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capsaicin receptor

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https://www.readbyqxmd.com/read/28439004/endocannabinoid-system-acts-as-a-regulator-of-immune-homeostasis-in-the-gut
#1
Nandini Acharya, Sasi Penukonda, Tatiana Shcheglova, Adam T Hagymasi, Sreyashi Basu, Pramod K Srivastava
Endogenous cannabinoids (endocannabinoids) are small molecules biosynthesized from membrane glycerophospholipid. Anandamide (AEA) is an endogenous intestinal cannabinoid that controls appetite and energy balance by engagement of the enteric nervous system through cannabinoid receptors. Here, we uncover a role for AEA and its receptor, cannabinoid receptor 2 (CB2), in the regulation of immune tolerance in the gut and the pancreas. This work demonstrates a major immunological role for an endocannabinoid. The pungent molecule capsaicin (CP) has a similar effect as AEA; however, CP acts by engagement of the vanilloid receptor TRPV1, causing local production of AEA, which acts through CB2...
April 24, 2017: Proceedings of the National Academy of Sciences of the United States of America
https://www.readbyqxmd.com/read/28438981/acute-inflammation-reveals-gabaa-receptor-mediated-nociception-in-mouse-dorsal-root-ganglion-neurons-via-pge2-receptor-4-signaling
#2
In Jeong Jang, Alexander J Davies, Nozomi Akimoto, Seung Keun Back, Pa Reum Lee, Heung Sik Na, Hidemasa Furue, Sung Jun Jung, Yong Ho Kim, Seog Bae Oh
Gamma-aminobutyric acid (GABA) depolarizes dorsal root ganglia (DRG) primary afferent neurons through activation of Cl(-) permeable GABAA receptors but the physiologic role of GABAA receptors in the peripheral terminals of DRG neurons remains unclear. In this study, we investigated the role of peripheral GABAA receptors in nociception using a mouse model of acute inflammation. In vivo, peripheral administration of the selective GABAA receptor agonist muscimol evoked spontaneous licking behavior, as well as spinal wide dynamic range (WDR) neuron firing, after pre-conditioning with formalin but had no effect in saline-treated mice...
April 2017: Physiological Reports
https://www.readbyqxmd.com/read/28428628/inflammatory-and-neuropathic-nociception-is-preserved-in-gpr55-knockout-mice
#3
Lawrence M Carey, Tannia Gutierrez, Liting Deng, Wan-Hung Lee, Ken Mackie, Andrea G Hohmann
The G-protein coupled receptor GPR55 has been postulated to serve as a novel cannabinoid receptor. A previous report indicated that GPR55 knockout mice fail to develop mechanical hyperalgesia, suggesting a pro-nociceptive role for GPR55 in the control of nociceptive responding. However, GPR55 knockout mice remain incompletely characterized in models of pathological pain. Here we provide a comprehensive assessment of responses of GPR55 knockout and wild-type mice to mechanical and thermal (heat, cold) stimulation in multiple, mechanistically distinct models of inflammatory and neuropathic pain...
April 20, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28424466/the-role-of-the-brown-adipose-tissue-in-%C3%AE-3-adrenergic-receptor-activation-induced-sleep-metabolic-and-feeding-responses
#4
Éva Szentirmai, Levente Kapás
Brown adipose tissue (BAT) is regulated by the sympathetic nervous system via β3-adrenergic receptors (β3-AR). Here we tested the hypothesis that pharmacological stimulation of β3-ARs leads to increased sleep in mice and if this change is BAT dependent. In wild-type (WT) animals, administration of CL-316,243, a selective β3-AR agonist, induced significant increases in non-rapid-eye movement sleep (NREMS) lasting for 4-10 h. Simultaneously, electroencephalographic slow-wave activity (SWA) was significantly decreased and body temperature was increased with a delay of 5-6 h...
April 19, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28392320/contrasting-effects-of-atp-and-adenosine-on-capsaicin-challenge-in-asthmatic-patients
#5
Ozen K Basoglu, Amir Pelleg, Sergei A Kharitonov, Peter J Barnes
BACKGROUND: Adenosine 5'-triphosphate (ATP) stimulates pulmonary vagal slow conducting C-fibres and fast conducting Aδ-fibres with rapidly adapting receptors (RARs). Pulmonary C-fibres but not RARs are also sensitive to capsaicin, a potent tussigenic agent in humans. Thus, the aim of this study was to determine the effects of ATP and its metabolite adenosine (given as adenosine 5'-monophosphate, AMP) on capsaicin challenge in asthmatic patients. METHODS: Cough (quantified as visual analogue scale, VAS), dyspnoea (quantified as Borg score), and FEV1 were quantified following bronchoprovocation using capsaicin, adenosine and ATP in healthy non-smokers (age 40±4y, 6 males), smokers (45±4y, 5 males) and asthmatic patients (37±3y, 5 males); n = 10 in each group...
April 6, 2017: Pulmonary Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/28374409/antinociceptive-effect-of-natural-and-synthetic-alkamides-involves-trpv1-receptors
#6
Vianey de la Rosa-Lugo, Macdiel Acevedo-Quiroz, Myrna Déciga-Campos, María Yolanda Rios
OBJECTIVE: To establish the role of TRPV1 receptor in the antinociceptive effect of natural alkamides (i.e. affinin, longipinamide A, longipenamide A and longipenamide B) isolated from Heliopsis longipes (A. Gray) S.F. Blake and some related synthetic alkamides (i.e. N-isobutyl-feruloylamide and N-isobutyl-dihydroferuloylamide). METHODS: The orofacial formalin test was used to assess the antinociceptive activity of natural (1-30 μg, orofacial region) and synthetic alkamides (0...
April 4, 2017: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/28373693/trpv1-temperature-activation-is-specifically-sensitive-to-strong-decreases-in-amino-acid-hydrophobicity
#7
Jason O Sosa-Pagán, Edwin S Iversen, Jörg Grandl
Several transient receptor potential (TRP) ion channels can be directly activated by hot or cold temperature with high sensitivity. However, the structures and molecular mechanism giving rise to their high temperature sensitivity are not fully understood. One hypothesized mechanism assumes that temperature activation is driven by the exposure of hydrophobic residues to solvent. This mechanism further predicts that residues are exposed to solvent in a coordinated fashion, but without necessarily being located in close proximity to each other...
April 3, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28366470/ascending-projections-of-nociceptive-neurons-from-trigeminal-subnucleus-caudalis-a-population-approach
#8
Hiroto Saito, Ayano Katagiri, Shinji Okada, Lou Mikuzuki, Asako Kubo, Tatsuro Suzuki, Kinuyo Ohara, Jun Lee, Nobuhito Gionhaku, Toshimitsu Iinuma, David A Bereiter, Koichi Iwata
Second-order neurons in trigeminal subnucleus caudalis (Vc) and upper cervical spinal cord (C1) are critical for craniofacial pain processing and project rostrally to terminate in: ventral posteromedial thalamic nucleus (VPM), medial thalamic nuclei (MTN) and parabrachial nuclei (PBN). The contribution of each region to trigeminal nociception was assessed by the number of phosphorylated extracellular signal-regulated kinase-immunoreactive (pERK-IR) neurons co-labeled with fluorogold (FG). The phenotype of pERK-IR neurons was further defined by the expression of neurokinin 1 receptor (NK1)...
March 31, 2017: Experimental Neurology
https://www.readbyqxmd.com/read/28360106/ca-2-and-calpain-mediate-capsaicin-induced-ablation-of-axonal-terminals-expressing-transient-receptor-potential-vanilloid-1
#9
Sheng Wang, Sen Wang, Jamila Asgar, John Joseph, Jin Y Ro, Feng Wei, James N Campbell, Man-Kyo Chung
Capsaicin is an ingredient in spicy peppers that produces burning pain by activating transient receptor potential vanilloid 1 (TRPV1), a Ca2+-permeable ion channel in nociceptors. Capsaicin also has been used as an analgesic, and its topical administration is approved for the treatment of certain pain conditions. The mechanisms underlying capsaicin-induced analgesia likely involve reversible ablation of nociceptor terminals. However, the mechanisms underlying these effects are not well understood. To visualize TRPV1-lineage axons, a genetically engineered mouse model was used in which a fluorophore is expressed under TRPV1 promoter...
March 30, 2017: Journal of Biological Chemistry
https://www.readbyqxmd.com/read/28352332/inhibitory-effect-of-salvia-plebeia-leaf-extract-on-ultraviolet-induced-photoaging-associated-ion-channels-and-enzymes
#10
You-Jin Chang, Dong-Ung Lee, Da Yeong Nam, Sung Min Cho, Seungug Hong, Joo Hyun Nam, Woo Kyung Kim
In traditional Korean/Asian medicine, Salvia plebeia R.Br. (S. plebeia) leaves are used to treat inflammatory diseases, including dermatitis, cough, asthma and toothache. Recently, S. plebeia leaves have been applied in skin care, as they promote skin lightening and elasticity. Therefore, the present study investigated the anti-aging effects of S. plebeia leaf methanolic extract and its fractions (dichloromethane, ethylacetate and n-butanol). The results of a whole-cell patch clamp analysis indicated that the methanolic extract mediated ultraviolet (UV)-induced photoaging-associated ion channels, transient receptor potential vanilloid 1 (TRPV1) and calcium release-activated calcium channel protein 1 (ORAI1) channel activity in HEK293T cells overexpressing TRPV1 or ORAI1 and STIM1...
February 2017: Experimental and Therapeutic Medicine
https://www.readbyqxmd.com/read/28337115/hplc-dad-analysis-antinociceptive-and-anti-inflammatory-properties-of-the-ethanolic-extract-of-hyptis-umbrosa-in-mice
#11
Klécia S Dos Anjos, Heitor G Araújo-Filho, Marcelo C Duarte, Vicente C O Costa, Josean F Tavares, Marcelo S Silva, Jackson R G S Almeida, Nathália A C Souza, Larissa A Rolim, Irwin R A Menezes, Henrique D M Coutinho, Jullyana S S Quintans, Lucindo J Quintans-Júnior
Hyptis umbrosa (syn. Mesosphaerum sidifolium) (Lamiaceae Family) has been used to treat several conditions such as gastrointestinal disorders, skin infections, nasal congestion, fever and cramps. The objective of this study was to evaluate the chemical composition, analgesic and anti-inflammatory profiles of ethanol extract from leaves of Hyptis umbrosa (EEB). HPLC-DAD was used to determine the fingerprint chromatogram of the extract. Male Swiss mice were orally pretreated with EEB (100, 200 or 400 mg/kg; 60 min before initiating algesic stimulation) and antinociceptive activity was assessed using the acetic acid-induced writhing model, formalin test and hyperalgesia induced by glutamate or capsaicin...
2017: EXCLI journal
https://www.readbyqxmd.com/read/28336810/role-of-transient-receptor-potential-vanilloid-1-trpv1-in-the-modulation-of-airway-smooth-muscle-tone-and-calcium-handling
#12
Gene T Yocum, Jun Chen, Christine H Choi, Elizabeth A Townsend, Yi Zhang, Dingbang Xu, Xiao Wen Fu, Michael J Sanderson, Charles W Emala
Asthma is a common disorder characterized, in part, by airway smooth muscle (ASM) hyperresponsiveness. Transient receptor potential vanilloid 1 (TRPV1) is a non-selective cation channel expressed on airway nerve fibers that modulates afferent signals resulting in cough, and potentially bronchoconstriction. In the present study, the TRPV1 transcript was detected by RT-PCR in primary cultured human ASM cells, and the TRPV1 protein was detected in ASM of human trachea by immunohistochemistry. Proximity ligation assays suggest that TRPV1 is expressed in the sarcoplasmic reticulum membrane of human ASM cells in close association with sarco/endoplasmic reticulum Ca2+ ATPase 2...
March 23, 2017: American Journal of Physiology. Lung Cellular and Molecular Physiology
https://www.readbyqxmd.com/read/28324760/trpv1-agonism-inhibits-endothelial-cell-inflammation-via-activation-of-enos-no-pathway
#13
Youping Wang, Lin Cui, Hui Xu, Suxiao Liu, Feiyun Zhu, Fengna Yan, Si Shen, Mingjun Zhu
BACKGROUND AND AIMS: Transient receptor potential vanilloid type 1 channel (TRPV1) is found to be expressed in endothelial cells (ECs) and activate endothelial nitric oxide synthase (eNOS). Recent studies implicate TRPV1 in attenuating inflammatory responses. However, the mechanisms underlying the beneficial effects remain unclear. In this study, we investigated whether TRPV1 suppresses inflammatory responses of ECs via eNOS/NO pathway. METHODS: Human umbilical vein endothelial cells (HUVECs) and renal microvascular endothelial cells (MVECs) isolated from deoxycorticosterone (DOCA)-salt hypertensive mice were cultured in the presence of capsaicin (CAP, a specific TRPV1 agonist) with or without the specific inhibitor of TRPV1, NOS, or Ca(2+)-dependent phosphatidylinositol 3-kinase (PI3K)/Akt pathway, before lipopolysaccharide (LPS) stimulation...
May 2017: Atherosclerosis
https://www.readbyqxmd.com/read/28322839/derivatives-of-furanditerpenes-from-pterodon-genus-pharmacological-studies-disclose-their-potential-as-chronic-pain-relief-in-mice
#14
Humberto M Spindola, Rogério Grando, Mariana C Figueiredo, Rosana Basting, N C A Queiroz, Ângelo de Fátima, João E de Carvalho, Zaijie J Wang, M A Foglio
Pterodon genus fruits are commercially available at the Brazilian medicinal market used in folk medicine due to their anti-inflammatory, analgesic, and anti-rheumatic effects. Previous studies demonstrated that furanditerpenes possessing vouacapan skeleton, isolated from Pterodon genus, possess expressive antinociceptive activities, with promising moiety for the development of new analgesic products. The antinociceptive properties of compounds 6α,7β-6α-hidroxivouacapan-7β-17β-lactone (HVL) and 6α-oxovouacapan-7β-17β-lactone (OVL), semi-synthetic analogues of furanditerpenes previously reported as analgesic agents were evaluated on animal experimental models (Spindola et al...
June 5, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28321335/quantitative-thermal-testing-profiles-as-a-predictor-of-treatment-response-to-topical-capsaicin-in-patients-with-localized-neuropathic-pain
#15
A Serrano, D Torres, M Veciana, C Caro, J Montero, V Mayoral
There are no reliable predictors of response to treatment with capsaicin. Given that capsaicin application causes heat sensation, differences in quantitative thermal testing (QTT) profiles may predict treatment response. The aim of this study was to determine whether different QTT profiles could predict treatment outcomes in patients with localized peripheral neuropathic pain (PeLNP). We obtained from medical records QTT results and treatment outcomes of 55 patients treated between 2010 and 2013. Warm sensation threshold (WST) and heat pain threshold (HPT) values were assessed at baseline at the treatment site and in the asymptomatic, contralateral area...
2017: Pain Research and Treatment
https://www.readbyqxmd.com/read/28319947/effects-of-capsaicin-on-older-patients-with-oropharyngeal-dysphagia-a-double-blind-placebo-controlled-crossover-study
#16
Rui Nakato, Noriaki Manabe, Sayako Shimizu, Kozo Hanayama, Akiko Shiotani, Jiro Hata, Ken Haruma
BACKGROUND/AIMS: The standard of care for older patients with oropharyngeal dysphagia (OD) is poor. Stimulation of transient receptor potential vanilloid 1 might become a pharmacological strategy for these patients. This study aimed to compare the therapeutic effect of film food containing 0.75 µg of capsaicin in these patients. METHODS: In a crossover, randomized trial, 49 patients with OD were provided capsaicin or identical placebo at least 7 days apart. Patients' reported symptoms during repeated swallowing, the volume, pH and substance P (SP) concentrations in saliva, and cervical esophageal wall motion evaluated by ultrasonographic tissue Doppler imaging were obtained before and after capsaicin or placebo administration...
March 21, 2017: Digestion
https://www.readbyqxmd.com/read/28295390/mechanically-sensitive-a%C3%AE-nociceptors-that-innervate-bone-marrow-respond-to-changes-in-intra-osseous-pressure
#17
Sara Nencini, Jason Ivanusic
Whilst the sensory neurons and nerve terminals that innervate bone marrow have a morphology and molecular phenotype consistent with a role in nociception, little is known about their physiology or the mechanisms that generate and maintain bone pain. In the present study, we provide evidence that Aδ nociceptors that innervate the bone marrow respond to high threshold noxious mechanical stimulation, exhibit fatigue in response to prior stimulation, and in some cases can be sensitized by capsaicin. They can be classified on the basis of their response properties as either phasic-tonic units that appear to code for different intensities of intra-osseous pressure, or phasic units that code for the rate of change in intra-osseous pressure...
March 15, 2017: Journal of Physiology
https://www.readbyqxmd.com/read/28294062/warming-up-to-new-possibilities-with-the-capsaicin-receptor-trpv1-mtor-ampk-and-erythropoietin
#18
Kenneth Maiese
BACKGROUND: Transient receptor potential (TRP) channels are a superfamily of ion channels termed after the trp gene in Drosophila that are diverse in structure and control a wide range of biological functions including cell development and growth, thermal regulation, and vascular physiology. Of significant interest is the transient receptor potential cation channel subfamily V member 1 (TRPV1) receptor, also known as the capsaicin receptor and the vanilloid receptor 1, that is a non-selective cation channel sensitive to a host of external stimuli including capsaicin and camphor, venoms, acid/basic pH changes, and temperature...
March 13, 2017: Current Neurovascular Research
https://www.readbyqxmd.com/read/28291541/evidence-for-a-novel-neurohumoral-antinociceptive-mechanism-mediated-by-peripheral-capsaicin-sensitive-nociceptors-in-conscious-rats
#19
Gábor Pethő, Kata Bölcskei, Réka Füredi, Bálint Botz, Teréz Bagoly, Erika Pintér, János Szolcsányi
Stimulation of capsaicin-sensitive peripheral sensory nerve terminals induces remote anti-inflammatory effects throughout the body of anesthetized rats and guinea-pigs mediated by somatostatin. As somatostatin has also antinociceptive effects, the study aimed at investigating whether similar remote antinociceptive effects can be demonstrated in awake animals. In conscious rats, nociceptive nerve endings of the right hind paw decentralized by cutting the sciatic and saphenous nerves 18h before were chemically stimulated, and drop of the noxious heat threshold (heat hyperalgesia) induced by prior (18h before) plantar incision was measured on the contralateral, left hind paw using an increasing-temperature water bath...
February 10, 2017: Neuropeptides
https://www.readbyqxmd.com/read/28281854/capsaicin-pretreatment-reversed-pulmonary-arterial-hypertension-by-alleviating-inflammation-via-p38mapk-pathway
#20
Ying Xu, Qin Gu, Chen Qu
Purpose/Aim: Pulmonary arterial hypertension (PAH) is a lethal disease associated with pulmonary vascular remodeling as well as inflammation. As a kind of tachykinin secreted by nerves and inflammatory cells, substance P (SP) has been proved to be involved in the progression of PAH. Capsaicin can deplete substance P and provide benefits in PAH. However, the mechanism is still unclear. In this article, we aim to illustrate the possible mechanism involved in the process of capsaicin alleviating PAH. MATERIALS AND METHODS: A single injection of monocrotaline (MCT) to male Sprague-Dawley (SD) rats was conducted to induce PAH...
February 2017: Experimental Lung Research
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