor & Extract Manufacturer Association (FEMA) as FEMA 4809...
April 11, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28656459/involvement-of-thermosensitive-trp-channels-in-energy-metabolism
#8
REVIEW
Kunitoshi Uchida, Katsuya Dezaki, Takeshi Yoneshiro, Tatsuo Watanabe, Jun Yamazaki, Masayuki Saito, Toshihiko Yada, Makoto Tominaga, Yusaku Iwasaki
To date, 11 thermosensitive transient receptor potential (thermo-TRP) channels have been identified. Recent studies have characterized the mechanism of thermosensing by thermo-TRPs and the physiological role of thermo-TRPs in energy metabolism. In this review, we highlight the role of various thermo-TRPs in energy metabolism and hormone secretion. In the pancreas, TRPM2 and other TRPs regulate insulin secretion. TRPV2 expressed in brown adipocytes contributes to differentiation and/or thermogenesis. Sensory nerves that express TRPV1 promote increased energy expenditure by activating sympathetic nerves and adrenaline secretion...
September 2017: Journal of Physiological Sciences: JPS
https://www.readbyqxmd.com/read/28651550/a-novel-trpm8-agonist-relieves-dry-eye-discomfort
#9
Jee Myung Yang, Fengxian Li, Qin Liu, Marco Rüedi, Edward Tak Wei, Michael Lentsman, Hyo Seok Lee, Won Choi, Seong Jin Kim, Kyung Chul Yoon
BACKGROUND: Physical cooling of the eye surface relieves ocular discomfort, but translating this event to drug treatment of dry eye discomfort not been studied. Here, we synthesized a water-soluble TRPM8 receptor agonist called cryosim-3 (C3, 1-diisopropylphosphorylnonane) which selectively activates TRPM8 (linked to cooling) but not TRPV1 or TRPA1 (linked to nociception) and tested C3 in subjects with mild forms of dry eye disease. METHODS: A set of 1-dialkylphosphoryalkanes were tested for activation of TRPM8, TRPV1 and TRPA1 receptors in transfected cells...
June 26, 2017: BMC Ophthalmology
https://www.readbyqxmd.com/read/28631948/possible-contribution-of-pannexin-1-to-capsaicin-induced-atp-release-in-rat-nasal-columnar-epithelial-cells
#10
Toyoaki Ohbuchi, Ba Hung Do, Hiroki Koizumi, Shoko Takeuchi, Yoichi Ueta, Hideaki Suzuki
Current evidence indicates that transient receptor potential (TRP) channel activity involves a relationship between opening of pannexin-1 and release of ATP into the extracellular space. We examined the effects of agonists of thermosensitive TRP channels (TRPM8, TRPA1, TRPV1, and TRPV2) on ATP release from rat nasal mucosa, and measured ciliary beat frequency (CBF) using digital high-speed video imaging. Single-cell patch clamping from dissociated rat nasal columnar epithelial cells was performed to confirm the relationship between pannexin-1 and TRP...
February 10, 2017: Channels
https://www.readbyqxmd.com/read/28626113/effects-of-%C3%AE-estradiol-on-cold-sensitive-receptor-channel-trpm8-in-ovariectomized-rats
#11
Takuro Kubo, Shunichiro Tsuji, Tsukuru Amano, Fumi Yoshino, Yoko Niwa, Kyoko Kasahara, Saori Yoshida, Ken-Ichi Mukaisho, Hiroyuki Sugihara, Sachiko Tanaka, Fuminori Kimura, Kentaro Takahashi, Takashi Murakami
Transient receptor potential cation channel subfamily M member 8 (TRPM8) is associated with sensitivity to cold sensation in mammals. A previous study demonstrated that TRPM8 was overexpressed in the skin of ovariectomized (OVX) rats due to the loss of estrogen. In the present study, we investigated whether estrogen replacement restricts overexpression of the TRPM8 channel in the skin of OVX rats. We divided 15 Sprague Dawley rats into three groups: a non-operated group (NON-OPE), an ovariectomy group (OVX), and a group subjected to estrogen replacement during 4 weeks beginning 7 days after ovariectomy (OVX+E2)...
June 19, 2017: Experimental Animals
https://www.readbyqxmd.com/read/28603038/a-cross-species-translational-pharmacokinetic-pharmacodynamic-evaluation-of-core-body-temperature-reduction-by-the-trpm8-blocker-pf-05105679
#12
James R Gosset, Kevin Beaumont, Tomomi Matsuura, Wendy Winchester, Neil Attkins, Sophie Glatt, Ian Lightbown, Kristina Ulrich, Sonia Roberts, Jolie Harris, Emir Mesic, Tamara van Steeg, Diana Hijdra, Piet H van der Graaf
PF-05105679 is a moderately potent TRPM8 blocker which has been evaluated for the treatment of cold pain sensitivity. The TRPM8 channel is responsible for the sensation of cold environmental temperatures and has been implicated in regulation of core body temperature. Consequently, blockade of TRPM8 has been suggested to result in lowering of core body temperature. As part of the progression to human studies, the effect of PF-05105679 on core body temperature has been investigated in animals. Safety pharmacology studies showed that PF-05105679 reduced core body temperature in a manner that was inversely related to body weight of the species tested (greater exposure to PF-05105679 was required to lower temperature by 1°C in higher species)...
June 7, 2017: European Journal of Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28571526/trpa1-channels-mediate-hgf-response-to-phenytoin
#13
M J López-González, E Luis, O Fajardo, V Meseguer, K Gers-Barlag, S Niñerola, F Viana
Drug-induced gingival enlargement (GE) is a frequent adverse effect observed in patients treated with anticonvulsant, immunosuppressant, and some antihypertensive medications-the antiepileptic phenytoin being the main drug associated with GE due to its high incidence (around 50%). The molecular mechanisms behind drug-induced gingival overgrowth are still unknown. By reverse transcription polymerase chain reaction, we demonstrate that the calcium-permeable ion channels TRPA1, TRPV1, and its capsaicin-insensitive isoform TRPV1b are expressed in human gingival fibroblasts (HGFs), the most abundant cellular type in periodontal tissue...
March 1, 2017: Journal of Dental Research
https://www.readbyqxmd.com/read/28554243/functional-interactions-between-transient-receptor-potential-m8-and-transient-receptor-potential-v1-in-the-trigeminal-system-relevance-to-migraine-pathophysiology
#14
Yohei Kayama, Mamoru Shibata, Tsubasa Takizawa, Keiji Ibata, Toshihiko Shimizu, Taeko Ebine, Haruki Toriumi, Michisuke Yuzaki, Norihiro Suzuki
Background Recent genome-wide association studies have identified transient receptor potential M8 ( TRPM8) as a migraine susceptibility gene. TRPM8 is a nonselective cation channel that mediates cool perception. However, its precise role in migraine pathophysiology is elusive. Transient receptor potential V1 (TRPV1) is a nonselective cation channel activated by noxious heat. Both TRPM8 and TRPV1 are expressed in trigeminal ganglion (TG) neurons. Methods We investigated the functional roles of TRPM8 and TRPV1 in a meningeal inflammation-based migraine model by measuring the effects of facial TRPM8 activation on thermal allodynia and assessing receptor coexpression changes in TG neurons...
January 1, 2017: Cephalalgia: An International Journal of Headache
https://www.readbyqxmd.com/read/28550110/trpm8-inhibits-endothelial-cell-migration-via-a-non-channel-function-by-trapping-the-small-gtpase-rap1
#15
Tullio Genova, Guillaume P Grolez, Chiara Camillo, Michela Bernardini, Alexandre Bokhobza, Elodie Richard, Marco Scianna, Loic Lemonnier, Donatella Valdembri, Luca Munaron, Mark R Philips, Virginie Mattot, Guido Serini, Natalia Prevarskaya, Dimitra Gkika, Alessandra Fiorio Pla
Endothelial cell adhesion and migration are critical steps of the angiogenic process, whose dysfunction is associated with tumor growth and metastasis. The TRPM8 channel has recently been proposed to play a protective role in prostate cancer by impairing cell motility. However, the mechanisms by which it could influence vascular behavior are unknown. Here, we reveal a novel non-channel function for TRPM8 that unexpectedly acts as a Rap1 GTPase inhibitor, thereby inhibiting endothelial cell motility, independently of pore function...
July 3, 2017: Journal of Cell Biology
https://www.readbyqxmd.com/read/28499580/transient-receptor-potential-trp-channels-as-molecular-targets-in-lung-toxicology-and-associated-diseases
#16
REVIEW
Alexander Dietrich, Dirk Steinritz, Thomas Gudermann
The lungs as the gateways of our body to the external environment are essential for gas exchange. They are also exposed to toxicants from two sides, the airways and the vasculature. Apart from naturally produced toxic agents, millions of human made chemicals were produced since the beginning of the industrial revolution whose toxicity still needs to be determined. While the knowledge about toxic substances is increasing only slowly, a paradigm shift regarding the proposed mechanisms of toxicity at the plasma membrane emerged...
April 26, 2017: Cell Calcium
https://www.readbyqxmd.com/read/28499240/establishment-of-a-rat-model-of-chronic-prostatitis-chronic-pelvic-pain-syndrome-cp-cpps-induced-by-immunization-with-a-novel-peptide-t2
#17
Awais Ullah Ihsan, Farhan Ullah Khan, Waqas Nawaz, Muhammad Zahid Khan, Mengqi Yang, Xiaohui Zhou
BACKGROUND: The exact etiological mechanism of Chronic Prostatitis/chronic pelvic pain syndrome (CP/CPPS) is still unclear however autoimmunity is the most valid theory. We developed a rat model of Chronic Prostatitis/chronic pelvic pain syndrome by using a novel peptide (T2) isolated from TRPM8. This model might be beneficial in elucidating mechanisms involved in the pathogenesis of Chronic Prostatitis/Chronic Pelvic Pain Syndrome (CP/CPPS). METHODS: 40 male Sprague-Dawley rats with an average weight of 180-220g were equally distributed into five groups...
July 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28496415/inflammatory-effects-of-menthol-vs-non-menthol-cigarette-smoke-extract-on-human-lung-epithelial-cells-a-double-hit-on-trpm8-by-reactive-oxygen-species-and-menthol
#18
An-Hsuan Lin, Meng-Han Liu, Hsin-Kuo B Ko, Diahn-Warng Perng, Tzong-Shyuan Lee, Yu Ru Kou
Clinical studies suggest that smokers with chronic obstructive pulmonary disease who use menthol cigarettes may display more severe lung inflammation than those who smoke non-menthol cigarette. However, the mechanisms for this difference remain unclear. Menthol is a ligand of transient receptor potential melastatin-8 (TRPM8), a Ca(2+)-permeant channel sensitive to reactive oxygen species (ROS). We previously reported that exposure of human bronchial epithelial cells (HBECs) to non-menthol cigarette smoke extract (Non-M-CSE) triggers a cascade of inflammatory signaling leading to IL-8 induction...
2017: Frontiers in Physiology
https://www.readbyqxmd.com/read/28472061/sex-differences-in-mouse-transient-receptor-potential-cation-channel-subfamily-m-member-8-expressing-trigeminal-ganglion-neurons
#19
Robert M Caudle, Stephanie L Caudle, Alan C Jenkins, Andrew H Ahn, John K Neubert
The detection of cool temperatures is thought to be mediated by primary afferent neurons that express the cool temperature sensing protein Transient Receptor Potential Cation Channel, Subfamily M, Member 8 (TRPM8). Using mice, this study tested the hypothesis that sex differences in sensitivity to cool temperatures were mediated by differences in neurons that express TRPM8. Ion currents from TRPM8 expressing trigeminal ganglion (TRG) neurons in females demonstrated larger hyperpolarization-activated cyclic nucleotide-gated currents (Ih) than male neurons at both 30° and 18°C...
2017: PloS One
https://www.readbyqxmd.com/read/28440188/trp-channels-as-novel-targets-for-endogenous-ligands-focus-on-endocannabinoids-and-nociceptive-signalling
#20
Maksim V Storozhuk, Alexander V Zholos
The endocannabinoid system is gaining steadily increasing research interest as its important role in the regulation of many fundamental physiological processes becomes more and more evident. One area which received particularly significant attention concerns targeting the endocannabinoid system as a useful strategy in pain control, especially in refractory, difficult to treat cases of chronic pain. Apart from the classical targets of cannabinoids, the CB1 and CB2 receptors, several members of the large TRP family of Ca2+-permeable cation channels have been designated as "ionotropic cannabinoid receptors" to highlight their role in cannabinoid signalling...
April 24, 2017: Current Neuropharmacology
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