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Serotonergic receptors AND pain

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https://www.readbyqxmd.com/read/29729247/ionic-plasticity-and-pain-the-loss-of-descending-serotonergic-fibers-after-spinal-cord-injury-transforms-how-gaba-affects-pain
#1
Yung-Jen Huang, James W Grau
Activation of pain (nociceptive) fibers can sensitize neural circuits within the spinal cord, inducing an increase in excitability (central sensitization) that can foster chronic pain. The development of spinally-mediated central sensitization is regulated by descending fibers and GABAergic interneurons. In adult animals, the co-transporter KCC2 maintains a low intracellular concentration of the anion Cl- . As a result, when the GABA-A receptor is engaged, Cl- flows in the neuron which has a hyperpolarizing (inhibitory) effect...
May 2, 2018: Experimental Neurology
https://www.readbyqxmd.com/read/29719465/antinociceptive-and-anti-inflammatory-effects-of-ginsenoside-rf-in-a-rat-model-of-incisional-pain
#2
Min Kyoung Kim, Hyun Kang, Chong Wha Baek, Yong Hun Jung, Young Cheol Woo, Geun Joo Choi, Hwa Yong Shin, Kyung Soo Kim
Background: Ginseng saponin has long been used as a traditional Asian medicine and is known to be effective in treating various kinds of pain. Ginsenoside Rf is one of the biologically active saponins found in ginseng. We evaluated ginsenoside Rf's antinociceptive and anti-inflammatory effects, and its mechanism of action on adrenergic and serotonergic receptors, in an incisional pain model. Methods: Mechanical hyperalgesia was induced via plantar incision in rats followed by intraperitoneal administration of increasing doses of ginsenoside Rf (vehicle, 0...
April 2018: Journal of Ginseng Research
https://www.readbyqxmd.com/read/29582424/antinociceptive-and-anti-inflammatory-effects-of-1-2-bis-4-methoxyphenylselanyl-styrene-in-mice-involvement-of-the-serotonergic-system
#3
Roberta Gonçalves Anversa, Fernanda Severo Sabedra Sousa, Paloma Taborda Birmann, David Borba Lima, Eder João Lenardão, César Augusto Bruning, Lucielli Savegnago
BACKGROUND: Pain is one of the most prevalent, costly and disabling conditions that reduces quality of life. Although there are many analgesics available, there is some concern regarding their efficacy, safety and side effects. Organic selenium compounds are attractive targets of various research groups due to their pharmacological properties. OBJECTIVES: The aim of this study was to evaluate the antinociceptive and anti-inflammatory activity of 1,2-bis-(4-methoxyphenylselanyl) styrene (BMOSE) in mice, as well as to investigate the mechanism involved in the antinociceptive effect...
March 27, 2018: Journal of Pharmacy and Pharmacology
https://www.readbyqxmd.com/read/29451703/mechanisms-of-imidazoline-i-2-receptor-agonist-induced-antinociception-in-rats-involvement-of-monoaminergic-neurotransmission
#4
Justin N Siemian, Kaixuan Wang, Yanan Zhang, Jun-Xu Li
BACKGROUND AND PURPOSE: Although the antinociceptive efficacies of imidazoline I2 receptor agonists have been established, the exact post-receptor mechanisms remain unknown. This study tested the hypothesis that monoaminergic transmission is critical for I2 receptor agonist-induced antinociception. EXPERIMENTAL APPROACH: von Frey filaments were used to assess antinociceptive effects of two I2 receptor agonists, 2-BFI and CR4056 on chronic constriction injury (CCI)-induced neuropathic pain or complete Freund's adjuvant (CFA)-induced inflammatory pain in rats...
May 2018: British Journal of Pharmacology
https://www.readbyqxmd.com/read/29392233/regular-physical-activity-prevents-development-of-chronic-muscle-pain-through-modulation-of-supraspinal-opioid-and-serotonergic-mechanisms
#5
Renan G Brito, Lynn A Rasmussen, Kathleen A Sluka
Introduction: It is generally believed that exercise produces its effects by activating central opioid receptors; there are little data that support this claim. The periaqueductal gray (PAG) and rostral ventromedial medulla (RVM) are key nuclei in opioid-induced analgesia, and opioids interact with serotonin to produce analgesia. Objectives: The purpose was to examine central inhibitory mechanisms involved in analgesia produced by wheel running. Methods: C57/Black6 mice were given access to running wheels in their home cages before induction of chronic muscle hyperalgesia and compared with those without running wheels...
September 2017: Pain Reports (Baltimore, Md.)
https://www.readbyqxmd.com/read/29366515/antinociceptive-profiles-and-mechanisms-of-centrally-administered-oxyntomodulin-in-various-mouse-pain-models
#6
Soo-Hyun Park, Jae-Ryeong Lee, Sang-Pil Jang, Seyung-Hwan Park, Hee-Jung Lee, Jung-Woo Hong, Hong-Won Suh
In the present study, the antinociceptive profiles of oxyntomodulin were examined in ICR mice. Oxyntomodulin administered intrathecally (i.t.) and intracerebroventricularly (i.c.v.) (from 1 to 5μg/5μl) showed an antinociceptive effect in a dose-dependent manner as measured in the acetic acid-induced writhing test. Moreover, cumulative response time of nociceptive behaviors induced by intraplantar formalin injection was reduced by i.t. or i.c.v. treatment with oxyntomodulin during the second, but not the first phase...
April 2018: Neuropeptides
https://www.readbyqxmd.com/read/29274353/oxidative-stress-in-the-amygdala-contributes-to-neuropathic-pain
#7
B Sagalajev, H Wei, Z Chen, I Albayrak, A Koivisto, A Pertovaara
Earlier studies indicate that the central nucleus of the amygdala (CeA) contributes to neuropathic pain. Here we studied whether amygdaloid administration of antioxidants or antagonists of TRPA1 that is among ion channels activated by oxidative stress attenuates nociceptive or affective pain in experimental neuropathy, and whether this effect involves amygdaloid astrocytes or descending serotonergic pathways acting on the spinal 5-HT1A receptor. The experiments were performed in rats with spared nerve injury (SNI)...
December 20, 2017: Neuroscience
https://www.readbyqxmd.com/read/29169951/regulation-of-noradrenergic-and-serotonergic-systems-by-cannabinoids-relevance-to-cannabinoid-induced-effects
#8
REVIEW
Aitziber Mendiguren, Erik Aostri, Joseba Pineda
The cannabinoid system is composed of Gi/o protein-coupled cannabinoid type 1 receptor (CB1 ) and cannabinoid type 2 (CB2 ) receptor and endogenous compounds. The CB1 receptor is widely distributed in the central nervous system (CNS) and it is involved in the regulation of common physiological functions. At the neuronal level, the CB1 receptor is mainly placed at GABAergic and glutamatergic axon terminals, where it modulates excitatory and inhibitory synapses. To date, the involvement of CB2 receptor in the regulation of neurotransmission in the CNS has not been clearly shown...
January 1, 2018: Life Sciences
https://www.readbyqxmd.com/read/29126856/nlx-112-a-highly-selective-5-ht-1a-receptor-agonist-effects-on-body-temperature-and-plasma-corticosterone-levels-in-rats
#9
A Newman-Tancredi, R Depoortère, E Carilla-Durand, J P Tarayre, M Kleven, W Koek, L Bardin, M A Varney
NLX-112 (a.k.a. F13640 or befiradol), exhibits nanomolar affinity, exceptional selectivity and high agonist efficacy at 5-hydroxytryptamine 5-HT1A receptors. It possesses marked activity in a variety of animal models of depression, pain and L-DOPA-induced dyskinesia. However, its influence on translational biomarkers of central 5-HT1A receptor activation has not been previously described. Here, we report on the activity, in rats, of NLX-112 to increase plasma corticosterone levels and produce hypothermia, two responses which are also elicited by 5-HT1A receptor agonists in humans...
February 2018: Pharmacology, Biochemistry, and Behavior
https://www.readbyqxmd.com/read/29054049/individual-variability-in-clinical-effect-and-tolerability-of-opioid-analgesics-importance-of-drug-interactions-and-pharmacogenetics
#10
REVIEW
Vigdis Solhaug, Espen Molden
BACKGROUND: As pain is often a comorbid condition, many patients use opioid analgesics in combination with several other drugs. This implies a generally increased risk of drug interactions, which along with inherent pharmacogenetic variability and other factors may cause differences in therapeutic response of opioids. AIM: To provide an overview of interactions and pharmacogenetic variability of relevance for individual differences in effect and tolerability of opioid analgesics, which physicians and other healthcare professionals should be aware of in clinical practice...
October 17, 2017: Scandinavian Journal of Pain
https://www.readbyqxmd.com/read/28993250/monoaminergic-descending-pathways-contribute-to-modulation-of-neuropathic-pain-by-increasing-intensity-treadmill-exercise-after-peripheral-nerve-injury
#11
Victor M Lopez-Alvarez, Maria Puigdomenech, Xavier Navarro, Stefano Cobianchi
This study characterizes the impact of increasing-intensity treadmill exercise (iTR) on noradrenergic (NE) and serotonergic (5HT) modulation of neuropathic pain. Following sciatic nerve transection and repair (SNTR) rats developed significant mechanical and thermal hyperalgesia that was partially prevented by iTR performed during the first 2weeks after injury. Marked decrease in the expression of 5HT2A and α1A and β-, but not α2A adrenergic receptors in the spinal cord dorsal horn was associated to SNTR and recovered by iTR, particularly in lamina II...
January 2018: Experimental Neurology
https://www.readbyqxmd.com/read/28874746/rgma-inhibition-with-human-monoclonal-antibodies-promotes-regeneration-plasticity-and-repair-and-attenuates-neuropathic-pain-after-spinal-cord-injury
#12
Andrea J Mothe, Nardos G Tassew, Alirezha P Shabanzadeh, Romeo Penheiro, Robin J Vigouroux, Lili Huang, Christine Grinnell, Yi-Fang Cui, Emma Fung, Philippe P Monnier, Bernhard K Mueller, Charles H Tator
Traumatic spinal cord injury (SCI) causes a cascade of degenerative events including cell death, axonal damage, and the upregulation of inhibitory molecules which prevent regeneration and limit recovery. Repulsive guidance molecule A (RGMa) is a potent neurite growth inhibitor in the central nervous system, exerting its repulsive activity by binding the Neogenin receptor. Here, we show for the first time that inhibitory RGMa is markedly upregulated in multiple cell types after clinically relevant impact-compression SCI in rats, and importantly, also in the injured human spinal cord...
September 5, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28856708/degeneration-of-serotonin-neurons-triggers-spasticity-in-amyotrophic-lateral-sclerosis
#13
Hajer El Oussini, Jelena Scekic-Zahirovic, Pauline Vercruysse, Christine Marques, Sylvie Dirrig-Grosch, Stéphane Dieterlé, Gina Picchiarelli, Jérôme Sinniger, Caroline Rouaux, Luc Dupuis
OBJECTIVE: Spasticity occurs in a wide range of neurological diseases, including neurodegenerative diseases, after trauma, and after stroke, and is characterized by increased reflexes leading to muscle hypertonia. Spasticity is a painful symptom and can severely restrict everyday life, but might also participate in maintaining a low level of motor function in severely impaired patients. Constitutive activity of the serotonin receptors 5-HT2B/C is required for the development of spasticity after spinal cord injury and during amyotrophic lateral sclerosis (ALS)...
September 2017: Annals of Neurology
https://www.readbyqxmd.com/read/28763302/intramuscularly-injected-neurotropin-reduced-muscular-mechanical-hyperalgesia-induced-by-repeated-cold-stress-in-rats
#14
Teruaki Nasu, Shiori Murase, Yoshiko Takeda-Uchimura, Kazue Mizumura
An extract of rabbit skin inflamed by inoculation with the vaccinia virus, neurotropin [by intravenous, oral, and intramuscular (i.m.) administration], has been used in China and Japan for the treatment of chronic pain. In this study, we investigated the analgesic mechanism of i.m. neurotropin. Rats were exposed to repeated cold stress, and muscular mechanical hyperalgesia was evaluated by measuring the withdrawal threshold of the gastrocnemius muscle using Randall-Selitto apparatus. I.m. but not subcutaneous, neurotropin dose dependently reduced the repeated cold stress-induced muscular mechanical hyperalgesia for 3 h, but it had no effect in normal rats...
April 2018: Behavioural Pharmacology
https://www.readbyqxmd.com/read/28736332/5-hydroxytryptamine-2a-receptors-of-the-dorsal-raphe-nucleus-mediate-panic-like-behaviours-and-fear-induced-antinociception-elicited-by-neuronal-activation-in-the-central-nucleus-of-the-inferior-colliculus
#15
Raimundo da Silva Soares, Luiz Luciano Falconi-Sobrinho, Tayllon Dos Anjos-Garcia, Norberto Cysne Coimbra
It has been established that chemical stimulation of the inferior colliculus (IC) of laboratory animals evokes fear-related defensive responses, which are considered panic attack-like behaviours. In addition, there is evidence that defensive reactions provoked by chemical stimulation of midbrain tectum neurons may induce an antinociceptive response. Morphologically, the IC receives projections from other mesencephalic structures, such as the dorsal raphe nucleus (DRN), a region rich in serotonergic neurons that play a critical role in the control of defensive behaviours...
July 20, 2017: Behavioural Brain Research
https://www.readbyqxmd.com/read/28730896/cannabinoid-hyperemesis-syndrome-potential-mechanisms-for-the-benefit-of-capsaicin-and-hot-water-hydrotherapy-in-treatment
#16
John R Richards, Jeff M Lapoint, Guillermo Burillo-Putze
INTRODUCTION: Cannabinoid hyperemesis syndrome is a clinical disorder that has become more prevalent with increasing use of cannabis and synthetic cannabinoids, and which is difficult to treat. Standard antiemetics commonly fail to alleviate the severe nausea and vomiting characteristic of the syndrome. Curiously, cannabinoid hyperemesis syndrome patients often report dramatic relief of symptoms with hot showers and baths, and topical capsaicin. OBJECTIVES: In this review, we detail the pharmacokinetics and pharmacodynamics of capsaicin and explore possible mechanisms for its beneficial effect, including activation of transient receptor potential vanilloid 1 and neurohumoral regulation...
January 2018: Clinical Toxicology
https://www.readbyqxmd.com/read/28730894/low-5-ht1b-receptor-binding-in-the-migraine-brain-a-pet-study
#17
Marie Deen, Hanne D Hansen, Anders Hougaard, Sofi da Cunha-Bang, Martin Nørgaard, Claus Svarer, Sune H Keller, Carsten Thomsen, Messoud Ashina, Gitte M Knudsen
Background The pathophysiology of migraine may involve dysfunction of serotonergic signaling. In particular, the 5-HT1B receptor is considered a key player due to the efficacy of 5-HT1B receptor agonists for treatment of migraine attacks. Aim To examine the cerebral 5-HT1B receptor binding in interictal migraine patients without aura compared to controls. Methods Eighteen migraine patients, who had been migraine free for >48 hours, and 16 controls were scanned after injection of the 5-HT1B receptor specific radioligand [(11)C]AZ10419369 for quantification of cerebral 5-HT1B receptor binding...
January 1, 2017: Cephalalgia: An International Journal of Headache
https://www.readbyqxmd.com/read/28671718/antinociceptive-effects-of-low-level-laser-therapy-at-3-and-8%C3%A2-j-cm-2-in-a-rat-model-of-postoperative-pain-possible-role-of-endogenous-opioids
#18
Fabio C Pereira, Julia R Parisi, Caio B Maglioni, Gabriel B Machado, Paulino Barragán-Iglesias, Josie R T Silva, Marcelo L Silva
Low-level laser therapy (LLLT) is the direct application of light to stimulate cell responses (photobiomodulation) to promote tissue healing, reduce inflammation, and induce analgesia; the molecular basis for these effects of LLLT remains unclear. The objective of this study was to evaluate the analgesic effect of LLLT in the rat plantar incision model of postoperative pain as well as to investigate some of the possible mechanisms involved in this effect. Wistar rats were submitted to plantar incision and treated with LLLT (830 nm, continuous-mode, 30 mW/cm(2) , 1-12 J/cm(2) )...
July 3, 2017: Lasers in Surgery and Medicine
https://www.readbyqxmd.com/read/28655928/brain-activity-changes-in-a-macaque-model-of-oxaliplatin-induced-neuropathic-cold-hypersensitivity
#19
Kazuaki Nagasaka, Kazunori Yamanaka, Shinya Ogawa, Hiroyuki Takamatsu, Noriyuki Higo
The antineoplastic agent oxaliplatin induces a painful peripheral neuropathy characterized by an acute cold hypersensitivity. There is a lack of effective treatments to manage oxaliplatin-induced cold hypersensitivity which is due, in part, to a lack of understanding of the pathophysiology of oxaliplatin-induced cold hypersensitivity. Thus, brain activity in oxaliplatin-treated macaques was examined using functional magnetic resonance imaging (fMRI). Oxaliplatin treatment reduced tail withdrawal latency to a cold (10 °C) stimulus, indicating cold hypersensitivity and increased activation in the secondary somatosensory cortex (SII) and the anterior insular cortex (Ins) was observed...
June 27, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28606116/characterization-of-serotonin-induced-inhibition-of-excitatory-synaptic-transmission-in-the-anterior-cingulate-cortex
#20
Zhen Tian, Manabu Yamanaka, Matteo Bernabucci, Ming-Gao Zhao, Min Zhuo
Excitatory synaptic transmission in central synapses is modulated by serotonin (5-HT). The anterior cingulate cortex (ACC) is an important cortical region for pain perception and emotion. ACC neurons receive innervation of projecting serotonergic nerve terminals from raphe nuclei, but the possible effect of 5-HT on excitatory transmission in the ACC has not been investigated. In the present study, we investigated the role of 5-HT on glutamate neurotransmission in the ACC slices of adult mice. Bath application of 5-HT produced dose-dependent inhibition of evoked excitatory postsynaptic currents (eEPSCs)...
June 12, 2017: Molecular Brain
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