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capsaicin receptor

Johann Hammer
OBJECTIVES: The diagnosis of functional dyspepsia (FD) is challenging due to the lack of reliable biological markers to support the diagnosis. We assessed the relevance of a previously validated simple test for chemical hypersensitivity in the setting of a gastrointestinal outpatient department. METHODS: A total of 224 outpatients who were referred for evaluation of gastrointestinal symptoms in the absence of alarm symptoms swallowed a capsule containing 0.75 mg capsaicin...
March 13, 2018: American Journal of Gastroenterology
Rafael Taeho Han, Han-Byul Kim, Young-Beom Kim, Kyungmin Choi, Gi Yeon Park, Pa Reum Lee, JaeHee Lee, Hye Young Kim, Chul-Kyu Park, Youngnam Kang, Seog Bae Oh, Heung Sik Na
Recent studies have provided several lines of evidence that peripheral administration of oxytocin induces analgesia in human and rodents. However, the exact underlying mechanism of analgesia still remains elusive. In the present study, we aimed to identify which receptor could mediate the analgesic effect of intraperitoneal injection of oxytocin and its cellular mechanisms in thermal pain behavior. We found that oxytocin-induced analgesia could be reversed by d(CH2 )5 [Tyr(Me)2 ,Dab5 ] AVP, a vasopressin-1a (V1a) receptor antagonist, but not by desGly-NH2 -d(CH2 )5 [DTyr2 , Thr4 ]OVT, an oxytocin receptor antagonist...
March 2018: Korean Journal of Physiology & Pharmacology
Sung Eun Wang, Seung Yeon Ko, Yong-Seok Kim, Sungsin Jo, Seung Hoon Lee, Sung Jun Jung, Hyeon Son
Transient receptor potential vanilloid 1 (TRPV1) affects mood and neuroplasticity in the brain, where its role is poorly understood. In the present study we investigated whether capsaicin (8-methyl-N-vanillyl-trans-6-nonenamide), an agonist of TRPV1, induced chromatin remodeling and thereby altered gene expression related to synaptic plasticity. We found that capsaicin treatment resulted in upregulation of histone deacetylase 2 (HDAC2) in the mouse hippocampus and HDAC2 was enriched at Psd95, synaptophysin, GLUR1, GLUR2 promoters...
March 9, 2018: Experimental & Molecular Medicine
Justyna Maliszewska, Sonia Marcinkowska, Anna Nowakowska, Hanna Kletkiewicz, Justyna Rogalska
Some natural alkaloids, e.g. capsaicin and camphor, are known to induce a desensitization state, causing insensitivity to pain or noxious temperatures in mammals by acting on TRP receptors. Our research, for the first time, demonstrated that a phenomenon of pharmacological blockade of heat sensitivity may operate in American cockroach, Periplaneta americana (L.). We studied the escape reaction time from 50°C for American cockroaches exposed to multiple doses of different drugs affecting thermo-TRP. Capsaicin, capsazepine, and camphor induced significant changes in time spent at noxious ambient temperatures...
2018: PloS One
E Sjögren, T Kullenberg, B Jonzon, M Segerdahl, O Stålberg, M M Halldin, A K Sundgren-Andersson
BACKGROUND: The transient receptor potential cation channel subfamily V 1 (TRPV1) is involved in nociception and has thus been of interest for drug developers, as a target for novel analgesics. However, several oral TRPV1 antagonists have failed in development, and novel approaches to target TRPV1 with innovative chemistry are needed. METHOD: This work describes an intradermal microdosing approach in humans for pharmacodynamic deductions and pharmacological profiling of compounds...
March 5, 2018: European Journal of Pain: EJP
Shunsuke Nakamori, Jun Takahashi, Sumiko Hyuga, Toshiko Tanaka-Kagawa, Hideto Jinno, Masashi Hyuga, Takashi Hakamatsuka, Hiroshi Odaguchi, Yukihiro Goda, Toshihiko Hanawa, Yoshinori Kobayashi
The article Ephedra Herb extract activates/desensitizes transient receptor potential vanilloid 1 and reduces capsaicin-induced pain, written by Shunsuke Nakamori, Jun Takahashi, Sumiko Hyuga, Toshiko Tanaka-Kagawa, Hideto Jinno, Masashi Hyuga, Takashi Hakamatsuka, Hiroshi Odaguchi, Yukihiro Goda, Toshihiko Hanawa and Yoshinori Kobayashi, was originally published Online First without open access. After publication in volume 71, issue 1, page 105-113 the author decided to opt for Open Choice and to make the article an open access publication...
March 1, 2018: Journal of Natural Medicines
Daichi Utsumi, Kenjiro Matsumoto, Takuya Tsukahara, Kikuko Amagase, Makoto Tominaga, Shinichi Kato
Transient receptor potential (TRP) vanilloid 1 (TRPV1) and TRP ankyrin 1 (TRPA1), which are non-selective cation channels, play important roles in the sensation of pain. This study investigated the roles of TRPV1 and TRPA1 in dextran sulfate sodium (DSS)-induced murine colitis. DSS (2%) administered for 7 days caused severe colitis that was significantly less severe in TRPV1-deficient (TRPV1KO) and TRPA1-deficient (TRPA1KO) mice than that in wild-type (WT) mice. Similar colitis attenuations were observed in TRPV1KO and TRPA1KO mice but not in WT mice that had been transplanted with bone marrow cells from WT, TRPA1KO, or TRPV1KO mice...
February 8, 2018: Journal of Pharmacological Sciences
Doris Lam, Zeinab Momeni, Michael Theaker, Santosh Jagadeeshan, Yasuhiko Yamamoto, Juan P Ianowski, Verónica A Campanucci
Diabetes mellitus is associated with sensory abnormalities, including exacerbated responses to painful (hyperalgesia) or non-painful (allodynia) stimuli. These abnormalities are symptoms of diabetic peripheral neuropathy (DPN), which is the most common complication that affects approximately 50% of diabetic patients. Yet, the underlying mechanisms linking hyperglycemia and symptoms of DPN remain poorly understood. The transient receptor potential vanilloid 1 (TRPV1) channel plays a central role in such sensory abnormalities and shows elevated expression levels in animal models of diabetes...
2018: PloS One
Jonathan E Harms, Audrey J Stone, Marc P Kaufman
Patients with peripheral artery disease show an exaggerated pressor response to mild exercise, an effect attributable to the exercise pressor reflex, whose afferent arm is comprised of the thinly myelinated group III and unmyelinated group IV afferents. Previously, we found that DAMGO, a μ opioid agonist injected into the femoral artery, attenuated the exaggerated exercise pressor reflex in rats with ligated femoral arteries, a preparation which simulates the blood flow patterns to muscle that is seen in patients with PAD...
February 21, 2018: Journal of Neurophysiology
Tobias M Backes, Oliver G Rössler, Xin Hui, Carsten Grötzinger, Peter Lipp, Gerald Thiel
Transient receptor potential vanilloid 1 (TRPV1) channels were originally described as the receptors of capsaicin, the main constituent of hot chili pepper. The biological functions of TRPV1 channels include pain sensation and inflammatory thermal hyperalgesia. Here, we show that stimulation of HEK293 cells expressing TRPV1 channels (H2C1 cells) with capsaicin or the TRPV1 ligand resiniferatoxin activated transcription mediated by the transcription factor AP-1. No cell death was occurring under these experimental conditions...
February 13, 2018: Biochemical Pharmacology
Dinesh Thapa, Elizabeth A Cairns, Anna-Maria Szczesniak, James T Toguri, Meggie D Caldwell, Melanie E M Kelly
Background and Purpose: Corneal injury can result in dysfunction of corneal nociceptive signaling and corneal sensitization. Activation of the endocannabinoid system has been reported to be analgesic and anti-inflammatory. The purpose of this research was to investigate the antinociceptive and anti-inflammatory effects of cannabinoids with reported actions at cannabinoid 1 (CB1 R) and cannabinoid 2 (CB2 R) receptors and/or noncannabinoid receptors in an experimental model of corneal hyperalgesia. Methods: Corneal hyperalgesia (increased pain response) was generated using chemical cauterization of the corneal epithelium in wild-type (WT) and CB2 R knockout (CB2 R-/- ) mice...
2018: Cannabis and Cannabinoid Research
M P Pereira, H Lüling, A Dieckhöfer, S Steinke, C Zeidler, K Agelopoulos, S Ständer
BACKGROUND: Topical capsaicin shows efficacy in the treatment of brachioradial pruritus, however its mechanisms of action remain unclear. OBJECTIVE: The effect of capsaicin on the epidermis (i.e. peripheral expression of non-neuronal sensory receptors on keratinocytes, morphological changes in innervation) is still unknown. We aimed to investigate the effect of topical capsaicin on keratinocyte expression of TRP channels and on the intraepidermal nerve fibre density (IENFD) in patients with brachioradial pruritus...
February 10, 2018: Journal of the European Academy of Dermatology and Venereology: JEADV
Valerie B O'Leary, Marie O'Connell, Inga Antyborzec, Vasilis Ntziachristos, J Oliver Dolly, Saak V Ovsepian
Acute and chronic trigeminal (TG) neuropathies are the cause of considerable distress, with limited treatments available at present. Nociceptive neurons enriched with the vanilloid type 1 receptor (VR1) partake in pain sensation and sensitization in the TG system. While VR1 blockers with anti-nociceptive potential are of substantial medical interest, their use remains limited due to poor selectivity and lack of cell-targeting capabilities. This study describes a methodology for the alleviation of nociception via targeted depletion of VR1 in TG sensory neurons in rats...
February 9, 2018: Neurotherapeutics: the Journal of the American Society for Experimental NeuroTherapeutics
Hjalte H Andersen, Antoinette I M van Laarhoven, Frederik D Justesen, Jacob B Pedersen, Laurits L Sørensen, Line P Jensen, Lars Arendt-Nielsen
Specially designed transcutaneous electrical stimulation paradigms can be used to provoke experimental itch. However, it is unclear which primary afferent fibers are activated and whether they represent pathophysiologically relevant, C-fiber mediated itch. Since low-threshold mechano-receptors have recently been implicated in pruriception we aimed to characterize the peripheral primary afferent subpopulation conveying electrically evoked itch in humans (50Hz stimulation, 100μs square pulses, stimulus-response function to graded stimulus intensity)...
February 14, 2018: Neuroscience Letters
Luigino Calzetta, Paola Rogliani, Elena Pistocchini, Maurizio Mattei, Giuseppe Cito, Pietro Alfonsi, Clive Page, Maria Gabriella Matera
Recurrent airway obstruction (RAO) is a main characteristic of horses with severe equine asthma syndrome. The presence of bacterial lipopolysaccharide (LPS) in the airways of horses is thought to play a crucial role in the clinical expression of this disorder. This study pharmacologically characterized the effect of LPS on the responsiveness of equine bronchial tissue. Equine isolated bronchi were incubated overnight with LPS (0.1-100 ng/ml) and then stimulated by electrical field stimulation (EFS). The role of capsaicin sensitive-sensory nerves (capsaicin desensitization treatment), neurokinin-2 (NK2 ) receptors (blocked by GR159897), transient receptor potential vanilloid type 1 receptors (TRPV1; blocked by SB366791), and neurokinin A (NKA) were investigated...
January 30, 2018: Pulmonary Pharmacology & Therapeutics
Andrew M Moon, Sarah A Buckley, Nicholas M Mark
Cannabinoid hyperemesis syndrome (CHS) is a clinical entity in which marijuana users develop nausea, vomiting, and abdominal pain that improves with hot water bathing or cannabis cessation. Previous models suggest that CHS arises solely from the derangement of cannabinoid receptor type 1 signaling. However, involvement of transient receptor potential vanilloid subtype 1 (TRPV1) receptor, which is activated by marijuana, capsaicin, and heat, could fill gaps in existing models, including the enigmatic role of hot water bathing...
2018: ACG Case Reports Journal
Miguel Ortíz-Rentería, Rebeca Juárez-Contreras, Ricardo González-Ramírez, León D Islas, Félix Sierra-Ramírez, Itzel Llorente, Sidney A Simon, Marcia Hiriart, Tamara Rosenbaum, Sara L Morales-Lázaro
The Transient Receptor Potential Vanilloid 1 (TRPV1) ion channel is expressed in nociceptors where, when activated by chemical or thermal stimuli, it functions as an important transducer of painful and itch-related stimuli. Although the interaction of TRPV1 with proteins that regulate its function has been previously explored, their modulation by chaperones has not been elucidated, as is the case for other mammalian TRP channels. Here we show that TRPV1 physically interacts with the Sigma 1 Receptor (Sig-1R), a chaperone that binds progesterone, an antagonist of Sig-1R and an important neurosteroid associated to the modulation of pain...
February 13, 2018: Proceedings of the National Academy of Sciences of the United States of America
E Sjögren, M M Halldin, O Stålberg, A K Sundgren-Andersson
BACKGROUND: The transient receptor potential vanilloid receptor 1 (TRPV1) is a nonselective cation channel involved in the mediation of peripheral pain to the central nervous system. As such, the TRPV1 is an accessible molecular target that lends itself well to the understanding of nociceptive signalling. This study encompasses preclinical investigations of three molecules with the prospect to establish them as suitable analgesic model compounds in human intradermal pain relief studies...
January 26, 2018: European Journal of Pain: EJP
J B Lindström, N T Pierce, M I Latz
Transient receptor potential (TRP) ion channels are common components of mechanosensing pathways, mainly described in mammals and other multicellular organisms. To gain insight into the evolutionary origins of eukaryotic mechanosensory proteins, we investigated the involvement of TRP channels in mechanosensing in a unicellular eukaryotic protist, the dinoflagellate Lingulodinium polyedra. BLASTP analysis of the protein sequences predicted from the L. polyedra transcriptome revealed six sequences with high similarity to human TRPM2, TRPM8, TRPML2, TRPP1, and TRPP2; and characteristic TRP domains were identified in all sequences...
October 2017: Biological Bulletin
Kelsey M Nation, Milena De Felice, Pablo I Hernandez, David W Dodick, Volker Neugebauer, Edita Navratilova, Frank Porreca
The response of diffuse noxious inhibitory controls (DNIC) is often decreased, or lost, in stress-related functional pain syndromes. Because the dynorphin/kappa opioid receptor (KOR) pathway is activated by stress, we determined its role in DNIC using a model of stress-induced functional pain. Male, Sprague-Dawley rats were primed for 7 days with systemic morphine resulting in opioid-induced hyperalgesia. Fourteen days after priming, when hyperalgesia was resolved, rats were exposed to environmental stress and DNIC was evaluated by measuring hind paw response threshold to noxious pressure (test stimulus) after capsaicin injection in the forepaw (conditioning stimulus)...
January 23, 2018: Pain
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