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Nociceptive pain

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https://www.readbyqxmd.com/read/28324649/sulfonamides-as-selective-nav1-7-inhibitors-optimizing-potency-pharmacokinetics-and-metabolic-properties-to-obtain-atropisomeric-quinolinone-am-0466-that-affords-robust-in-vivo-activity
#1
Russell F Graceffa, Alessandro A Boezio, Jessica Able, Steven Altmann, Loren M Berry, Christiane M Boezio, John R Butler, Margaret Y Chu-Moyer, Melanie Cooke, Erin F DiMauro, Thomas A Dineen, Elma Feric Bojic, Robert S Foti, Robert T Fremeau, Angel Guzman-Perez, Hua Gao, Hakan Gunaydin, Hongbing Huang, Liyue Huang, Christopher Ilch, Michael Jarosh, Thomas Kornecook, Charles R Kreiman, Daniel S La, Joseph Ligutti, Benjamin Charles Milgram, Min-Hwa Jasmine Lin, Isaac E Marx, Hanh Nho Nguyen, Emily A Peterson, Gwen Rescourio, John Roberts, Laurie B Schenkel, Roman Shimanovich, Brian Andrew Sparling, John Stellwagen, Kristin Taborn, Karina R Vaida, Jean Wang, John T S Yeoman, Violeta L Yu, Dawn Zhu, Bryan D Moyer, Matthew M Weiss
Due to its strong genetic validation, NaV1.7 has attracted significant interest as a target for the treatment of pain. We have previously reported on a number of structurally distinct bicyclic heteroarylsulfonamides as NaV1.7 inhibitors that demonstrate high levels of selectivity over other NaV isoforms. Herein, we report the discovery and optimization of a novel series of atropisomeric quinolinone sulfonamide inhibitors of NaV1.7, which demonstrate nanomolar inhibition of NaV1.7 and exhibit high levels of selectivity over other sodium channel isoforms...
March 21, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28323508/nefopam-hydrochloride-loaded-microspheres-for-post-operative-pain-management-synthesis-physicochemical-characterization-and-in-vivo-evaluation
#2
Neelam Sharma, Sandeep Arora, Jitender Madan
Once-daily oral dosage of nefopam hydrochloride loaded sustained release microspheres (NPH-MS) was investigated as novel therapeutic strategy for post-operative pain management. Microspheres were synthesized using poly-3-hydroxybutyrate and poly-(ɛ-caprolactone) by double emulsion solvent evaporation technique. NPH-MS were characterized through FTIR, PXRD and SEM. In-vitro drug release study revealed sustained behavior till 24 h. Haemolysis was <5% which signified haemocompatibility of formulation. ED50 in rat tail-flick anti-nociceptive test was found ∼18...
March 21, 2017: Artificial Cells, Nanomedicine, and Biotechnology
https://www.readbyqxmd.com/read/28320042/calcium-channel-modulation-as-a-target-in-chronic-pain-control
#3
REVIEW
Ryan Patel, Carlota Montagut-Bordas, Anthony H Dickenson
Neuropathic pain remains poorly treated for large numbers of patients and little progress has been made in developing novel classes of analgesics. To redress this issue, ziconotide (Prialt(TM) ) was developed and approved as a first in class synthetic version of ω-conotoxin MVIIA, a Cav 2.2 peptide blocker. Unfortunately, the impracticalities of intrathecal delivery, low therapeutic index and severe neurological side effects associated with ziconotide has restricted its use to exceptional circumstances. Ziconotide exhibits no state or use dependent block of Cav 2...
March 20, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28318085/inflammatory-double-hit-model-of-temporomandibular-joint-disorder-with-elevated-ccl2-cxcl9-cxcl10-rantes-and-behavioural-hypersensitivity-in-tnfr1-r2-mice
#4
S L McIlwrath, R Nesemeier, F Ma, H S Oz, L Zhang, K N Westlund
BACKGROUND: Patients with temporomandibular joint disorders (TMD), reactive arthritis and rheumatoid arthritis often have combined etiology of hereditary and microenvironmental factors contributing to joint pain. Multiple clinical and animal studies indicate 'double-hit' inflammatory insults can cause chronic inflammation. The first inflammatory insult primes the immune system and subsequent insults elicit amplified responses. The present 'double hit' study produced a chronic orofacial pain model in mice with genetic deletion of both TNFα receptors (TNFR1/R2-/-), investigating the main nociceptive signalling pathways in comparisons to wild type mice...
March 20, 2017: European Journal of Pain: EJP
https://www.readbyqxmd.com/read/28315395/acute-intravenous-administration-of-dietary-constituent-theanine-suppresses-noxious-neuronal-transmission-of-trigeminal-spinal-nucleus-caudalis-in-rats
#5
Shiori Takehana, Yoshiko Kubota, Nobuo Uotsu, Kei Yui, Yoshihito Shimazu, Mamoru Takeda
Theanine is a non-dietary amino acid linked to the modulation of synaptic transmission in the central nervous system, although the acute effects of theanine in vivo, particularly on nociceptive transmission in the trigeminal system, remain to be determined. The present study investigated whether acute intravenous theanine administration to rats attenuates the excitability of wide dynamic range (WDR) spinal trigeminal nucleus caudalis (SpVc) neurons in response to nociceptive and non-nociceptive mechanical stimulation in vivo...
March 14, 2017: Brain Research Bulletin
https://www.readbyqxmd.com/read/28315341/low-doses-of-tizanidine-synergize-the-anti-nociceptive-and-anti-inflammatory-effects-of-ketorolac-or-naproxen-while-reducing-of-side-effects
#6
Selene I Patiño-Camacho, Myrna Déciga-Campos, Karla Beltrán-Villalobos, Dalia A Castro-Vidal, Rosa M Montiel-Ruiz, Francisco J Flores-Murrieta
The aim of the present study was to determine whether tizanidine, an alpha2-adrenoceptor agonist, is able to increase the anti-inflammatory and anti-nociceptive effects of naproxen and ketorolac with a low incidence of gastric injury and spontaneous activity in rats. The anti-inflammatory effect was assayed in a carrageenan test, and oral administration of tizanidine (ED40 = 0.94 ± 0.2mg/kg), naproxen (ED40 = 3.18 ± 0.4mg/kg), and ketorolac (ED40 = 16.4 ± 1.9mg/kg) showed a dose-dependent effect on inflammation...
March 14, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28315267/pharmacological-modulation-of-the-sigma-1-receptor-and-the-treatment-of-pain
#7
Manuel Merlos, Javier Burgueño, Enrique Portillo-Salido, Carlos Ramón Plata-Salamán, José Miguel Vela
There is a critical need for new analgesics acting through new mechanisms of action, which could increase the efficacy with respect to existing therapies and reduce their unwanted effects. Current preclinical evidence supports the modulatory role of sigma-1 receptors (σ1R) in nociception, mainly based on the pain-attenuated phenotype of σ1R knockout mice and on the antinociceptive effect exerted by σ1R antagonists on pains of different etiologies. σ1R is highly expressed in different pain areas of the CNS and the periphery (particularly dorsal root ganglia), and interacts and modulates the functionality of different receptors and ion channels ...
2017: Advances in Experimental Medicine and Biology
https://www.readbyqxmd.com/read/28306698/oral-application-of-magnesium-l-threonate-attenuates-vincristine-induced-allodynia-and-hyperalgesia-by-normalization-of-tumor-necrosis-factor-%C3%AE-nuclear-factor-%C3%AE%C2%BAb-signaling
#8
Ting Xu, Dai Li, Xin Zhou, Han-Dong Ouyang, Li-Jun Zhou, Hang Zhou, Hong-Mei Zhang, Xu-Hong Wei, Guosong Liu, Xian-Guo Liu
BACKGROUND: Antineoplastic agents, including vincristine, often induce neuropathic pain and magnesium deficiency clinically, but the causal link between them has not been determined. No drug is available for treating this form of neuropathic pain. METHODS: Injection of vincristine (0.1 mg · kg · day, intraperitoneally, for 10 days) was used to induce nociceptive sensitization, which was accessed with von Frey hairs and the plantar tester in adult male Sprague-Dawley rats...
March 17, 2017: Anesthesiology
https://www.readbyqxmd.com/read/28303458/calcitonin-gene-related-peptide-and-pain-a-systematic-review
#9
REVIEW
Wendy Sophie Schou, Sait Ashina, Faisal Mohammad Amin, Peter J Goadsby, Messoud Ashina
BACKGROUND: Calcitonin gene-related peptide (CGRP) is widely distributed in nociceptive pathways in human peripheral and central nervous system and its receptors are also expressed in pain pathways. CGRP is involved in migraine pathophysiology but its role in non-headache pain has not been clarified. METHODS: We performed a systematic literature search on PubMed, Embase and ClinicalTrials.gov for articles on CGRP and non-headache pain covering human studies including experimental studies and randomized clinical trials...
December 2017: Journal of Headache and Pain
https://www.readbyqxmd.com/read/28302538/protective-effects-of-garcinol-against-neuropathic-pain-evidence-from-in-vivo-and-in-vitro-studies
#10
Yi-Wei Wang, Xiang Zhang, Chun-Long Chen, Qing-Zhen Liu, Jia-Wen Xu, Qing-Qing Qian, Wei-Yan Li, Yan-Ning Qian
Neuroinflammatory processes have a vital role in the pathogenesis of neuropathic pain. Garcinol, harvested from Garcinia indica, is known to exert potent anti-inflammatory properties. Recent studies have indicated that Garcinol may inhibit activation of nuclear factor-κB (NF-κB) by inhibiting NF-κB/p65 acetylation. These findings prompted us to evaluate the protective effects of Garcinol in the lumbar fifth spinal nerve ligation (SNL)-induced rat model of neuropathic pain and Lipopolysaccharide(LPS)-stimulated primary cultured microglia...
March 13, 2017: Neuroscience Letters
https://www.readbyqxmd.com/read/28301400/the-role-of-calcitonin-gene-related-peptide-in-peripheral-and-central-pain-mechanisms-including-migraine
#11
Smriti Iyengar, Michael H Ossipov, Kirk W Johnson
Calcitonin gene-related peptide (CGRP) is a 37-amino acid peptide found primarily in the C and Aδ sensory fibers arising from the dorsal root and trigeminal ganglia, as well as the central nervous system. Calcitonin gene-related peptide was found to play important roles in cardiovascular, digestive, and sensory functions. Although the vasodilatory properties of CGRP are well documented, its somatosensory function regarding modulation of neuronal sensitization and of enhanced pain has received considerable attention recently...
April 2017: Pain
https://www.readbyqxmd.com/read/28300633/the-medullary-dorsal-reticular-nucleus-as-a-relay-for-descending-pronociception-induced-by-the-mglur5-in-the-rat-infralimbic-cortex
#12
Ana David-Pereira, Boriss Sagalajev, Hong Wei, Armando Almeida, Antti Pertovaara, Filipa Pinto-Ribeiro
Metabotropic glutamate receptor 5 (mGluR5) activation in the infralimbic cortex (IL) induces pronociceptive behavior in healthy and monoarthritic rats. Here we studied whether the medullary dorsal reticular nucleus (DRt) and the spinal TRPV1 are mediating the IL/mGluR5-induced spinal pronociception and whether the facilitation of pain behavior is correlated with changes in spinal dorsal horn neuron activity. For drug administrations, all animals had a cannula in the IL as well as a cannula in the DRt or an intrathecal catheter...
March 11, 2017: Neuroscience
https://www.readbyqxmd.com/read/28298760/the-effectiveness-of-intravenous-dexmedetomidine-on-perioperative-hemodynamics-analgesic-requirement-and-side-effects-profile-in-patients-undergoing-laparoscopic-surgery-under-general-anesthesia
#13
Vinayak Panchgar, Akshaya N Shetti, H B Sunitha, Vithal K Dhulkhed, A V Nadkarni
BACKGROUND: There is an upward surge in the use of laparoscopic surgeries due to various advantages when compared to open surgeries. Major advantages are, due to small incisions which are cosmetically acceptable and most of them are now daycare procedures. Problem of economic burden and hospital bed occupancy has been overcome with laparoscopic surgeries. All these advantages are not free from disadvantages, as hemodynamic changes such as hypertension; tachycardia and other surgical-related complications are commonly observed intraoperatively...
January 2017: Anesthesia, Essays and Researches
https://www.readbyqxmd.com/read/28295825/effectiveness-of-manual-therapy-versus-surgery-in-pain-processing-due-to-carpal-tunnel-syndrome-a-randomized-clinical-trial
#14
C Fernández-de-Las-Peñas, J Cleland, M Palacios-Ceña, S Fuensalida-Novo, C Alonso-Blanco, J A Pareja, F Alburquerque-Sendín
BACKGROUND: People with carpal tunnel syndrome (CTS) exhibit widespread pressure pain and thermal pain hypersensitivity as a manifestation of central sensitization. The aim of our study was to compare the effectiveness of manual therapy versus surgery for improving pain and nociceptive gain processing in people with CTS. METHODS: The trial was conducted at a local regional Hospital in Madrid, Spain from August 2014 to February 2015. In this randomized parallel-group, blinded, clinical trial, 100 women with CTS were randomly allocated to either manual therapy (n = 50), who received three sessions (once/week) of manual therapies including desensitization manoeuvres of the central nervous system, or surgical intervention (n = 50) group...
March 14, 2017: European Journal of Pain: EJP
https://www.readbyqxmd.com/read/28295390/mechanically-sensitive-a%C3%AE-nociceptors-that-innervate-bone-marrow-respond-to-changes-in-intra-osseous-pressure
#15
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/28294632/do-vulvodynia-tcm-patterns-differ-by-pain-types-beginning-evidence-supporting-the-concept
#16
Judith M Schlaeger, Hui Yan Cai, Xu Nenggui, Alana D Steffens, Wang Lin, Diana J Wilkie
INTRODUCTION: Vulvodynia affects a maximum of 14 million U.S. women; however, it has not been adequately characterized. Traditional Chinese Medicine (TCM) offers pattern diagnoses that may be considered vulvodynia phenotypes and may guide the development of more targeted treatments. OBJECTIVES: In women with vulvodynia, to explore relationships between the TCM patterns and pain. DESIGN/METHODS: In an exploratory study, 36 women diagnosed with vulvodynia had a TCM assessment and completed the Short Form McGill Pain Questionnaire (SF-MPQ)...
March 15, 2017: Journal of Alternative and Complementary Medicine: Research on Paradigm, Practice, and Policy
https://www.readbyqxmd.com/read/28292021/antinociceptive-pharmacological-profile-of-dysphania-graveolens-in-mouse
#17
Myrna Déciga-Campos, Rachel Mata, Isabel Rivero-Cruz
This work evaluates the potential antinociceptive activity of Dysphania graveolens, traditional medicinal plant used in Mexico to treat stomach pain. A CH2Cl2-MeOH extract, infusion and essential oil from aerial parts of Dysphania graveolens were evaluated in hot plate and writhing tests in mice. The metabolites pinostrobin, pinocembrin and chrysin were isolated from the Dysphania graveolens infusion; next, they were evaluated in both nociceptive tests. To confirm the antinociceptive activity and explore the possible participation of opioid, GABA and serotonin receptors in the pharmacological mechanism, a formalin test was used...
March 7, 2017: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
https://www.readbyqxmd.com/read/28291587/comparison-of-sedation-and-mechanical-antinociception-induced-by-intravenous-administration-of-acepromazine-and-four-dose-rates-of-dexmedetomidine-in-donkeys
#18
Ignacio Lizarraga, Fernanda Castillo-Alcala, Lauren S Robinson
OBJECTIVE: To assess and compare the sedative and antinociceptive effects of four dosages of dexmedetomidine in donkeys. STUDY DESIGN: Randomized, controlled, crossover, Latin-square, blinded study. ANIMALS: Six healthy, castrated, adult, standard donkeys. METHODS: Dexmedetomidine (2, 3, 4 and 5 μg kg(-1); D2, D3, D4 and D5), acepromazine (0.1 mg kg(-1)) and saline were administered intravenously to each donkey and a 1 week interval was allowed between successive trials on each animal...
January 11, 2017: Veterinary Anaesthesia and Analgesia
https://www.readbyqxmd.com/read/28288900/the-mechanism-of-back-pain-relief-by-spinal-manipulation-relies-on-decreased-temporal-summation-of-pain
#19
Christopher Randoll, Vincent Gagnon-Normandin, Jessica Tessier, Suzie Bois, Nabi Rustamov, Julie O'Shaughnessy, Martin Descarreaux, Mathieu Piché
The aim of the present study was to determine whether thoracic spinal manipulation (SM) decreases temporal summation of back pain. The study comprised 2 controlled experiments including 16 and 15 healthy participants, respectively. Each study included 6 sessions during which painful or non-painful electrical stimulations were delivered in three conditions: 1) control 2) light mechanical stimulus (MS) or 3) SM. Electrical stimulation was applied on the thoracic spine (T4), in the area where SM and MS were performed...
March 10, 2017: Neuroscience
https://www.readbyqxmd.com/read/28288793/a-novel-zebrafish-based-model-of-nociception
#20
J Christopher Taylor, L Savannah Dewberry, Stacie K Totsch, Lindsey R Yessick, Jennifer J DeBerry, Stephen A Watts, Robert E Sorge
Chronic pain affects the lives of millions yearly, but few new treatments are available. Due to decreasing budgets and increasing costs of preclinical research, alternatives are sought with high translatability and low cost. Here we demonstrate the utility of a zebrafish-based model of nociception to serve as a novel screening tool for analgesic drugs. Zebrafish swimming behavior was measured following administration of various algogens including histamine, cinnamaldehyde, mustard oil, acetic acid and complete Freund's adjuvant...
March 10, 2017: Physiology & Behavior
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