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TRPV1 receptor agonist

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https://www.readbyqxmd.com/read/28701511/n-arachidonoyl-dopamine-modulates-acute-systemic-inflammation-via-nonhematopoietic-trpv1
#1
Samira K Lawton, Fengyun Xu, Alphonso Tran, Erika Wong, Arun Prakash, Mark Schumacher, Judith Hellman, Kevin Wilhelmsen
N-Arachidonoyl dopamine (NADA) is an endogenous lipid that potently activates the transient receptor potential vanilloid 1 (TRPV1), which mediates pain and thermosensation. NADA is also an agonist of cannabinoid receptors 1 and 2. We have reported that NADA reduces the activation of cultured human endothelial cells by LPS and TNF-α. Thus far, in vivo studies using NADA have focused on its neurologic and behavioral roles. In this article, we show that NADA potently decreases in vivo systemic inflammatory responses and levels of the coagulation intermediary plasminogen activator inhibitor 1 in three mouse models of inflammation: LPS, bacterial lipopeptide, and polymicrobial intra-abdominal sepsis...
July 12, 2017: Journal of Immunology: Official Journal of the American Association of Immunologists
https://www.readbyqxmd.com/read/28687197/opioid-receptor-activation-is-involved-in-neuroprotection-induced-by-trpv1-channel-activation-against-excitotoxicity-in-the-rat-retina
#2
Kenji Sakamoto, Taiyo Kuroki, Tomonori Sagawa, Hiroko Ito, Asami Mori, Tsutomu Nakahara, Kunio Ishii
Recently, we reported that capsaicin, a transient receptor potential vanilloid type1 (TRPV1) agonist, protected against excitotoxicity induced by intravitreal N-methyl-D-aspartic acid (NMDA) in the rats in vivo. It has been reported that morphine, an opioid receptor agonist, ameliorated excitotoxicity induced by ischemia-reperfusion in the retina, and that capsaicin-induced neuroprotection was reduced by naloxone, an opioid receptor antagonist in the brain. The aim of the present study is to clarify whether activation of opioid receptors is involved in the capsaicin-induced neuroprotection in the retina...
July 4, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28681979/trpv1-channels-in-human-skeletal-muscle-feed-arteries-implications-for-vascular-function
#3
Stephen J Ives, Song Young Park, Oh Sung Kwon, Jayson R Gifford, Robert H I Andtbacka, John R Hyngstrom, Russell S Richardson
To examine the role of transient receptor potential vanilloid type 1 (TRPV1 ) ion channel in the vascular function of human skeletal muscle feed arteries (SMFAs) and if activation of this heat-sensitive receptor could be involved in modulating vascular function, SMFAs from 16 humans (63 ± 5, 41-89 yrs) were studied using wire myography with capsaicin (TRPV1 agonist) and without (control). Specifically, phenylephrine (PE, α1 -adrenergic receptor agonist), dexemedetomidine (DEX, α2 -adrenergic receptor agonist), acetylcholine (ACh), and sodium nitroprusside (SNP) concentration response curves (CRCs) were performed to assess the role of TRPV1 channels in α-receptor-mediated vasocontraction as well as endothelium-dependent and independent vasorelaxation, respectively...
July 6, 2017: Experimental Physiology
https://www.readbyqxmd.com/read/28680405/cannabinoids-and-vanilloids-in-schizophrenia-neurophysiological-evidence-and-directions-for-basic-research
#4
REVIEW
Rafael N Ruggiero, Matheus T Rossignoli, Jana B De Ross, Jaime E C Hallak, Joao P Leite, Lezio S Bueno-Junior
Much of our knowledge of the endocannabinoid system in schizophrenia comes from behavioral measures in rodents, like prepulse inhibition of the acoustic startle and open-field locomotion, which are commonly used along with neurochemical approaches or drug challenge designs. Such methods continue to map fundamental mechanisms of sensorimotor gating, hyperlocomotion, social interaction, and underlying monoaminergic, glutamatergic, and GABAergic disturbances. These strategies will require, however, a greater use of neurophysiological tools to better inform clinical research...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28680392/direct-anandamide-activation-of-trpv1-produces-divergent-calcium-and-current-responses
#5
Axel J Fenwick, Daniel K Fowler, Shaw-Wen Wu, Forrest J Shaffer, Jonathan E M Lindberg, Dallas C Kinch, James H Peters
In the brainstem nucleus of the solitary tract (NTS), primary vagal afferent neurons express the transient receptor potential vanilloid subfamily member 1 (TRPV1) at their central terminals where it contributes to quantal forms of glutamate release. The endogenous membrane lipid anandamide (AEA) is a putative TRPV1 agonist in the brain, yet the extent to which AEA activation of TRPV1 has a neurophysiological consequence is not well established. We investigated the ability of AEA to activate TRPV1 in vagal afferent neurons in comparison to capsaicin (CAP)...
2017: Frontiers in Molecular Neuroscience
https://www.readbyqxmd.com/read/28671709/transient-receptor-potential-a1-trpa1-agonists-inhibit-contractions-of-the-isolated-human-ureter
#6
Philipp Weinhold, Martin Hennenberg, Frank Strittmatter, Christian G Stief, Christian Gratzke, Petter Hedlund
AIMS: Mechanoafferent and peristaltic mechanisms of the human ureter involve transient receptor potential V1 (TRPV1)- and purinoceptor-mediated functions. Hydrogen sulphide, an endogenous TRPA1 ligand, is linked to inhibitory neurotransmission of the pig ureter. No information is available on TRPA1 activity in the human ureter. We therefore examined the distribution and function of TRPA1 in the human ureter. METHODS: Expression of TRPA1 in human ureter tissue was studied by Western blot and immunofluorescence...
July 3, 2017: Neurourology and Urodynamics
https://www.readbyqxmd.com/read/28671132/capsaicin-attenuates-amyloid-%C3%AE-induced-synapse-loss-and-cognitive-impairments-in-mice
#7
Long Chen, Zhilin Huang, Yehong Du, Min Fu, Huili Han, Yutian Wang, Zhifang Dong
Alzheimer's disease (AD) is the most common cause of progressive cognitive impairment in the aged. The aggregation of the amyloid β-protein (Aβ) is a hallmark of AD and is linked to synapse loss and cognitive impairment. Capsaicin, a specific agonist of the transient receptor potential vanilloid 1 (TRPV1), has been proven to ameliorate stress-induced AD-like pathological and cognitive impairments, but it is unclear whether TRPV1 activation can affect cognitive and synaptic functions in Aβ-induced mouse model of AD...
June 27, 2017: Journal of Alzheimer's Disease: JAD
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/28640864/targeting-breast-cancer-cells-by-mrs1477-a-positive-allosteric-modulator-of-trpv1-channels
#10
Mustafa Nazıroğlu, Bilal Çiğ, Walter Blum, Csaba Vizler, Andrea Buhala, Annamária Marton, Róbert Katona, Katalin Jósvay, Beat Schwaller, Zoltán Oláh, László Pecze
There is convincing epidemiological and experimental evidence that capsaicin, a potent natural transient receptor potential cation channel vanilloid member 1 (TRPV1) agonist, has anticancer activity. However, capsaicin cannot be given systemically in large doses, because of its induction of acute pain and neurological inflammation. MRS1477, a dihydropyridine derivative acts as a positive allosteric modulator of TRPV1, if added together with capsaicin, but is ineffective, if given alone. Addition of MRS1477 evoked Ca2+ signals in MCF7 breast cancer cells, but not in primary breast epithelial cells...
2017: PloS One
https://www.readbyqxmd.com/read/28637794/a-trpv1-to-secretagogin-regulatory-axis-controls-pancreatic-%C3%AE-cell-survival-by-modulating-protein-turnover
#11
Katarzyna Malenczyk, Fatima Girach, Edit Szodorai, Petter Storm, Åsa Segerstolpe, Giuseppe Tortoriello, Robert Schnell, Jan Mulder, Roman A Romanov, Erzsébet Borók, Fabiana Piscitelli, Vincenzo Di Marzo, Gábor Szabó, Rickard Sandberg, Stefan Kubicek, Gert Lubec, Tomas Hökfelt, Ludwig Wagner, Leif Groop, Tibor Harkany
Ca(2+)-sensor proteins are generally implicated in insulin release through SNARE interactions. Here, secretagogin, whose expression in human pancreatic islets correlates with their insulin content and the incidence of type 2 diabetes, is shown to orchestrate an unexpectedly distinct mechanism. Single-cell RNA-seq reveals retained expression of the TRP family members in β-cells from diabetic donors. Amongst these, pharmacological probing identifies Ca(2+)-permeable transient receptor potential vanilloid type 1 channels (TRPV1) as potent inducers of secretagogin expression through recruitment of Sp1 transcription factors...
July 14, 2017: EMBO Journal
https://www.readbyqxmd.com/read/28631948/possible-contribution-of-pannexin-1-to-capsaicin-induced-atp-release-in-rat-nasal-columnar-epithelial-cells
#12
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/28622417/the-antimigraine-butterbur-ingredient-isopetasin-desensitises-peptidergic-nociceptors-via-the-transient-receptor-potential-ankyrin-1-channel
#13
Silvia Benemei, Francesco De Logu, Simone Li Puma, Ilaria Maddalena Marone, Elisabetta Coppi, Filippo Ugolini, Wolfgang Liedtke, Pollastro Federica, Giovanni Appendino, Pierangelo Geppetti, Serena Materazzi, Romina Nassini
BACKGROUND AND PURPOSE: The mechanism of the antimigraine action of butterbur [Petasites hybridus (L.) Gaertn.] is unknown. Here, we investigated the ability of isopetasin, a major butterbur constituent, to specifically target the transient receptor ankyrin 1 (TRPA1) channel and to affect functional responses relevant to migraine. EXPERIMENTAL APPROACH: Single cell calcium imaging and patch-clamp recordings in human and rodent TRPA1-expressing cells, neurogenic motor responses in isolated rat/mouse urinary bladder, release of calcitonin gene-related peptide (CGRP) from mouse spinal cord in vitro, and facial rubbing in mice and meningeal blood flow in rat were examined...
June 16, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28621704/sensitization-of-trpv1-and-trpa1-via-peripheral-mglur5-signaling-contributes-to-thermal-and-mechanical-hypersensitivity
#14
Kuniya Honda, Masamichi Shinoda, Masahiro Kondo, Kohei Shimizu, Hisashi Yonemoto, Katsuhiko Otsuki, Ryuta Akasaka, Akihiko Furukawa, Koichi Iwata
Peripheral tissue inflammation or injury causes glutamate release from nociceptive axons, keratinocytes and Schwann cells, resulting in thermal hypersensitivity. However, the detailed molecular mechanisms underlying glutamate-induced thermal hypersensitivity are unknown. The aim of this study was to clarify the involvement of peripheral transient receptor potential (TRP) ankyrin 1 (TRPA1), TRP vanilloid 1 (TRPV1) and protein kinase C epsilon (PKCε) in glutamate-induced pain hypersensitivity. The amount of glutamate in the facial tissue was significantly increased 3 days after facial CFA injection...
June 8, 2017: Pain
https://www.readbyqxmd.com/read/28620299/the-alkamide-trans-pellitorine-targets-ppar%C3%AE-via-trpv1-and-trpa1-to-reduce-lipid-accumulation-in-developing-3t3-l1-adipocytes
#15
Barbara Lieder, Mathias Zaunschirm, Ann-Katrin Holik, Jakob P Ley, Joachim Hans, Gerhard E Krammer, Veronika Somoza
Adipose tissue is an important endocrine organ in the human body. However, pathological overgrowth is associated with chronic illness. Regulation of adipogenesis and maturation of adipocytes via bioactive compounds in our daily diet has been in focus of research in the past years and showed promising results for agonists of the ion channels transient receptor potential channel (TRP) V1 and A1. Here, we investigated the anti-adipogenic potential and underlying mechanisms of the alkamide trans-pellitorine present in Piper nigrum via TRPV1 and TRPA1 in 3T3-L1 cells...
2017: Frontiers in Pharmacology
https://www.readbyqxmd.com/read/28602628/overexpression-of-fibulin-5-attenuates-burn-induced-inflammation-via-trpv1-cgrp-pathway
#16
Xiaoqian Hou, Hui Li, Chunhua Zhang, Junling Wang, Xiuli Li, Xin Li
Fibulin-5, a multifunctional extracellular matrix protein, is up-regulated in response to mechanical injury and can promote dermal wound healing. This study aimed to explore the role and mechanism of Fibulin-5 in the pathogenesis of post-burn inflammation in thermally-injured mice. Here, we found that Fibulin-5 was up-regulated in the dorsal root ganglion (DRG) of burn-injured mice. After nociceptive behavioral testing, DRG was isolated and cultured to detect the mechanism of Fibulin-5 in thermal injury models by recombinant adenovirus overexpressing Fibulin-5, RT-qPCR, Western Blot, ELISA, AP20187 (an activator of one kind of kinase phosphorylating the α subunit of eukaryotic initiation factor 2, eIF2α), capsaicin (an agonist of transient receptor potential vanilloid (TRPV)-1), and an anti-CGRP neutralizing antibody...
June 8, 2017: Experimental Cell Research
https://www.readbyqxmd.com/read/28539997/interaction-between-the-cannabinoid-and-vanilloid-systems-on-anxiety-in-male-rats
#17
Nafiseh Faraji, Alireza Komaki, Iraj Salehi
INTRODUCTION: Previous studies have shown that the cannabinoid system is involved in anxiety. In addition, transient receptor potential vanilloid type-1 (TRPV1) channels are new targets for the development of anxiolytics. The present study investigated the possible interaction between the cannabinoid and vanilloid systems on anxiety-like behavior in rats. METHODS: Four different groups of male Wistar rats received intraperitoneal (IP) injections of (1) vehicle (DMSO+saline), (2) cannabinoid receptor agonist WIN55212-2 (WIN) (1 mg/kg), (3) TRPV1 receptor antagonist capsazepine (CPZ) (5 mg/kg), or (4) combined WIN (1 mg/kg) and CPZ (5 mg/kg) treatment 30 minutes before testing in the elevated plus maze...
March 2017: Basic and Clinical Neuroscience
https://www.readbyqxmd.com/read/28531316/a-comprehensive-method-to-quantify-adaptations-by-male-and-female-mice-with-hot-flashes-induced-by-the-neurokinin-b-receptor-agonist-senktide
#18
Ashley A Krull, Sarah A Larsen, Donald K Clifton, Genevieve Neal-Perry, Robert A Steiner
Vasomotor symptoms (VMS, or hot flashes) plague millions of reproductive age men and women who have natural or iatrogenic loss of sex steroid production. Many affected individuals are left without treatment options because of contraindications to hormone replacement therapy and the lack of equally effective non-hormonal alternatives. Moreover, development of safer, more effective therapies has been stymied by the lack of an animal model that recapitulates the hot flash phenomenon and enables direct testing of hypotheses regarding the pathophysiology underlying hot flashes...
May 22, 2017: Endocrinology
https://www.readbyqxmd.com/read/28526335/the-spider-toxin-ph%C3%AE-1%C3%AE-recombinant-possesses-strong-analgesic-activity
#19
Flavia Karine Rigo, Gabriela Trevisan, Samira Dal-Toé De Prá, Marta Nascimento Cordeiro, Marcia Helena Borges, Juliana Figueiredo Silva, Flavia Viana Santa Cecilia, Alessandra Hubner de Souza, Gabriela de Oliveira Adamante, Alessandra Marcon Milioli, Célio José de Castro Junior, Juliano Ferreira, Marcus Vinicius Gomez
The native Phα1β - a Voltage-Gated Calcium Channel (VGCC) blocker - and its Recombinant Version - were both tested in rodent pain models with an intraplantar injections of capsaicin or formalin, a chronic constriction injury, and melanoma cancer related pain. The formalin nociceptive behaviour in the neurogenic phase was not affected by the toxin pre-treatments, while in the inflammatory phase, Phα1β and the Recombinant form caused a significant reduction. The nociception that was triggered by capsaicin, an agonist of the TRPV1 vanilloid receptor, was totally blocked by 100 pmol/site, i...
July 2017: Toxicon: Official Journal of the International Society on Toxinology
https://www.readbyqxmd.com/read/28515697/trpa1-channels-modify-trpv1-mediated-current-responses-in-dorsal-root-ganglion-neurons
#20
Takayoshi Masuoka, Makiko Kudo, Yuka Yamashita, Junko Yoshida, Noriko Imaizumi, Ikunobu Muramatsu, Matomo Nishio, Takaharu Ishibashi
The transient receptor potential vanilloid 1 (TRPV1) channel is highly expressed in a subset of sensory neurons in the dorsal root ganglia (DRG) and trigeminal ganglia of experimental animals, responsible for nociception. Many researches have revealed that some TRPV1-positive neurons co-express the transient receptor potential ankyrin 1 (TRPA1) channel whose activities are closely modulated by TRPV1 channel. However, it is less investigated whether the activities of TRPV1 channel are modulated by the presence of TRPA1 channel in primary sensory neurons...
2017: Frontiers in Physiology
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