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capsaicin receptor

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https://www.readbyqxmd.com/read/28230360/capsaicin-reduces-blood-glucose-by-increasing-insulin-levels-and-glycogen-content-better-than-capsiate-in-streptozotocin-induced-diabetic-rats
#1
Shiqi Zhang, Xiaohan Ma, Zhang Lei, Hui Sun, Xiong Liu
Chili peppers exhibit anti-obesity, anti-cancer, anti-diabetic, and pain- and itchiness-relieving effects on animals and humans; these effects are due to capsaicin, which is the main pungent and biologically active component of pepper. Capsiate, a nonpungent capsaicin analogue and is similar to capsaicin in terms of structure and biological activity. In this study, we investigated whether capsaicin and capsiate exhibit the same hypoglycemic effects on rats with type 1 diabetes (T1D). Experimental rats were categorized into four groups: control, model, capsaicin, and capsiate groups...
February 23, 2017: Journal of Agricultural and Food Chemistry
https://www.readbyqxmd.com/read/28225806/capsaicin-reduces-alzheimer-associated-tau-changes-in-the-hippocampus-of-type-2-diabetes-rats
#2
Weijie Xu, Juanhong Liu, Delin Ma, Gang Yuan, Yan Lu, Yan Yang
Type 2 diabetes (T2D) is a high-risk factor for Alzheimer's disease (AD) due to impaired insulin signaling pathway in brain. Capsaicin is a specific transient receptor potential vanilloid 1 (TRPV1) agonist which was proved to ameliorate insulin resistance. In this study, we investigated whether dietary capsaicin could reduce the risk of AD in T2D. T2D rats were fed with capsaicin-containing high fat (HF) diet for 10 consecutive days (T2D+CAP). Pair-fed T2D rats (T2D+PF) fed with the HF-diet of average dose of T2D+CAP group were included to control for the effects of reduced food intake and body weight...
2017: PloS One
https://www.readbyqxmd.com/read/28225032/4-isopropylcyclohexanol-has-potential-analgesic-effects-through-the-inhibition-of-anoctamin-1-trpv1-and-trpa1-channel-activities
#3
Yasunori Takayama, Hidemasa Furue, Makoto Tominaga
Interactions between calcium-activated chloride channel anoctamin 1 (ANO1) and transient receptor potential vanilloid 1 (TRPV1) enhance pain sensations in mice, suggesting that ANO1 inhibition could have analgesic effects. Here we show that menthol and the menthol analogue isopropylcyclohexane (iPr-CyH) inhibited ANO1 channels in mice. The iPr-CyH derivative 4-isopropylcyclohexanol (4-iPr-CyH-OH) inhibited mouse ANO1 currents more potently than iPr-CyH. Moreover, 4-iPr-CyH-OH inhibited the activities of TRPV1, TRP ankyrin 1 (TRPA1), TRP melastatin 8 (TRPM8) and TRPV4...
February 22, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28214687/gastroprotective-effect-and-mechanism-of-action-of-croton-rhamnifolioides-essential-oil-in-mice
#4
Cinara Soares Vidal, Anita Oliveira Brito Pereira Bezerra Martins, Andressa de Alencar Silva, Maria Rayane Correia de Oliveira, Jaime Ribeiro-Filho, Thaís Rodrigues de Albuquerque, Henrique Douglas Melo Coutinho, Jackson Roberto Guedes da Silva Almeida, Lucindo Jose Quintans, Irwin Rose Alencar de Menezes
BACKGROUND: Croton rhamnifolioides Pax is a plant species that have been used in the folk medicine to treat ulcers, inflammations and hypertension. However, despite the relevant data obtained from ethnopharmacological studies, the pharmacological properties endorsing the efficacy of this plant to treat ulcer remain to be elucidated. HYPOTHESIS/PURPOSE: The present study aimed to characterize the chemical profile and evaluate the gastroprotective activity of the essential oil obtained from C...
February 16, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28213106/oral-treatment-with-essential-oil-of-hyptis-spicigera-lam-lamiaceae-reduces-acute-pain-and-inflammation-in-mice-potential-interactions-with-transient-receptor-potential-trp-ion-channels
#5
Róli Rodrigues Simões, Igor Dos Santos Coelho, Stella Célio Junqueira, Glauce Regina Pigatto, Marcos José Salvador, Adair Roberto Soares Santos, Felipe Meira de Faria
ETHNOPHARMACOLOGICAL RELEVANCE: The genus Hyptis comprehends almost 400 species widespread in tropical and temperate regions of America. The use of Hyptis spicigera Lam. (Lamiaceae) is reported in traditional medicine due to its gastroprotective, anti-inflammatory and analgesic properties. AIM OF THE STUDY: The rationale of this study was to investigate the potential use of the essential oil of H. spicigera (EOHs) as analgesic. MATERIAL AND METHODS: The antinociceptive effect of EOHs was verified analyzing acute nocifensive behavior of mice induced by chemical noxious stimuli [i...
February 14, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28210904/acute-and-neuropathic-orofacial-antinociceptive-effect-of-eucalyptol
#6
José de Maria de Albuquerque de Melo Júnior, Marina de Barros Mamede Vidal Damasceno, Sacha Aubrey Alves Rodrigues Santos, Talita Matias Barbosa, João Ronielly Campêlo Araújo, Antonio Eufrásio Vieira-Neto, Deysi Viviana Tenazoa Wong, Roberto César Pereira Lima-Júnior, Adriana Rolim Campos
Terpenes have a wide range of pharmacological properties, including antinociceptive action. The anti-inflammatory and antinociceptive effects of eucalyptol are well established. The purpose of this study was to evaluate the antinociceptive effect of eucalyptol on acute and neuropathic orofacial pain in rodent models. Acute orofacial and corneal nociception was induced with formalin, capsaicin, glutamate and hypertonic saline in mice. In another series, animals were pretreated with capsazepine or ruthenium red to evaluate the involvement of TRPV1 receptors in the effect of eucalyptol...
February 16, 2017: Inflammopharmacology
https://www.readbyqxmd.com/read/28205139/the-potentiating-effect-of-calcitonin-gene-related-peptide-on-transient-receptor-potential-vanilloid-1-activity-and-the-electrophysiological-responses-of-rat-trigeminal-neurons-to-nociceptive-stimuli
#7
Duangthip Chatchaisak, Mark Connor, Anan Srikiatkhachorn, Banthit Chetsawang
Growing evidence suggests that calcitonin gene-related peptide (CGRP) participates in trigeminal nociceptive responses. However, the role of CGRP in sensitization or desensitization of nociceptive transduction remains poorly understood. In this study, we sought to further investigate the CGRP-induced up-regulation of transient receptor potential vanilloid-1 (TRPV1) and the responses of trigeminal neurons to nociceptive stimuli. Rat trigeminal ganglion (TG) organ cultures and isolated trigeminal neurons were incubated with CGRP...
February 15, 2017: Journal of Physiological Sciences: JPS
https://www.readbyqxmd.com/read/28196712/ipomoea-pes-caprae-l-r-br-convolvulaceae-as-a-topical-herbal-medicine-to-relieve-pain-and-inflammation-promising-tool-against-effects-due-to-toxin-skin-contact
#8
Cristiane da Silva Barth, Hugo Guilherme Tolentino de Souza, Lilian W Rocha, Gislaine Francieli da Silva, Mariana Ferreira Dos Anjos, Veronica D'Avila Pastor, Tania Mari Belle Bresolin, Angelica Garcia Couto, José Roberto Santin, Nara Lins Meira Quintão
ETHNOPHARMACOLOGICAL RELEVANCE: Ipomoea pes-caprae is known as bayhops, beach morning glory or goat's foot, and in Brazil as salsa-de-praia. Its leaves are used in worldwide folk medicine for the relief of jellyfish-stings symptoms. The literature only reports the anti-inflammatory and neutralizing effects of a nonpolar plant derived, without validating the popular use or exploring the mechanism of action. AIM OF THE STUDY: This study aimed to evaluate and validate the topical effects of a semisolid containing hydroethanolic extract obtained from the aerial parts of I...
February 11, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28195064/catecholamines-reduce-transient-receptor-potential-vanilloid-type-1-desensitization-in-cultured-dorsal-root-ganglia-neurons
#9
A Filippi, C Caruntu, R O Gheorghe, A Deftu, B Amuzescu, V Ristoiu
Sympathetic nervous system and adrenergic receptors are involved in the modulation of dorsal root ganglia neuronal activity, with TRPV1 receptor as an important downstream effector. It is already known that adrenergic sensitization of TRPV1 receptors or catecholamine-induced TRPV1 upregulation are involved in increased excitability and pain via mainly α1 adrenergic receptors, but it is not known if reduced TRPV1 desensitization is involved in this process, as well. Therefore, the aims of this study were to evaluate the effects of epinephrine and norepinephrine on TRPV1 desensitization induced by repeated applications of capsaicin and to assess what would be the involvement of the major α1, α2 and β adrenergic receptor subtypes...
December 2016: Journal of Physiology and Pharmacology: An Official Journal of the Polish Physiological Society
https://www.readbyqxmd.com/read/28188777/enhanced-ability-of-trpv1-channels-in-regulating-glutamatergic-transmission-after-repeated-morphine-exposure-in-the-nucleus-accumbens-of-rat
#10
Haitao Zhang, Dong Jia, Yuan Wang, Liang Qu, Xuelian Wang, Jian Song, Lijun Heng, Guodong Gao
Glutamatergic projections to nucleus accumbens (NAc) drive drug-seeking behaviors during opioids withdrawal. Modulating glutamatergic neurotransmission provides a novel pharmacotherapeutic avenue for treatment of opioids dependence. Great deals of researches have verified that transient receptor potential vanilloid 1 (TRPV1) channels alters synaptic transmitter release and regulate neural plasticity. In the present study, whole-cell patch clamp recordings were adopted to examine the activity of TRPV1 Channels in regulating glutamate-mediated excitatory postsynaptic currents (EPSCs) in NAc of rat during morphine withdrawal for 3 days and 3 weeks...
February 7, 2017: Brain Research
https://www.readbyqxmd.com/read/28182310/ankyrin-rich-membrane-spanning-protein-as-a-novel-modulator-of-transient-receptor-potential-vanilloid-1-function-in-nociceptive-neurons
#11
J Peter, C Kasper, M Kaufholz, R Buschow, J Isensee, T Hucho, F W Herberg, F Schwede, C Stein, S-E Jordt, M Brackmann, V Spahn
BACKGROUND: The ion channel TRPV1 is mainly expressed in small diameter dorsal root ganglion (DRG) neurons, which are involved in the sensation of acute noxious thermal and chemical stimuli. Direct modifications of the channel by diverse signalling events have been intensively investigated, but little is known about the composition of modulating macromolecular TRPV1 signalling complexes. Here, we hypothesize that the novel adaptor protein ankyrin-rich membrane spanning protein/kinase D interacting substrate (ARMS) interacts with TRPV1 and modulates its function in rodent DRG neurons...
February 9, 2017: European Journal of Pain: EJP
https://www.readbyqxmd.com/read/28177520/broad-spectrum-efficacy-with-ly2969822-an-oral-prodrug-of-metabotropic-glutamate-2-3-mglu2-3-receptor-agonist-ly2934747-in-rodent-pain-models
#12
Michael P Johnson, Mark A Muhlhauser, Eric S Nisenbaum, Rosa M A Simmons, Beth M Forster, Kelly L Knopp, Lijuan Yang, Denise Morrow, Dominic L Li, Jeffrey D Kennedy, Steven Swanson, James A Monn
BACKGROUND AND PURPOSE: A body of evidence suggests activation of metabotropic glutamate 2/3 (mGlu2/3 ) receptors would be an effective analgesic in chronic pain conditions. Thus, the analgesic properties of a novel mGlu2/3 receptor agonist prodrug were investigated. EXPERIMENTAL APPROACH: After oral absorption, the prodrug LY2969822 rapidly converts to the brain penetrant, potent, and subtype-selective mGlu2/3 receptor agonist LY2934747. Behavioral assessments of allodynia, hyperalgesia, or nocifensive behaviors in preclinical pain models were determined after administration of LY2969822 of 0...
February 8, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28154330/analgesic-effects-and-side-effects-of-ephedra-herb-extract-and-ephedrine-alkaloids-free-ephedra-herb-extract
#13
Yoshinori Kobayashi
 Ephedra Herb is classified "pungent, slightly bitter, and warm" in tastes and natures, and is used to provide warmth to the body, dispel coldness, remove dampness, and reduce pain. Similar herbs are "pungent and hot" chili peppers, "pungent and hot" evodia fruit," "pungent and warm" ginger, "pungent and hot" processed ginger, "pungent and hot" Zanthoxylum fruit, etc. These herbs are prescribed to provide heat to the outer or inner body. Some pungent components such as capsaicin, evodiamine, gingerol, and shogaol are known to be activators of transient receptor potential vanilloid 1 (TRPV1)...
2017: Yakugaku Zasshi: Journal of the Pharmaceutical Society of Japan
https://www.readbyqxmd.com/read/28153725/differences-in-the-effects-of-four-trpv1-channel-antagonists-on-lipopolysaccharide-induced-cytokine-production-and-cox-2-expression-in-murine-macrophages
#14
Yuki Ninomiya, Sei-Ichi Tanuma, Mitsutoshi Tsukimoto
Sepsis is a systemic inflammatory response syndrome triggered by lipopolysaccharide (LPS), an outer membrane component of gram-negative bacteria, and cytokine production via LPS-induced macrophage activation is deeply involved in its pathogenesis. Effective therapy of sepsis has not yet been established. However, it was reported that transient receptor potential vanilloid 1 (TRPV1) channel antagonist capsazepine (CPZ; a capsaicin analogue) attenuates sepsis in a murine model [Ang et al., PLoS ONE 6(9) (2011) e24535; J...
March 11, 2017: Biochemical and Biophysical Research Communications
https://www.readbyqxmd.com/read/28141955/investigational-new-drugs-for-allergic-rhinitis
#15
Peter A Ricketti, Sultan Alandijani, Chen Hsing Lin, Thomas B Casale
Allergic rhinitis (AR) is a multifactorial disease characterized by paroxysmal symptoms of sneezing, rhinorrhea, postnasal drip and nasal congestion. For over a century, subcutaneous allergen immunotherapy (SCIT) has been recognized as the most effective therapy to date that may modify the underlying disease course and provide long-term benefits for individuals refractory to pharmacotherapy. However, over the past 25 years, there has been substantial growth in developing alternative therapies to traditional SCIT...
January 31, 2017: Expert Opinion on Investigational Drugs
https://www.readbyqxmd.com/read/28133727/diet-induced-obesity-enhances-trpv1-mediated-neurovascular-reactions-in-the-dura-mater
#16
Balázs Marics, Barna Peitl, Kitti Pázmándi, Attila Bácsi, József Németh, Orsolya Oszlács, Gábor Jancsó, Mária Dux
OBJECTIVE: Exploring the pathophysiological changes in transient receptor potential vanilloid 1 (TRPV1) receptor of the trigeminovascular system in high-fat, high-sucrose (HFHS) diet-induced obesity of experimental animals. BACKGROUND: Clinical and experimental observations suggest a link between obesity and migraine. Accumulating evidence indicates that metabolic and immunological alterations associated with obesity may potentially modulate trigeminovascular functions...
January 30, 2017: Headache
https://www.readbyqxmd.com/read/28123347/forsythoside-a-exerts-antipyretic-effect-on-yeast-induced-pyrexia-mice-via-inhibiting-transient-receptor-potential-vanilloid-1-function
#17
Cuiling Liu, Hongchang Su, Hongye Wan, Qingxia Qin, Xuan Wu, Xiangying Kong, Na Lin
Transient receptor potential vanilloid 1 (TRPV1) is a non-selective cation channel gated by noxious heat, playing major roles in thermoregulation. Forsythoside A (FT-A) is the most abundant phenylethanoid glycosides in Fructus Forsythiae, which has been prescribed as a medicinal herb for treating fever in China for a long history. However, how FT-A affects pyrexia and what is the underlying molecular mechanism remain largely unknown. Here we found that FT-A exerted apparent antipyretic effect through decreasing the levels of prostaglandin E2 (PGE2) and interleukin 8 (IL-8) in a dose-dependent fashion on the yeast induced pyrexia mice...
2017: International Journal of Biological Sciences
https://www.readbyqxmd.com/read/28120884/phosphorylated-histone-3-at-serine-10-identifies-activated-spinal-neurons-and-contributes-to-the-development-of-tissue-injury-associated-pain
#18
Jose Vicente Torres-Pérez, Péter Sántha, Angelika Varga, Peter Szucs, Joao Sousa-Valente, Botond Gaal, Miklós Sivadó, Anna P Andreou, Sara Beattie, Bence Nagy, Klara Matesz, J Simon C Arthur, Gábor Jancsó, Istvan Nagy
Transcriptional changes in superficial spinal dorsal horn neurons (SSDHN) are essential in the development and maintenance of prolonged pain. Epigenetic mechanisms including post-translational modifications in histones are pivotal in regulating transcription. Here, we report that phosphorylation of serine 10 (S10) in histone 3 (H3) specifically occurs in a group of rat SSDHN following the activation of nociceptive primary sensory neurons by burn injury, capsaicin application or sustained electrical activation of nociceptive primary sensory nerve fibres...
January 25, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28118665/functional-properties-of-sensory-nerve-terminals-of-the-mouse-cornea
#19
Omar González-González, Federico Bech, Juana Gallar, Jesús Merayo-Lloves, Carlos Belmonte
Purpose: To define the firing properties of sensory nerve terminals innervating the adult mouse cornea in response to external stimuli of differing modality. Methods: Extracellular electrical activity of single corneal sensory nerve terminals was recorded in excised eyes of C57BL/6J mice. Eyes were placed in a recording chamber and were continuously superfused with warm saline solution. Nerve terminal impulse (NTI) activity was recorded by means of a glass pipette (tip ∼ 50 μm), applied on the corneal surface...
January 1, 2017: Investigative Ophthalmology & Visual Science
https://www.readbyqxmd.com/read/28115552/xenin-augments-duodenal-anion-secretion-via-activation-of-afferent-neural-pathways
#20
Izumi Kaji, Yasutada Akiba, Ikuo Kato, Koji Maruta, Atsukazu Kuwahara, Jonathan D Kaunitz
Xenin-25, a neurotensin (NT)-related anorexigenic gut hormone generated mostly in the duodenal mucosa, is believed to increase the rate of duodenal ion secretion, since xenin-induced diarrhea is not present after Roux-en-Y gastric bypass surgery. Since the local effects of xenin on duodenal ion secretion have remained uninvestigated, we thus examined the neural pathways underlying xenin-induced duodenal anion secretion. Intravenous infusion of xenin-8, a bioactive C-terminal fragment of xenin-25, dose-dependently increased the rate of duodenal HCO3- secretion in perfused duodenal loops of anesthetized rats...
January 23, 2017: Journal of Pharmacology and Experimental Therapeutics
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