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https://www.readbyqxmd.com/read/28934547/multifunctional-hybrid-compounds-derived-from-2-2-5-dioxopyrrolidin-1-yl-3-methoxypropanamides-with-anticonvulsant-and-antinociceptive-properties
#1
Michał Abram, Mirosław Zagaja, Szczepan Mogilski, Marta Andres-Mach, Gniewomir Latacz, Sebastian Baś, Jarogniew J Łuszczki, Katarzyna Kieć-Kononowicz, Krzysztof Kamiński
The focused set of new pyrrolidine-2,5-diones as potential broad-spectrum hybrid anticonvulsants was described. These derivatives integrate on the common structural scaffold the chemical fragments of well-known antiepileptic drugs such as ethosuximide, levetiracetam, and lacosamide. Such hybrids demonstrated effectiveness in two of the most widely used animal seizure models, namely, the maximal electroshock (MES) test and the psychomotor 6 Hz (32 mA) seizure model. Compound 33 showed the highest anticonvulsant activity in these models (ED50 MES = 79...
September 21, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28930174/capsaicin-supplementation-improved-risk-factors-of-coronary-heart-disease-in-individuals-with-low-hdl-c-levels
#2
Yu Qin, Li Ran, Jing Wang, Li Yu, He-Dong Lang, Xiao-Lan Wang, Man-Tian Mi, Jun-Dong Zhu
Low high-density lipoprotein cholesterol (HDL-C) is associated with an increased risk of coronary heart disease (CHD). This study aimed to evaluate the effects of capsaicin intervention on the serum lipid profile in adults with low HDL-C. In a randomized, double-blind, controlled clinical trial, 42 eligible subjects were randomly assigned to the capsaicin (n = 21, 4 mg of capsaicin daily) or to the control group (n = 21, 0.05 mg of capsaicin daily) and consumed two capsaicin or control capsules, which contained the powder of the skin of different peppers, twice daily for three months...
September 20, 2017: Nutrients
https://www.readbyqxmd.com/read/28924972/targeting-nociceptive-trp-channels-to-treat-chronic-pain-current-state-of-the-field
#3
REVIEW
Magdalene M Moran, Arpad Szallasi
Control of chronic pain is frequently inadequate and/or associated with intolerable adverse effects, prompting a frantic search for new therapeutics and new therapeutic targets. Nearly two decades of preclinical and clinical research supports the involvement of Transient Receptor Potential (TRP) channels in temperature perception, nociception and sensitization. Although there has been considerable excitement around the therapeutic potential of this channel family since the cloning and identification of TRPV1 as the capsaicin receptor more than 20 years ago, only modulators of a few channels have been tested clinically...
September 19, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28915983/single-treatment-with-capsaicin-8-patch-may-reduce-pain-and-sleep-interference-up-to-12-weeks-in-patients-with-painful-diabetic-peripheral-neuropathy
#4
Daniel A Ostrovsky
No abstract text is available yet for this article.
September 2017: Explore: the Journal of Science and Healing
https://www.readbyqxmd.com/read/28913979/physical-pain-increases-interpersonal-trust-in-females
#5
C Wang, J Gao, Y Ma, C Zhu, X-W Dong
BACKGROUND: People behave and interact with others differently when experiencing physical pain. Pain has dramatic effects on one's emotional responses, cognitive functions and social interaction. However, little has been known about whether and how physical pain influences interpersonal trust in social interaction. In the present study, we examined the influence of physical pain on trusting behaviour. METHODS: A total of 112 healthy participants were recruited and assigned to physical pain condition (induced by Capsaicin) and control condition (with hand cream), respectively...
September 14, 2017: European Journal of Pain: EJP
https://www.readbyqxmd.com/read/28902951/brachioradial-pruritus-and-notalgia-paraesthetica-a-comparative-observational-study-of-clinical-presentation-and-morphological-pathologies
#6
Manuel P Pereira, Hannah Lüling, Anette Dieckhöfer, Sabine Steinke, Claudia Zeidler, Sonja Ständer
Brachioradial pruritus (BRP) and notalgia paraesthetica (NP) represent 2 of the most common neuropathic itch syndromes. A total of 58 consecutive patients presenting at the Center for Chronic Pruritus, University Hospital Münster, were analysed with regard to clinical presentation, anatomical and morphological pathologies, impairment in quality of life, and response to treatment with topical capsaicin. Patients with BRP reported stinging and burning more often than those with NP. In the BRP group structural magnetic resonance imaging abnormalities more frequently correlated with localization of the symptoms compared with in patients with NP...
September 13, 2017: Acta Dermato-venereologica
https://www.readbyqxmd.com/read/28899508/pellitorine-an-extract-of-tetradium-daniellii-is-an-antagonist-of-the-ion-channel-trpv1
#7
Zoltán Oláh, Dóra Rédei, László Pecze, Csaba Vizler, Katalin Jósvay, Péter Forgó, Zoltán Winter, György Dombi, Gerda Szakonyi, Judit Hohmann
BACKGROUND: Transient Receptor Potential Vanilloid 1 (TRPV1) confers noxious heat and inflammatory pain signals in the peripheral nervous system. Clinical trial of resiniferatoxin from Euphorbia species is successfully aimed at TRPV1 in cancer pain management and heading toward new selective painkiller status that further validates this target for drug discovery efforts. Evodia species, used in traditional medicine for hundreds of years, are a recognised source of different TRPV1 agonists, but no antagonist has yet been reported...
October 15, 2017: Phytomedicine: International Journal of Phytotherapy and Phytopharmacology
https://www.readbyqxmd.com/read/28898491/skin-denervation-does-not-alter-cortical-potentials-to-surface-concentric-electrode-stimulation-a-comparison-with-laser-evoked-potentials-and-contact-heat-evoked-potentials
#8
S La Cesa, G Di Stefano, C Leone, A Pepe, E Galosi, F Alu, A Fasolino, G Cruccu, M Valeriani, A Truini
BACKGROUND: In the neurophysiological assessment of patients with neuropathic pain, laser evoked potentials (LEPs), contact heat evoked potentials (CHEPs) and the evoked potentials by the intraepidermal electrical stimulation via concentric needle electrode are widely agreed as nociceptive specific responses; conversely, the nociceptive specificity of evoked potentials by surface concentric electrode (SE-PREPs) is still debated. METHODS: In this neurophysiological study we aimed at verifying the nociceptive specificity of SE-PREPs...
September 12, 2017: European Journal of Pain: EJP
https://www.readbyqxmd.com/read/28890700/dietary-capsaicin-improves-glucose-homeostasis-and-alters-the-gut-microbiota-in-obese-diabetic-ob-ob-mice
#9
Jun-Xian Song, Hui Ren, Yuan-Feng Gao, Chong-You Lee, Su-Fang Li, Feng Zhang, Long Li, Hong Chen
Background: The effects of capsaicin on obesity and glucose homeostasis are still controversial and the mechanisms underlying these effects remain largely unknown. This study aimed to investigate the potential relationship between the regulation of obesity and glucose homeostasis by dietary capsaicin and the alterations of gut microbiota in obese diabetic ob/ob mice. Methods: The ob/ob mice were subjected to a normal, low-capsaicin (0.01%), or high-capsaicin (0.02%) diet for 6 weeks, respectively. Obesity phenotypes, glucose homeostasis, the gut microbiota structure and composition, short-chain fatty acids, gastrointestinal hormones, and pro-inflammatory cytokines were measured...
2017: Frontiers in Physiology
https://www.readbyqxmd.com/read/28884860/pharmacological-treatment-of-oro-facial-pain-health-technology-assessment-including-a-systematic-review-with-network-meta-analysis
#10
REVIEW
B Häggman-Henrikson, P Alstergren, T Davidson, E D Högestätt, P Östlund, S Tranaeus, S Vitols, T List
This health technology assessment evaluated the efficacy of pharmacological treatment in patients with oro-facial pain. Randomised controlled trials were included if they reported pharmacological treatment in patients ≥18 years with chronic (≥3 months) oro-facial pain. Patients were divided into subgroups: TMD-muscle [temporomandibular disorders (TMD) mainly associated with myalgia]; TMD-joint (TMD mainly associated with temporomandibular joint pain); and burning mouth syndrome (BMS). The primary outcome was pain intensity reduction after pharmacological treatment...
October 2017: Journal of Oral Rehabilitation
https://www.readbyqxmd.com/read/28879245/effects-of-high-dose-capsaicin-on-tmd-subjects-a-randomized-clinical-study
#11
B K Campbell, R B Fillingim, S Lee, R Brao, D D Price, J K Neubert
Temporomandibular joint disorder (TMD) is a complex musculoskeletal disorder that presents with pain, limited jaw opening, and abnormal noises in the temporomandibular joint. Despite the significant impact that TMD has in terms of suffering and financial burden, relatively few new treatments have emerged; therefore, development of novel treatments to treat TMD pain remains a high priority. The rationale of this study was to use a double-blind, vehicle-controlled clinical trial to evaluate the effects of a high-concentration (8%) capsaicin cream on TMD...
January 2017: JDR Clinical and Translational Research
https://www.readbyqxmd.com/read/28877968/action-potential-broadening-in-capsaicin-sensitive-drg-neurons-from-frequency-dependent-reduction-of-kv3-current
#12
Pin Liu, Nathaniel T Blair, Bruce P Bean
Action potential shape is a key determinant of cellular electrophysiological behavior. We found that in small-diameter capsaicin-sensitive dorsal root ganglia neurons corresponding to nociceptors (from rats of either sex), stimulation at frequencies as low as 1 Hz produced progressive broadening of the action potentials. Stimulation at 10 Hz for three seconds resulted in an increase in action potential width by an average of 76 ± 7% at 22 °C and by 38 ± 3% at 35 °C. Action potential clamp experiments showed that spike broadening results from frequency-dependent reduction of potassium current during spike repolarization...
September 6, 2017: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/28873562/fast-analysis-of-capsaicinoids-in-naga-jolokia-extracts-capsicum-chinense-by-high-performance-liquid-chromatography-using-fused-core-columns
#13
Tea Stipcovich, Gerardo F Barbero, Marta Ferreiro-González, Miguel Palma, Carmelo G Barroso
A rapid high-performance liquid chromatography method with a C18 reverse-phase fused-core column has been developed for the determination and quantification of the main capsaicinoids (nornordihydrocapsaicin, nordihydrocapsaicin, capsaicin, dihydrocapsaicin, homocapsaicin and homodihydrocapsaicin) present in Naga Jolokia peppers. A fused-core Kinetex™ C18 column (50×2.1mm i.d.; 2.6μm) was used for the analysis. The chromatographic separation was obtained with a gradient method in which the mobile phase was water (0...
January 15, 2018: Food Chemistry
https://www.readbyqxmd.com/read/28872473/capsaicin-8-patch-repeat-treatment-in-nondiabetic-peripheral-neuropathic-pain-a-52-week-open-label-single-arm-safety-study
#14
Rafael Gálvez, Marie-Louise Navez, Graeme Moyle, Christian Maihöfner, Malcolm Stoker, Etienne Ernault, Turo J Nurmikko, Nadine Attal
OBJECTIVES: To investigate the long-term safety and tolerability of capsaicin 8% patch repeat treatment in nondiabetic patients with peripheral neuropathic pain. METHODS: A prospective, open-label, observational study in patients with postherpetic neuralgia, posttraumatic or postsurgical nerve injury, HIV-associated distal sensory polyneuropathy, or other peripheral neuropathic pain, and average daily pain score ≥4, who received ≤6 capsaicin 8% patch treatments over 52 weeks according to clinical need (retreatment at 9 to 12 wk intervals)...
October 2017: Clinical Journal of Pain
https://www.readbyqxmd.com/read/28868961/serotonin-gated-inward-currents-are-three-times-more-frequent-in-rat-hairy-skin-sensory-afferents-than-in-those-innervating-the-skeletal-muscle
#15
Leonardo Fierro
Tight whole-cell patch clamp was performed in 191 DiI (1,1'-dioctadecyl-3,3,3'3'-tetramethylindocarbocyanine perchlorate) retrogradely labeled rat sensory afferents from skin shoulders ( n = 93) and biceps femoris muscles ( n = 98). 5-HT-gated inward currents were evoked with 50-µM serotonin (5-HT; 5-hydroxytryptamine), and their frequency and current densities were compared between skin and skeletal muscle sensory afferents. To evaluate if 5-HT-gated inward currents coexist with other ligand-gated currents, the skin and skeletal muscle sensory afferents were also sequentially exposed to external solution at pH 6...
January 2017: Molecular Pain
https://www.readbyqxmd.com/read/28867743/effects-of-capsaicin-coadministered-with-eicosapentaenoic-acid-on-obesity-related-dysregulation-in-high-fat-fed-mice
#16
Yoshihiko Hirotani, Junta Fukamachi, Rina Ueyama, Yoko Urashima, Kenji Ikeda
Obesity-induced inflammation contributes to the development of metabolic disorders such as insulin resistance, type 2 diabetes, fatty liver disease, and cardiovascular disease. In this study, we investigated whether the combination of eicosapentaenoic acid (EPA) and capsaicin could protect against high-fat diet (HFD)-induced obesity and related metabolic disorders. The experiments were performed using male C57BL/6J mice that were fed one of the following diets for 10 weeks: standard chow (5.3% fat content) (normal group), a HFD (32...
2017: Biological & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28867580/ethanol-potentiates-heat-response-in-the-carotid-artery-via-trpv1
#17
Seham Mustafa, Hishaam N Ismael
AIM: Ethanol is one of the most widely used recreational drugs in the world. At high concentrations, it can induce carotid artery vasoconstriction. Hyperthermia potentiates its effects resulting in carotid artery vasoconstriction at any concentration. The aim of this study is to investigate the interaction between ethanol and heating and to understand the underlying mechanisms leading to their synergistic effect. MATERIALS AND METHODS: Isometric tension of rabbit carotid artery ring segments suspended in organ baths filled with Krebs solution was recorded...
August 31, 2017: Life Sciences
https://www.readbyqxmd.com/read/28861768/capsaicin-protects-against-oxidative-insults-and-alleviates-behavioral-deficits-in-rats-with-6-ohda-induced-parkinson-s-disease-via-activation-of-trpv1
#18
ZhenXiang Zhao, JianFeng Wang, LingLing Wang, XiaoMei Yao, YiLin Liu, Ye Li, Si Chen, Tao Yue, XiaoTang Wang, WenFei Yu, YiMing Liu
Increasing evidence suggests that capsaicin may play a role in modulating neuronal function and controlling motor behavior. However, the underlying mechanism is still unclear and the activation of transient receptor potential vanilloid 1 (TRPV1) might be involved in. This study investigated the potential neuroprotective role of capsaicin in a rat model of 6-hydroxydopamine (6-OHDA)-induced Parkinson's disease (PD). Capsaicin was treated intraperitoneally for the 6-OHDA induced PD rats and the locomotor activity and abnormal involuntary movements were found alleviated...
August 31, 2017: Neurochemical Research
https://www.readbyqxmd.com/read/28856444/mechanisms-of-curcumin-induced-gastroprotection-against-ethanol-induced-gastric-mucosal-lesions
#19
Renata Czekaj, Jolanta Majka, Katarzyna Magierowska, Zbigniew Sliwowski, Marcin Magierowski, Robert Pajdo, Agata Ptak-Belowska, Marcin Surmiak, Slawomir Kwiecien, Tomasz Brzozowski
BACKGROUND: Curcumin, a pleiotropic substance used for centuries in traditional medicine, exhibits antioxidant, anti-inflammatory and antiproliferative efficacy against various tumours, but the role of curcumin in gastroprotection is little studied. We determined the effect of curcumin against gastric haemorrhagic lesions induced by 75% ethanol and alterations in gastric blood flow (GBF) in rats with cyclooxygenase-1 (COX-1) and COX-2 activity inhibited by indomethacin, SC-560 or rofecoxib, inhibited NO-synthase activity, capsaicin denervation and blockade of TRPV1 receptors by capsazepine...
August 30, 2017: Journal of Gastroenterology
https://www.readbyqxmd.com/read/28843204/toxicity-of-emerging-antifouling-biocides-to-non-target-freshwater-organisms-from-three-trophic-levels
#20
Isabel B Oliveira, Ksenia J Groh, Rene Schönenberger, Carlos Barroso, Kevin V Thomas, Marc J-F Suter
Antifouling (AF) systems provide the most cost-effective protection against biofouling. Several AF biocides have, however, caused deleterious effects in the environment. Subsequently, new compounds have emerged that claim to be more environment-friendly, but studies on their toxicity and environmental risk are necessary in order to ensure safety. This work aimed to assess the toxicity of three emerging AF biocides, tralopyril, triphenylborane pyridine (TPBP) and capsaicin, towards non-target freshwater organisms representing three trophic levels: algae (Chlamydomonas reinhardtii), crustacean (Daphnia magna) and fish (Danio rerio)...
August 1, 2017: Aquatic Toxicology
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