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Dong Fang et al.
Pain, 156(6), 1124-1144 (2015-03-17)
Primary and metastatic cancers that affect bone are frequently associated with severe and intractable pain. The mechanisms underlying the pathogenesis of bone cancer pain still remain largely unknown. Previously, we have reported that sensitization of primary sensory dorsal root ganglion
The heat is on: does direct application of capsaicin to autonomic nerves produce a specific deafferentation?
Helen E Raybould
The Journal of physiology, 591(6), 1405-1405 (2013-03-19)
Xinying Jia et al.
FEBS letters, 588(17), 3047-3054 (2014-06-17)
The airway epithelium is exposed to a range of irritants in the environment that are known to trigger inflammatory response such as asthma. Transient receptor potential vanilloid 1 (TRPV1) is a Ca(2+)-permeable cation channel critical for detecting noxious stimuli by
Dong Hoon Shin et al.
Experimental & molecular medicine, 40(5), 486-494 (2008-11-06)
Capsaicin (trans-8-methyl-N-vanillyl-6-nonenamide), the major pungent ingredient of red pepper, has been reported to possess anti-carcinogenic and anti-mutagenic activities. In this study, the anti-migration activity of capsaicin on highly metastatic B16-F10 melanoma cells was investigated. Capsaicin significantly inhibited the migration of
Yoshihisa Ogawa et al.
Bioorganic & medicinal chemistry letters, 20(7), 2111-2114 (2010-03-17)
The effect of essential oils, such as raspberry ketone, on androgen (AR) receptor was investigated using a MDA-kb2 human breast cancer cell line for predicting potential AR activity. Among them, eugenol had the highest AR antagonistic activity with its IC(50)
Wagner Hummig et al.
Journal of oral & facial pain and headache, 28(4), 350-359 (2014-10-28)
To assess the analgesic effect of pregabalin in orofacial models of acute inflammatory pain and of persistent pain associated with nerve injury and cancer, and so determine its effectiveness in controlling orofacial pains having different underlying mechanisms. Orofacial capsaicin and
Alec R Nickolls et al.
Cell reports, 30(3), 932-946 (2020-01-23)
Efficient and homogeneous in vitro generation of peripheral sensory neurons may provide a framework for novel drug screening platforms and disease models of touch and pain. We discover that, by overexpressing NGN2 and BRN3A, human pluripotent stem cells can be transcriptionally
Evan E Lebovitz et al.
Molecular pain, 8, 70-70 (2012-09-25)
The prevalence of long-term opiate use in treating chronic non-cancer pain is increasing, and prescription opioid abuse and dependence are a major public health concern. To explore alternatives to opioid-based analgesia, the present study investigates a novel allosteric pharmacological approach
Natalie A Hawryluk et al.
Bioorganic & medicinal chemistry letters, 20(23), 7137-7141 (2010-10-16)
Utilization of a tetrahydro-pyrimdoazepine core as a bioisosteric replacement for a piperazine-urea resulted in the discovery a novel series of potent antagonists of TRPV1. The tetrahydro-pyrimdoazepines have been identified as having good in vitro and in vivo potency and acceptable
X Gao et al.
Neurogastroenterology and motility : the official journal of the European Gastrointestinal Motility Society, 27(12), 1817-1830 (2015-10-16)
Previous studies have demonstrated the efficacy of somatic stimulation for patients with gastrointestinal motility disorders. However, little effort has been made to investigate the effects of acupuncture on colonic motility, particularly in pathological conditions. The precise mechanism employed in the
Thais Biondino Sardella Giorno et al.
Pharmacology, biochemistry, and behavior, 135, 13-19 (2015-05-20)
Convolutamydine A has been shown to develop a significant antinociceptive effect. Here we demonstrated that new analogues (5-iodo-3-(2-oxopropyl)-3-hydroxy-2-oxindole (5-Iisa), 5-fluoro-3-(2-oxopropyl)-3-hydroxy-2-oxindole (5-Fisa), 5-chloro-3-(2-oxopropyl)-3-hydroxy-2-oxindole (5-Clisa) and 5-methyl-3-(2-oxopropyl)-3-hydroxy-2-oxindole (5-Meisa)), at 0.1-10mg/kg doses, have significant peripheral and central antinociceptive effects in thermal and chemical
Björn Rathsman et al.
Diabetologia, 57(8), 1703-1710 (2014-05-08)
We investigated skin microcirculation and its association with HbA1c and the incidence of ischaemic foot ulcer in patients with type 1 diabetes formerly randomised (1982-1984) to intensified conventional treatment (ICT) or standard treatment (ST) with insulin for a mean of
Clive Gentry et al.
Scientific reports, 5, 12771-12771 (2015-08-01)
Acetaminophen (APAP) is an effective antipyretic and one of the most commonly used analgesic drugs. Unlike antipyretic non-steroidal anti-inflammatory drugs, APAP elicits hypothermia in addition to its antipyretic effect. Here we have examined the mechanisms responsible for the hypothermic activity
Seungwon Choi et al.
Neuron, 78(5), 869-880 (2013-06-15)
Animals undergo periods of behavioral quiescence and arousal in response to environmental, circadian, or developmental cues. During larval molts, C. elegans undergoes a period of profound behavioral quiescence termed lethargus. Locomotion quiescence during lethargus was abolished in mutants lacking a
Stefano Evangelista
Progress in drug research. Fortschritte der Arzneimittelforschung. Progres des recherches pharmaceutiques, 68, 259-276 (2014-06-20)
Calcitonin gene-related peptide (CGRP), a 37 aminoacid-residue peptide, is a marker of afferent fibers in the upper gastrointestinal tract, being almost completely depleted following treatment with the selective neurotoxin capsaicin that targets these fibers via transient receptor potential vanilloid type-1
Johannes Wohlrab et al.
Skin pharmacology and physiology, 28(2), 65-74 (2014-10-04)
Epicutaneous application of capsaicin causes a long-lasting analgesic effect by binding to the membrane transient receptor potential vanilloid 1 (TRPV1) on mechanoheat-sensitive C and Aδ fibres, changing axonal integrity and inhibiting neurogenic inflammatory processes. To date, no information is available
David Acton et al.
Cell reports, 28(3), 625-639 (2019-07-18)
Acute itch can be generated by either chemical or mechanical stimuli, which activate separate pathways in the periphery and spinal cord. While substantial progress has been made in mapping the transmission pathway for chemical itch, the central pathway for mechanical
Timea Bencsik et al.
Pharmacology, 96(1-2), 86-89 (2015-07-15)
Piperine (P), a sensory stimulant in black pepper, is an agonist on TRPV1 receptors. Earlier work has showed capsaicin-sensitive and -insensitive mechanisms of the contractile action of P on the intestine. The current isolated organ study in the guinea-pig ileum
Kinga Sałat et al.
Pharmacology, biochemistry, and behavior, 122, 173-181 (2014-04-15)
Anticancer drugs - oxaliplatin (OXPT) and paclitaxel (PACLI) cause painful peripheral neuropathy activating Transient Receptor Potential (TRP) channels. Here we investigated the influence of 3-[4-(3-trifluoromethyl-phenyl)-piperazin-1-yl]-dihydrofuran-2-one (LPP1) and pregabalin on nociceptive thresholds in neuropathic pain models elicited by these drugs. Pharmacokinetics
Pedro L Martinez-Espinosa et al.
eLife, 4 (2015-11-13)
Two mammalian genes, Kcnt1 and Kcnt2, encode pore-forming subunits of Na(+)-dependent K(+) (KNa) channels. Progress in understanding KNa channels has been hampered by the absence of specific tools and methods for rigorous KNa identification in native cells. Here, we report
Michael J M Fischer et al.
Pflugers Archiv : European journal of physiology, 466(12), 2229-2241 (2014-03-20)
Transient receptor potential cation channel, subfamily V, member 1 (TRPV1) plays a key role in sensing environmental hazards and in enhanced pain sensation following inflammation. A considerable proportion of TRPV1-expressing cells also express transient receptor potential cation channel, subfamily A
Complex generalized instead of complex regional?
Tanja Schlereth et al.
Anesthesiology, 120(5), 1078-1079 (2014-03-14)
Long Zheng et al.
Oncology reports, 34(2), 1027-1034 (2015-06-18)
Capsaicin, a novel antitumor agent extracted from chili peppers, has been proven to induce growth inhibition in various types of cancer including prostate cancer. However, the detailed mechanisms remain largely undiscovered. In the present study, we explored the regulation of
M Couto et al.
Journal of investigational allergology & clinical immunology, 23(5), 289-301 (2013-11-23)
A high parasympathetic tone leading to bronchoconstriction and neurogenic inflammation is thought to have a major role in the pathogenesis of asthma. Transient receptor potential vanilloid 1 (TRPV1) is the hub of almost all neuronal inflammatory signaling pathways. A critical
Howard Smith et al.
Progress in drug research. Fortschritte der Arzneimittelforschung. Progres des recherches pharmaceutiques, 68, 129-146 (2014-06-20)
The TRPV1 receptor is known to play a role in nociceptive transmission in multiple organ systems, usually in response to the pain of inflammation. TRPV1 antagonism has so far shown limited benefit in antinociception. Capsaicin, a TRPV1 agonist, has been
Louisa Pettinger et al.
The Journal of neuroscience : the official journal of the Society for Neuroscience, 33(26), 10762-10771 (2013-06-28)
Analgesics targeting the δ-opioid receptor (DOR) may lead to fewer side effects than conventional opioid drugs, which mainly act on μ-opioid receptors (MOR), because of the less abundant expression of DOR in the CNS compared with MOR. Analgesic potential of
Azucena Perez-Burgos et al.
The Journal of physiology, 593(17), 3943-3957 (2015-06-19)
Certain probiotic bacteria have been shown to reduce distension-dependent gut pain, but the mechanisms involved remain obscure. Live luminal Lactobacillus reuteri (DSM 17938) and its conditioned medium dose dependently reduced jejunal spinal nerve firing evoked by distension or capsaicin, and
Corinna Kimball et al.
Molecular pharmacology, 88(1), 131-138 (2015-05-09)
The environmental irritant chloroform, a naturally occurring small volatile organohalogen, briefly became the world's most popular volatile general anesthetic (VGA) before being abandoned because of its low therapeutic index. When chloroform comes in contact with skin or is ingested, it
L Romero et al.
British journal of pharmacology, 166(8), 2289-2306 (2012-03-13)
The sigma-1 (σ(1) ) receptor is a ligand-regulated molecular chaperone that has been involved in pain, but there is limited understanding of the actions associated with its pharmacological modulation. Indeed, the selectivity and pharmacological properties of σ(1) receptor ligands used
Yasutada Akiba et al.
Digestive diseases and sciences, 60(4), 858-867 (2015-02-24)
Corticotropin-releasing factor (CRF) peptides exert profound effects on the secretomotor function of the gastrointestinal tract. Nevertheless, despite the presence of CRF peptides and receptors in colonic tissue, their influence on colonic blood flow (CBF) is unknown. To determine the effect
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