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transient receptor vanilloid 1

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https://www.readbyqxmd.com/read/29334670/genetic-ablation-of-trpv1-exacerbates-pressure-overload-induced-cardiac-hypertrophy
#1
Beihua Zhong, Jack Rubinstein, Shuangtao Ma, Donna H Wang
Transient receptor potential vanilloid 1 (TRPV1) channels expressed in sensory nerves may regulate vascular tone and cardiovascular function via their anti-inflammatory effects by releasing neuropeptide calcitonin gene-related peptide (CGRP). Inflammation plays a role in the progression of cardiac hypertrophy and TRPV1 activation may be key to cardiac inflammatory processes. The aim of this study was to test the hypothesis that TRPV1 modulates inflammatory processes to protect the heart from pressure overload-induced hypertrophy and inflammatory responses...
January 12, 2018: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/29331959/probenecid-improves-cardiac-function-in-patients-with-heart-failure-with-reduced-ejection-fraction-in-vivo-and-cardiomyocyte-calcium-sensitivity-in-vitro
#2
Nathan Robbins, Mark Gilbert, Mohit Kumar, James W McNamara, Patrick Daly, Sheryl E Koch, Ginger Conway, Mohamed Effat, Jessica G Woo, Sakthivel Sadayappan, Jack Rubinstein
BACKGROUND: Transient receptor potential vanilloid 2 is a calcium channel activated by probenecid. Probenecid is a Food and Drug Administration-approved uricosuric drug that has recently been shown to induce positive lusitropic and inotropic effects in animal models through cardiomyocyte transient receptor potential vanilloid 2 activation. The aim of this study was to test the hypothesis that oral probenecid can improve cardiac function and symptomatology in patients with heart failure with reduced ejection fraction and to further elucidate its calcium-dependent effects on myocyte contractility...
January 13, 2018: Journal of the American Heart Association
https://www.readbyqxmd.com/read/29317149/phenylquinoline-transient-receptor-potential-vanilloid-1-antagonists-for-the-treatment-of-pain-discovery-of-1-2-phenylquinoline-4-carbonyl-n-4-trifluoromethyl-phenyl-pyrrolidine-3-carboxamide
#3
Chen Liao, Yan Liu, Chunxia Liu, Jiaqi Zhou, Huilan Li, Nasi Wang, Jieming Li, Taiyu Liu, Hesham Ghaleb, Wenlong Huang, Hai Qian
Reported herein is the design, synthesis, and pharmacologic characterization of a class of TRPV1 antagonists constructed on a phenylquinoline platform that evolved from Cinchophen lead. This design composes three sections: a phenylquinoline headgroup attached to an aliphatic carboxamides, which is tethered at a phenyl tail group. Optimization of this design led to the identification of 37, comprising a pyrrolidine linker and a trifluoromethyl-phenyl tail. In the TRPV1 functional assay, using cells expressed hTRPV1, 37 antagonized capsaicin-induced Ca2+ influx, with an IC50 value of 10...
December 30, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/29306760/effect-of-acetaminophen-on-osteoblastic-differentiation-and-migration-of-mc3t3-e1-cells
#4
Yoshihiro Nakatsu, Fumio Nakagawa, Sen Higashi, Tomoko Ohsumi, Shunji Shiiba, Seiji Watanabe, Hiroshi Takeuchi
BACKGROUND: N-acetyl-p-aminophenol (APAP, acetaminophen, paracetamol) is a widely used analgesic/antipyretic with weak inhibitory effects on cyclooxygenase (COX) compared to non-steroidal anti-inflammatory drugs (NSAIDs). The mechanism of action of APAP is mediated by its metabolite that activates transient receptor potential channels, including transient receptor potential vanilloid 1 (TRPV1) and TRP ankyrin 1 (TRPA1) or the cannabinoid receptor type 1 (CB1). However, the exact molecular mechanism and target underlying the cellular actions of APAP remain unclear...
July 15, 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/29304162/adrenergic-receptors-inhibit-trpv1-activity-in-the-dorsal-root-ganglion-neurons-of-rats
#5
Yumi Matsushita, Miki Manabe, Naoki Kitamura, Izumi Shibuya
Transient receptor potential vanilloid type 1 (TRPV1) is a polymodal receptor channel that responds to multiple types of stimuli, such as heat, acid, mechanical pressure and some vanilloids. Capsaicin is the most commonly used vanilloid to stimulate TRPV1. TRPV1 channels are expressed in dorsal root ganglion neurons that extend to Aδ- and C-fibers and have a role in the transduction of noxious inputs to the skin into the electrical signals of the sensory nerve. Although noradrenergic nervous systems, including the descending antinociceptive system and the sympathetic nervous system, are known to modulate pain sensation, the functional association between TRPV1 and noradrenaline in primary sensory neurons has rarely been examined...
2018: PloS One
https://www.readbyqxmd.com/read/29301784/trpv4-transient-receptor-potential-vanilloid-4-channel-dependent-negative-feedback-mechanism-regulates-gq-protein-coupled-receptor-induced-vasoconstriction
#6
Kwangseok Hong, Eric L Cope, Leon J DeLalio, Corina Marziano, Brant E Isakson, Swapnil K Sonkusare
OBJECTIVE: Several physiological stimuli activate smooth muscle cell (SMC) GqPCRs (Gq protein-coupled receptors) to cause vasoconstriction. As a protective mechanism against excessive vasoconstriction, SMC GqPCR stimulation invokes endothelial cell vasodilatory signaling. Whether Ca2+ influx in endothelial cells contributes to the regulation of GqPCR-induced vasoconstriction remains unknown. Ca2+ influx through TRPV4 (transient receptor potential vanilloid 4) channels is a key regulator of endothelium-dependent vasodilation...
January 4, 2018: Arteriosclerosis, Thrombosis, and Vascular Biology
https://www.readbyqxmd.com/read/29288742/the-research-of-the-possible-mechanism-and-the-treatment-for-capsaicin-induced-cough
#7
Li Zhang, Tieying Sun, Longteng Liu, Lifang Wang
Unexplained chronic cough (UCC) affects millions of patients worldwide. New therapeutic approaches to this condition are urgently needed, since current treatment options provide only symptomatic relief. Cough reflex hypersensitivity has been shown to play an important role in the pathogenesis of UCC. The transient receptor potential vanilloid type 1 (TRPV1) is present on peripheral terminals of airway sensory nerves and modulation of its activity represents a potential target for the pharmacological treatment of UCC...
December 27, 2017: Pulmonary Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/29286076/activation-of-transient-receptor-potential-vanilloid-1-protects-the-heart-against-apoptosis-in-ischemia-reperfusion-injury-through-upregulating-the-pi3k-akt-signaling-pathway
#8
Xiao-Xue Jiang, Guan-Yu Liu, Han Lei, Zuo-Ling Li, Qing-Ping Feng, Wei Huang
Transient receptor potential vanilloid 1 (TRPV1) is a nonselective cation channel and a molecular integrator of noxious stimuli. TRPV1 activation confers cardiac protection against ischemia/reperfusion (I/R) injury. The present study aimed to investigate whether the cardioprotective effects of TRPV1 were associated with the inhibition of apoptosis via the phosphatidylinositol 3‑kinase (PI3K)/protein kinase B (Akt) and extracellular signal‑regulated protein kinase 1/2 (ERK1/2) signaling pathways. Briefly, the hearts of TRPV1 knockout (TRPV1‑/‑) or wild‑type (WT) mice were isolated and subjected to 30 min of ischemia followed by 60 min of reperfusion in a Langendorff apparatus in the presence or absence of the PI3K inhibitor, LY294002...
December 21, 2017: International Journal of Molecular Medicine
https://www.readbyqxmd.com/read/29274880/cb1-cannabinoid-receptor-agonist-mouse-vd-hemopressin-%C3%AE-produced-supraspinal-analgesic-activity-in-the-preclinical-models-of-pain
#9
Ting Zheng, Run Zhang, Ting Zhang, Meng-Na Zhang, Biao Xu, Jing-Jing Song, Ning Li, Hong-Hai Tang, Pei Wang, Rui Wang, Quan Fang
Mouse VD-hemopressin(α) (VD-Hpα) is an undecapeptide that selectively activates CB1 cannabinoid receptor in in vitro functional tests, and exerts CB1-mediated central antinociception in the mouse tail-flick assay. The aim of the present study was to further investigate the analgesic properties of supraspinal mouse VD-Hpα in a range of preclinical pain models. Our results indicated that the classical cannabinoid agonist WIN 55,212-2 produced supraspinal analgesia in preclinical pain models, which was selectively antagonized by the CB1 antagonist/inverse agonist AM251, but not by the CB2 antagonist AM630...
December 21, 2017: Brain Research
https://www.readbyqxmd.com/read/29274843/oxaliplatin-induced-changes-in-expression-of-transient-receptor-potential-channels-in-the-dorsal-root-ganglion-as-a-neuropathic-mechanism-for-cold-hypersensitivity
#10
Akiko Chukyo, Terumasa Chiba, Toshie Kambe, Ken Yamamoto, Kazuyoshi Kawakami, Kyoji Taguchi, Kenji Abe
Transient receptor potential (TRP) receptors are involved in the development of chemotherapy-induced peripheral neuropathic pain, which is a common side effect of selected chemotherapeutic agents such as oxaliplatin. However, the precise contribution of TRPs to this condition remains unknown. Cold hypersensitivity is the hallmark of oxaliplatin-induced neuropathy, so we used a preclinical model of oxaliplatin-induced cold hypersensitivity in rats to determine the effects of oxaliplatin on TRP channels. To this end, immunohistochemistry was used to examine TRP vanilloid 1 (TRPV1), TRP ankyrin 1 (TRPA1), and TRP melastatin 8 (TRPM8) expression in the rat dorsal root ganglion (DRG) after 4days of oxaliplatin treatment...
December 15, 2017: Neuropeptides
https://www.readbyqxmd.com/read/29259542/capsaicin-enhances-glutamatergic-synaptic-transmission-to-neonatal-rat-hypoglossal-motor-neurons-via-a-trpv1-independent-mechanism
#11
Prajwal P Thakre, Mark C Bellingham
We investigated whether capsaicin modulated synaptic transmission to hypoglossal motor neurons (HMNs) by acting on transient receptor potential vanilloid type 1 (TRPV1) receptors. Using whole-cell patch clamp recording from neonatal rat HMNs, we found that capsaicin increased spontaneous excitatory post-synaptic current (sEPSC) frequency and amplitude. Interestingly, the only effect of capsaicin on spontaneous inhibitory post-synaptic currents (sIPSCs) was a significant decrease in sIPSC amplitude without altering frequency, indicating a post-synaptic mechanism of action...
2017: Frontiers in Cellular Neuroscience
https://www.readbyqxmd.com/read/29259381/gender-differences-in-ghrelin-nociception-genes-psychological-factors-and-quality-of-life-in-functional-dyspepsia
#12
Yoon Jin Choi, Young Soo Park, Nayoung Kim, Yong Sung Kim, Sun Min Lee, Dong Ho Lee, Hyun Chae Jung
AIM: to evaluate gender differences in the aspect of ghrelin, nociception-related genes and psychological aspects and the quality of life (QoL) in Korean functional dyspepsia (FD) patients. METHODS: Total of 191 persons were prospectively enrolled between March 2013 and May 2016 in Seoul National Bundang Hospital, and classified into control and FD group based on ROME III criteria. Questionnaire included assessment for dyspepsia symptoms, QoL and anxiety or depression...
December 7, 2017: World Journal of Gastroenterology: WJG
https://www.readbyqxmd.com/read/29258175/capsaicin-friend-or-foe-in-skin-cancer-and-other-related-malignancies
#13
REVIEW
Simona-Roxana Georgescu, Maria-Isabela Sârbu, Clara Matei, Mihaela Adriana Ilie, Constantin Caruntu, Carolina Constantin, Monica Neagu, Mircea Tampa
Capsaicin is the main pungent in chili peppers, one of the most commonly used spices in the world; its analgesic and anti-inflammatory properties have been proven in various cultures for centuries. It is a lipophilic substance belonging to the class of vanilloids and an agonist of the transient receptor potential vanilloid 1 receptor. Taking into consideration the complex neuro-immune impact of capsaicin and the potential link between inflammation and carcinogenesis, the effect of capsaicin on muco-cutaneous cancer has aroused a growing interest...
December 16, 2017: Nutrients
https://www.readbyqxmd.com/read/29249037/transient-receptor-potential-vanilloid-3-trpv3-activation-plays-a-central-role-in-cardiac-fibrosis-induced-by-pressure-overload-in-rats-via-tgf-%C3%AE-1-pathway
#14
Yan Liu, Hanping Qi, Mingyao E, Pilong Shi, Qianhui Zhang, Shuzhi Li, Ye Wang, Yonggang Cao, Yunping Chen, Lina Ba, Jingquan Gao, Wei Huang, Hongli Sun
Cardiac fibrosis is a common pathologic change along with pressure overload. Recent studies indicated that transient receptor potential (TRP) channels played multiple roles in heart. However, the functional role of transient receptor potential vanilloid-3 (TRPV3) in cardiac fibrosis remained unclear. The present study was designed to investigate the relationship between TRPV3 activation and pressure overload-induced cardiac fibrosis. Pressure overload rats were successfully established by abdominal aortic constriction (AAC), and cardiac fibrosis was simulated by 100 nM angiotensin II (Ang II) in neonatal cardiac fibroblasts...
December 16, 2017: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/29247491/the-roles-of-trpv1-trpa1-and-trpm8-channels-in-chemical-and-thermal-sensitivity-of-the-mouse-oral-mucosa
#15
Tatjana I Kichko, Winfried Neuhuber, Gerd Kobal, Peter W Reeh
Spices in food and beverages and compounds in tobacco smoke interact with sensory irritant receptors of the transient receptor potential (TRP) cation channel family. TRPV1 (vanilloid type 1), TRPA1 (ankyrin 1) and TRPM8 (melastatin 8) not only elicit action potential signaling through trigeminal nerves, eventually evoking pungent or cooling sensations, but by their calcium conductance they also stimulate the release of calcitonin gene-related peptide (CGRP). This is measured as an index of neuronal activation to elucidate the chemo- and thermosensory transduction in the isolated mouse buccal mucosa of wildtypes and pertinent knockouts...
December 15, 2017: European Journal of Neuroscience
https://www.readbyqxmd.com/read/29247238/trpv1-mediated-pharmacological-hypothermia-promotes-improved-functional-recovery-following-ischemic-stroke
#16
Zhijuan Cao, Adithya Balasubramanian, Steen E Pedersen, Jonathan Romero, Robia G Pautler, Sean P Marrelli
Hypothermia shows promise for stroke neuroprotection, but current cooling strategies cause undesirable side effects that limit their clinical applications. Increasing efforts have focused on pharmacological hypothermia as a treatment option for stroke. Previously, we showed that activation of a thermoregulatory ion channel, transient receptor potential vanilloid 1 (TRPV1), by dihydrocapsaicin (DHC) produces reliable hypothermia. In this study, we investigate the effects of TRPV1-mediated hypothermia by DHC on long-term ischemic stroke injury and functional outcome...
December 15, 2017: Scientific Reports
https://www.readbyqxmd.com/read/29238714/corneal-nerve-fiber-structure-its-role-in-corneal-function-and-its-changes-in-corneal-diseases
#17
REVIEW
Hiroshi Eguchi, Akio Hiura, Hiroshi Nakagawa, Shunji Kusaka, Yoshikazu Shimomura
Recently, in vivo confocal microscopy is used to examine the human corneal nerve fibers morphology. Corneal nerve fiber architecture and its role are studied in healthy and pathological conditions. Corneal nerves of rats were studied by nonspecific acetylcholinesterase (NsAchE) staining. NsAchE-positive subepithelial (stromal) nerve fiber has been found to be insensitive to capsaicin. Besides, NsAchE-negative but capsaicin-sensitive subbasal nerve (leash) fibers formed thick mesh-like structure showing close interconnections and exhibit both isolectin B4- and transient receptor potential vanilloid channel 1- (TRPV1-) positive...
2017: BioMed Research International
https://www.readbyqxmd.com/read/29238305/mir-29a-suppresses-spermatogenic-cell-apoptosis-in-testicular-ischemia-reperfusion-injury-by-targeting-trpv4-channels
#18
Jin-Zhuo Ning, Wei Li, Fan Cheng, Wei-Min Yu, Ting Rao, Yuan Ruan, Run Yuan, Xiao-Bin Zhang, Dong Zhuo, Yang Du, Cheng-Cheng Xiao
Background: MicroRNAs (miRNAs) have emerged as gene expression regulators in the progression of ischemia-reperfusion injury (IRI). Accumulating evidences have indicated miR-29a play roles in myocardial and cerebral IRI. However, the role of miR-29a in testicular IRI has not been elucidated. Methods: Changes in expression of miR-29a and Transient Receptor Potential Vanilloid 4 (TRPV4) in animal samples and GC-1 spermatogenic cells were examined. The effects of miR-29a on spermatogenic cell apoptosis in testicular IRI were analyzed both in vitro and in vivo...
2017: Frontiers in Physiology
https://www.readbyqxmd.com/read/29237478/am404-paracetamol-metabolite-prevents-prostaglandin-synthesis-in-activated-microglia-by-inhibiting-cox-activity
#19
Soraya Wilke Saliba, Ariel R Marcotegui, Ellen Fortwängler, Johannes Ditrich, Juan Carlos Perazzo, Eduardo Muñoz, Antônio Carlos Pinheiro de Oliveira, Bernd L Fiebich
BACKGROUND: N-arachidonoylphenolamine (AM404), a paracetamol metabolite, is a potent agonist of the transient receptor potential vanilloid type 1 (TRPV1) and low-affinity ligand of the cannabinoid receptor type 1 (CB1). There is evidence that AM404 exerts its pharmacological effects in immune cells. However, the effect of AM404 on the production of inflammatory mediators of the arachidonic acid pathway in activated microglia is still not fully elucidated. METHOD: In the present study, we investigated the effects of AM404 on the eicosanoid production induced by lipopolysaccharide (LPS) in organotypic hippocampal slices culture (OHSC) and primary microglia cultures using Western blot, immunohistochemistry, and ELISA...
December 13, 2017: Journal of Neuroinflammation
https://www.readbyqxmd.com/read/29237283/ghrelin-attenuated-hyperalgesia-induced-by-chronic-nitroglycerin-cgrp-and-trpv1-as-targets-for-migraine-management
#20
Fereshteh Farajdokht, Gisou Mohaddes, Dariush Shanehbandi, Pouran Karimi, Shirin Babri
Background According to the neurovascular theory of migraine, activation of the trigeminovascular system contributes to the development of migraine. This study examined the effects of chronic intraperitoneal ghrelin (150 µg/kg) treatment on the development of chronic migraine induced by intermittent injection of nitroglycerin 10 mg/kg. Methods Baseline and post-drug (2 h following nitroglycerin injection) mechanical and thermal sensitivity were assessed by von Frey hair and tail immersion tests, respectively on days 1, 3, 5, 7, 9 and 11...
January 1, 2017: Cephalalgia: An International Journal of Headache
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