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transient receptor vanilloid 1

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https://www.readbyqxmd.com/read/29163050/mechanisms-of-cisplatin-induced-ototoxicity-and-otoprotection
#1
REVIEW
Sandeep Sheth, Debashree Mukherjea, Leonard P Rybak, Vickram Ramkumar
Evidence of significant hearing loss during the early days of use of cisplatin as a chemotherapeutic agent in cancer patients has stimulated research into the causes and treatment of this side effect. It has generally been accepted that hearing loss is produced by excessive generation of reactive oxygen species (ROS) in cell of the cochlea, which led to the development of various antioxidants as otoprotective agents. Later studies show that ROS could stimulate cochlear inflammation, suggesting the use of anti-inflammatory agents for treatment of hearing loss...
2017: Frontiers in Cellular Neuroscience
https://www.readbyqxmd.com/read/29159769/diversity-effect-of-capsaicin-on-different-types-of-skeletal-muscle
#2
Gan Zhou, Lina Wang, Yaqiong Xu, Kelin Yang, Lv Luo, Leshan Wang, Yongxiang Li, Jiawen Wang, Gang Shu, Songbo Wang, Ping Gao, Xiaotong Zhu, Qianyun Xi, Jiajie Sun, Yongliang Zhang, Qingyan Jiang
Capsaicin is a major pungent content in green and red peppers which are widely used as spice, and capsaicin may activate different receptors. To determine whether capsaicin has different effects on different types of skeletal muscle, we applied different concentrations (0, 0.01, and 0.02%) of capsaicin in the normal diet and conducted a four-week experiment on Sprague-Dawley rats. The fiber type composition, glucose metabolism enzyme activity, and different signaling molecules' expressions of receptors were detected...
November 20, 2017: Molecular and Cellular Biochemistry
https://www.readbyqxmd.com/read/29138447/the-semaphorin-3a-inhibitor-sm-345431-preserves-corneal-nerve-and-epithelial-integrity-in-a-murine-dry-eye-model
#3
Risa Yamazaki, Katsuya Yamazoe, Satoru Yoshida, Shin Hatou, Emi Inagaki, Hideyuki Okano, Kazuo Tsubota, Shigeto Shimmura
Dry eye disease (DED) is a common disorder causing discomfort and ocular fatigue. Corneal nerves are compromised in DED, which may further cause loss of corneal sensation and decreased tear secretion. Semaphorin 3A (Sema3A) is expressed by the corneal epithelium under stress, and is known as an inhibitor of axonal regeneration. Using a murine dry eye model, we found that topical SM-345431, a selective Sema3A inhibitor, preserved corneal sensitivity (2.3 ± 0.3 mm versus 1.4 ± 0.1 mm in vehicle control, p = 0...
November 14, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29137713/trpv1-a-potential-therapeutic-target-in-type-2-diabetes-and-comorbidities
#4
REVIEW
Dorte X Gram, Jens J Holst, Arpad Szallasi
With an estimated 422 million affected patients worldwide in 2016, type 2 diabetes (T2D) has reached pandemic proportions and represents a major unmet medical need. T2D is a polygenic disease with a chronic, low-grade inflammatory component. Second-generation transient receptor potential vanilloid-1 (TRPV1) antagonists are potent anti-inflammatory agents with proven clinical safety. In rodent models of T2D, TRPV1 blockade was shown to halt disease progression and improve glucose metabolism. Thus, we propose that TRPV1 antagonists merit further study as novel therapeutic approaches to potentially treat T2D and its comorbidities...
November 2017: Trends in Molecular Medicine
https://www.readbyqxmd.com/read/29134561/cannabinoid-receptor-type-1-agonist-acea-protects-neurons-from-death-and-attenuates-endoplasmic-reticulum-stress-related-apoptotic-pathway-signaling
#5
Talita A Vrechi, Fernanda Crunfli, Andressa P Costa, Andréa S Torrão
Neurodegeneration is the result of progressive destruction of neurons in the central nervous system, with unknown causes and pathological mechanisms not yet fully elucidated. Several factors contribute to neurodegenerative processes, including neuroinflammation, accumulation of neurotoxic factors, and misfolded proteins in the lumen of the endoplasmic reticulum (ER). Endocannabinoid signaling has been pointed out as an important modulatory system in several neurodegeneration-related processes, inhibiting the inflammatory response and increasing neuronal survival...
November 13, 2017: Neurotoxicity Research
https://www.readbyqxmd.com/read/29132924/impact-of-capsaicin-an-active-component-of-chili-pepper-on-pathogenic-chlamydial-growth-chlamydia-trachomatis-and-chlamydia-pneumoniae-in-immortal-human-epithelial-hela-cells
#6
Kazuya Yamakawa, Junji Matsuo, Torahiko Okubo, Shinji Nakamura, Hiroyuki Yamaguchi
Chlamydia trachomatis is the leading cause of sexually transmitted infections worldwide. Capsaicin, a component of chili pepper, which can stimulate actin remodeling via capsaicin receptor TRPV1 (transient receptor potential vanilloid 1) and anti-inflammatory effects via PPARγ (peroxisome proliferator-activated receptor-γ) and LXRα (liver X receptor α), is a potential candidate to control chlamydial growth in host cells. We examined whether capsaicin could inhibit C. trachomatis growth in immortal human epithelial HeLa cells...
November 10, 2017: Journal of Infection and Chemotherapy: Official Journal of the Japan Society of Chemotherapy
https://www.readbyqxmd.com/read/29132095/inhibition-of-tnf-reduces-mechanical-orofacial-hyperalgesia-induced-by-complete-freund-s-adjuvant-by-a-trpv1-dependent-mechanism-in-mice
#7
Krzysztof Lis, Tomasz Grygorowicz, Agnieszka Cudna, David E Szymkowski, Ewa Bałkowiec-Iskra
BACKGROUND: Inflammation in the orofacial region results in pain and is associated with many pathological states, including migraine, neuralgias and temporomandibular disorder. Although extensively studied, the mechanisms responsible for these conditions are not known and effective treatments are lacking. We reported earlier that the proinflammatory cytokine tumor necrosis factor (TNF) plays an important role in regulation of trigeminal ganglion (TG) neuron function in vitro. In the present study we investigated the role of TNF in mechanical hypersensitivity in mice...
June 3, 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/29125703/pharmacokinetics-and-safety-of-mavatrep-jnj-39439335-a-trpv1-antagonist-in-healthy-japanese-and-caucasian-men-a-double-blind-randomized-placebo-controlled-sequential-group-phase-1-study
#8
Prasarn Manitpisitkul, Kevin Shalayda, Lucille Russell, Panna Sanga, Bhavna Solanki, Joseph Caruso, Yuki Iwaki, John A Moyer
This single-center, double-blind, placebo-controlled, sequential-group phase 1 study evaluated the safety, tolerability, and pharmacokinetics (PK) of mavatrep (JNJ-39439335), a transient receptor potential vanilloid 1 antagonist, in healthy Japanese and caucasian subjects. In part 1, a single-ascending-dose study, 50 subjects (25 each healthy Japanese and caucasians) were enrolled and received a single oral dose of 10, 25, or 50 mg mavatrep. Caucasian subjects were matched to Japanese subjects with respect to age (±5 years) and body mass index (±5 kg/m(2) )...
November 10, 2017: Clinical Pharmacology in Drug Development
https://www.readbyqxmd.com/read/29125700/bioavailability-and-pharmacokinetics-of-trpv1-antagonist-mavatrep-jnj-39439335-tablet-and-capsule-formulations-in-healthy-men-two-open-label-crossover-single-dose-phase-1-studies
#9
Prasarn Manitpisitkul, Kevin Shalayda, Lucille Russell, Panna Sanga, Yinka Williams, Bhavna Solanki, Joseph Caruso, John A Moyer
To improve room temperature stability and oral bioavailability of mavatrep (JNJ-39439335, a transient receptor potential vanilloid subtype-1 antagonist), various formulations were initially developed and evaluated in 2 phase 1 open-label, randomized, 3-way crossover studies in healthy participants. Study 1 evaluated 2 new overencapsulated tablet formulations (formulations B and C) relative to an overencapsulated early tablet formulation (formulation A), using mavatrep HCl salt form. Because these tablets were still not room-temperature stable, in study 2: two free-base solid dispersion amorphous formulations (formulations D and E) were evaluated relative to the best encapsulated formulation from study 1 (formulation C) and also food effect...
November 10, 2017: Clinical Pharmacology in Drug Development
https://www.readbyqxmd.com/read/29105468/-effect-of-manual-acupuncture-electroacupuncture-and-moxibustion-on-intestinal-motility-and-expression-of-enteric-nervous-activity-related-proteins-in-functional-constipation-rats
#10
Xin Zhang, Xuan-Ping Zhang, Yu-Zhu Du, Hai-Jiao Xing, Rui Jia, Li-Jia Pan, Jing Xu, Chun-Sheng Jia
OBJECTIVE: To compare the effect of manual acupuncture (MA), electroacupuncture (EA) and moxibustion interventions on intestinal motility and expression of enteric nervous activity related proteins calcitonin gene related peptide (CGRP), transient receptor potential vanilloid 1 (TRPV 1) and proteinase activated receptor-4 (PAR-4) in colon tissue of rats with functional constipation (FC), so as to select a better intervention method for FC. METHODS: Sixty male SD rats were randomly divided into blank control (n=8), model (n=11), medication (n=8), MA (n=11), EA (n=11), and moxibustion (n=11) groups...
October 25, 2017: Zhen Ci Yan Jiu, Acupuncture Research
https://www.readbyqxmd.com/read/29105300/inhibition-of-transient-potential-receptor-vanilloid-type-1-suppresses-seizure-susceptibility-in-the-genetically-epilepsy-prone-rat
#11
Sue J Cho, Michelle A Vaca, Clive J Miranda, Prosper N'Gouemo
AIMS: Intracellular calcium plays an important role in neuronal hyperexcitability that leads to seizures. One calcium influx route of interest is the transient receptor potential vanilloid type 1 (TRPV1) channel. Here, we evaluated the effects of capsazepine (CPZ), a potent blocker of TRPV1 channels on acoustically evoked seizures (audiogenic seizures, AGS) in the genetically epilepsy-prone rat (GEPR-3), a model of inherited epilepsy. METHODS: Male and female GEPR-3s were used...
November 3, 2017: CNS Neuroscience & Therapeutics
https://www.readbyqxmd.com/read/29100756/trpv1-alterations-in-urinary-bladder-dysfunction-in-a-rat-model-of-stz-induced-diabetes
#12
Bizhan R Sharopov, Kseniya L Gulak, Igor B Philyppov, Anna V Sotkis, Yaroslav M Shuba
AIMS: More than half of diabetic patients experience voiding disorder termed diabetic urinary bladder dysfunction (DBD). Here we have investigated how the alterations in transient receptor potential vanilloid 1 (TRPV1) ion channel expressed in bladder-innervating afferents may contribute to DBD pathogenesis. MAIN METHODS: The rat model of streptozotocin (STZ)-induced diabetes was used. The functional profile of TRPV1 in retrogradely labeled afferent, bladder-innervating dorsal root ganglia (DRG) neurons was examined using patch clamp...
October 31, 2017: Life Sciences
https://www.readbyqxmd.com/read/29099043/involvement-of-opioid-system-trpm8-and-asic-receptors-in-antinociceptive-effect-of-arrabidaea-brachypoda-dc-bureau
#13
Vinícius Peixoto Rodrigues, Cláudia Quintino da Rocha, Larissa Lucena Périco, Raquel de Cássia Dos Santos, Rie Ohara, Catarine Massucato Nishijima, Emerson Ferreira Queiroz, Jean-Luc Wolfender, Lúcia Regina Machado da Rocha, Adair Roberto Soares Santos, Wagner Vilegas, Clélia Akiko Hiruma-Lima
Arrabidaea brachypoda (DC) Bureau is a medicinal plant found in Brazil. Known as "cipó-una", it is popularly used as a natural therapeutic agent against pain and inflammation. This study evaluated the chemical composition and antinociceptive activity of the dichloromethane fraction from the roots of A. brachypoda (DEAB) and its mechanism of action. The chemical composition was characterized by high-performance liquid chromatography, and this fraction is composed only of dimeric flavonoids. The antinociceptive effect was evaluated in formalin and hot plate tests after oral administration (10-100 mg/kg) in male Swiss mice...
November 2, 2017: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29082315/n-arachidonoyl-dopamine-a-novel-endocannabinoid-and-endovanilloid-with-widespread-physiological-and-pharmacological-activities
#14
REVIEW
Urszula Grabiec, Faramarz Dehghani
N-arachidonoyl dopamine (NADA) is a member of the family of endocannabinoids to which several other N-acyldopamines belong as well. Their activity is mediated through various targets that include cannabinoid receptors or transient receptor potential vanilloid (TRPV)1. Synthesis and degradation of NADA are not yet fully understood. Nonetheless, there is evidence that NADA plays an important role in nociception and inflammation in the central and peripheral nervous system. The TRPV1 receptor, for which NADA is a potent agonist, was shown to be an endogenous transducer of noxious heat...
2017: Cannabis and Cannabinoid Research
https://www.readbyqxmd.com/read/29081061/zoledronic-acid-bevacizumab-and-dexamethasone-induced-apoptosis-mitochondrial-oxidative-stress-and-calcium-signaling-are-decreased-in-human-osteoblast-like-cell-line-by-selenium-treatment
#15
Tayfun Yazıcı, Gülperi Koçer, Mustafa Nazıroğlu, İshak Suat Övey, Ahmi Öz
Increased intracellular free calcium ion (Ca(2+)) concentration induces excessive oxidative stress and apoptosis. Medical procedures such as zoledronic acid (Zol), bevacizumab (Bev), and dexamethasone (Dex) are usually used in the treatment of bone diseases (osteoporosis, Paget's disease, etc.) and to prevent metastasis in the bone although the procedures induce osteonecrosis of the jaw through excessive production of reactive oxygen species (ROS). Recently, we observed regulator roles of selenium (Se) on apoptosis and Ca(2+) entry through transient receptor potential vanilloid 1 (TRPV1) channels in the cancer cell lines...
October 28, 2017: Biological Trace Element Research
https://www.readbyqxmd.com/read/29080196/nitric-oxide-signaling-molecules-in-acupoints-toward-mechanisms-of-acupuncture
#16
Sheng-Xing Ma
Recent clinical trial studies have demonstrated that the effects of acupuncture on pain improvement are small and no difference between acupoints and non-points. Whether acupuncture needles must be inserted in specific points depends on whether acupoint specificity exists that is still not resolved, and is now urgent. Previous anatomical studies have demonstrated that acupoints exist higher number of nerve fibers/trunks, blood vessels, hair follicles, and sweat glands as well as density of the gap junction...
November 2017: Chinese Journal of Integrative Medicine
https://www.readbyqxmd.com/read/29079432/peripheral-nerve-injury-induced-rearrangement-of-neural-circuit-in-the-spinal-dorsal-horn-revealed-by-cross-correlation-analysis
#17
Yu Takemura, Shunsaku Kobayashi, Eiko Kato, Shigeki Yamaguchi, Yuuichi Hori
Peripheral nerve injury often induces abnormal pain states, such as hyperalgesia and allodynia. In this study, we attempted to elucidate how neurons are synaptically integrated into the neuronal circuitry in the spinal dorsal horn and how synaptic connectivity patterns among dorsal horn neurons are altered by peripheral nerve injury. Experiments were performed on 6-8-week-old ICR mice. Partial sciatic nerve ligation was performed. Transverse slices of the lumbar spinal cord were prepared. Spike activities were simultaneously recorded from multiple neurons in the superficial dorsal horn (SDH) using a multi-electrode array system, and cross-correlograms between spike trains of neuron pairs were constructed...
October 24, 2017: Neuroscience Letters
https://www.readbyqxmd.com/read/29071961/-effect-of-electroacupuncture-at-yintang-gv-29-and-tianshu-st-25-on-the-ethology-and-the-expression-of-trpv-1-receptor-in-colon-of-irritable-bowel-syndrome-rats
#18
Li-Hua Tan, Kai-Ge Li, Yan-Ying Wu, Ying Lan, Meng-Wei Guo, Wen-Lian Zhu, Lu-Fen Zhang, Ya-Fang Zhao, Xiao-Hong Li, Xiao-Xuan Ren
OBJECTIVE: To observe the ethology and expression of transient receptor potential vanilloid-1(TRPV 1) in colon of irritable bowel syndrome (IBS) rats treated by electroacupuncture (EA) at "Yintang" (GV 29) and "Tianshu" (ST 25), so as to explore the different effectiveness of different acupoints and its related mechanism underlying improvement of the symptoms of somatopsychic illness. METHODS: Thirty-two neonatal Wistar rats were randomly divided into blank control group, model group, Yintang (GV 29) group, and Tianshu (ST 25) group (n=8 in each group)...
April 25, 2017: Zhen Ci Yan Jiu, Acupuncture Research
https://www.readbyqxmd.com/read/29063115/-trpv1-an-important-molecule-involved-in-the-peripheral-sensitization-during-chronic-pain-and-central-pain-modulation
#19
Ying Zhang, Yun Wang
As chronic pain is a severe problem in clinics, study of the mechanisms of chronic pain and development of novel analgesic agents is of significance. In the past decade, our lab completed a series of studies on the regulatory mechanisms of functional sensitization and membrane trafficking of transient receptor potential vanilloid type 1 (TRPV1), a key molecule involved in the development of peripheral sensitization. Our studies elucidated the important regulatory roles of several protein kinases, including PKD1 (protein kinase D1), Cdk5 (cyclin-dependent kinase 5) and LIMK (LIM-motif containing kinase), in inflammatory thermal hyperalgesia...
October 25, 2017: Sheng Li Xue Bao: [Acta Physiologica Sinica]
https://www.readbyqxmd.com/read/29057994/effects-of-herpes-simplex-virus-vectors-encoding-poreless-trpv1-or-protein-phosphatase-1%C3%AE-in-a-rat-cystitis-model-induced-by-hydrogen-peroxide
#20
S Takai, T Majima, B Reinhart, W F Goins, Y Funahashi, M Gotoh, P Tyagi, J C Glorioso, N Yoshimura
Enhanced afferent excitability is considered to be an important pathophysiological basis of interstitial cystitis/bladder pain syndrome (IC/BPS). In addition, transient receptor potential vanilloid-1 (TRPV1) receptors are known to be involved in afferent sensitization. Animals with hydrogen peroxide (HP)-induced cystitis have been used as a model exhibiting pathologic characteristics of chronic inflammatory condition of the bladder. This study investigated the effect of gene therapy with replication-defective herpes simplex virus (HSV) vectors encoding poreless TRPV1 (PL) or protein phosphatase 1 α (PP1α), a negative regulator of TRPV1, using a HP-induced rat model of cystitis...
October 20, 2017: Gene Therapy
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