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https://www.readbyqxmd.com/read/28632393/the-antinociceptive-agent-sbfi-26-binds-to-anandamide-transporters-fabp5-and-fabp7-at-two-different-sites
#1
Hao-Chi Hsu, Simon Tong, Yuchen Zhou, Matthew W Elmes, Su Yan, Martin Kaczocha, Dale G Deutsch, Robert C Rizzo, Iwao Ojima, Huilin Li
Human FABP5 and FABP7 are intracellular endocannabinoid transporters. SBFI-26 is an -truxillic acid 1-naphthyl monoester that competitively inhibits the activities of FABP5 and FABP7 and produces antinociceptive and anti-inflammatory effects in mice. The synthesis of SBFI-26 yields several stereoisomers, and it is not known how the inhibitor binds the transporters. Here we report co-crystal structures of SBFI-26 in complex with human FABP5 and FABP7 at a resolution of 2.2 Å and 1.9 Å, respectively. We found that only (S)-SBFI-26 was present in the crystal structures...
June 20, 2017: Biochemistry
https://www.readbyqxmd.com/read/28631050/analgesia-nociception-index-ani-monitoring-in-patients-with-thoracic-paravertebral-block-a-randomized-controlled-study
#2
Nurseda Dundar, Alparslan Kus, Yavuz Gurkan, Kamil Toker, Mine Solak
The goal of the study was to evaluate the effectiveness of analgesia nociception index (ANI) monitoring during intraoperative period for patients with thoracic paravertebral block (TPVB) undergoing breast surgery under general anesthesia. This prospective randomized trial was performed after receiving ethics committee approval in 44 patients who were scheduled to undergo breast surgery under general anesthesia. TPVB was performed in the preoperative period using 20 mL of bupivacaine 0.25% at T4 level. Anesthesia maintenance was provided with sevoflurane in O2: air mixture and remifentanil infusion...
June 19, 2017: Journal of Clinical Monitoring and Computing
https://www.readbyqxmd.com/read/28629817/the-antinociceptive-effects-of-a-standardized-ethanol-extract-of-the-bidens-odorata-cav-asteraceae-leaves-are-mediated-by-atp-sensitive-k-channels
#3
Juan Ramón Zapata-Morales, Angel Josabad Alonso-Castro, Fabiola Domínguez, Candy Carranza-Álvarez, Mario Isiordia-Espinoza, Alejandro Hernández-Morales, Cesar Solorio-Alvarado
ETHNOPHARMACOLOGICAL RELEVANCE: Bidens odorata Cav (Asteraceae)is used for the empirical treatment of inflammation and pain. AIM OF THE STUDY: This work evaluatedthein vitro and in vivo toxicity, antioxidant activity, as well as the anti-inflammatory and antinociceptive effects of an ethanol extract from Bidens odorata leaves (BOE). MATERIALS AND METHODS: The in vitro toxicity of BOE (10-1000µg/ml) was evaluated with the comet assay in PBMC...
June 16, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28629730/synergistic-antinociceptive-effect-of-a-calcium-channel-blocker-and-a-trpv1-blocker-in-an-acute-pain-model-in-mice
#4
Manuella R Palhares, Juliana F Silva, Marcio Junior S Rezende, Duana C Santos, Cláudio A Silva-Junior, Márcia H Borges, Juliano Ferreira, Marcus V Gomez, Célio J Castro Junior
AIMS: Extensive evidence supports a role for voltage-gated calcium channels (VGCC) and TRPV1 receptors in pain transmission and modulation. We investigated the profile of analgesic interaction between Phα1β toxin (a VGCC blocker) and SB366791 (selective TRPV1 antagonist) in a model of acute pain induced by capsaicin. Changes in body temperature induced by combination regimens were also evaluated. MAIN METHODS: Isobolographic approach with a fixed dose-ratio of combined drugs was used to determine whether antinociceptive interaction of Phα1β and SB366791 are subadditive, additive or synergic...
June 16, 2017: Life Sciences
https://www.readbyqxmd.com/read/28628851/spinal-5-ht4-and-5-ht6-receptors-contribute-to-the-maintenance-of-neuropathic-pain-in-rats
#5
Jorge Baruch Pineda-Farias, Paulino Barragán-Iglesias, Alann Valdivieso-Sánchez, Juan Rodríguez-Silverio, Francisco Javier Flores-Murrieta, Vinicio Granados-Soto, Héctor Isaac Rocha-González
BACKGROUND: Nerve injury promotes release of 5-HT at the spinal cord. Once released, 5-HT may produce antinociceptive or pronociceptive effects depending of the nature of 5-HT receptors. The purpose of this study was to investigate the participation of spinal 5-HT4 and 5-HT6 receptors in the maintenance of neuropathic pain in rats. METHODS: Tactile allodynia was measured using von Frey hairs in male Wistar rats subjected to L5-L6 spinal nerve injury. Selective 5-HT4 (GR-113808, 0...
April 4, 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/28628078/nociceptor-interleukin-10-receptor-1-is-critical-for-muscle-analgesia-induced-by-repeated-bouts-of-eccentric-exercise-in-the-rat
#6
Pedro Alvarez, Oliver Bogen, Paul G Green, Jon D Levine
Delayed-onset muscle soreness is typically observed after strenuous or unaccustomed eccentric exercise. Soon after recovery, blunted muscle soreness is observed on repeated eccentric exercise, a phenomenon known as repeated bout effect (RBE). Although regular physical activity decreases muscle hyperalgesia, likely because of increased production of the anti-inflammatory cytokine interleukin-10 (IL-10) in the skeletal muscle, whether IL-10 also contributes to the antinociceptive effect of RBE is unknown. Furthermore, whether IL-10 attenuates muscle hyperalgesia by acting on muscle nociceptors remains to be established...
April 26, 2017: Pain
https://www.readbyqxmd.com/read/28627589/effect-of-the-spinal-apelin%C3%A2-apj-system-on-the-pathogenesis-of-chronic-constriction-injury%C3%A2-induced-neuropathic-pain-in-rats
#7
Qingming Xiong, Wanyou He, Hanbing Wang, Jun Zhou, Yajun Zhang, Jian He, Chengxiang Yang, Bin Zhang
Apelin is hypothesized to serve a dual function in pain processing. Spinal administration of apelin induces hyperalgesia, while opioid receptors are implicated in the antinociceptive effects of apelin in acute nociceptive models. However, whether the apelin‑apelin receptor (APJ) system is involved in neuropathic pain remains to be elucidated. The present study aimed to evaluate the impact and mechanism of the spinal apelin‑APJ system in neuropathic pain. Chronic constriction injury (CCI) of the sciatic nerve produced sustained spinal apelin and APJ upregulation, which was associated with mechanical allodynia and heat hyperalgesia development in the hind‑paw plantar surface...
June 9, 2017: Molecular Medicine Reports
https://www.readbyqxmd.com/read/28626482/the-possible-mechanisms-of-analgesia-produced-by-microinjection-of-morphine-into-the-lateral-habenula-in-the-acute-model-of-trigeminal-pain-in-rats
#8
Emad Khalilzadeh, Gholamreza Vafaei Saiah
This study aimed to assess the effect of intra-habenular injection of morphine on acute trigeminal pain in rats. Also here, we examined the involvement of raphe nucleus opioid and 5HT3 receptors on the antinociceptive activity of intra habenular morphine to explore the possibility of existence of descending antinociceptive relay between the habenula and raphe nucleus. The numbers of eye wiping response elicited by applying a drop (40 μL) of NaCl (5 M) solution on the corneal surface were taken as an index of acute trigeminal nociception...
June 2017: Research in Pharmaceutical Sciences
https://www.readbyqxmd.com/read/28625735/analgesic-and-physiological-effect-of-electroacupuncture-combined-with-epidural-lidocaine-in-goats
#9
Lu-Ying Cui, Ni-Ni Guo, Yu-Lin Li, Meng Li, Ming-Xing Ding
OBJECTIVE: To investigate physiological and antinociceptive effects of electroacupuncture (EA) with lidocaine epidural nerve block in goats. STUDY DESIGN: Prospective experimental trial. ANIMALS: Forty-eight hybrid male goats weighing 27 ± 2 kg. METHODS: The goats were randomly assigned to six groups: L2.2, epidural lidocaine (2.2 mg kg(-1)); L4.4, epidural lidocaine (4.4 mg kg(-1)); EA; EA-L1.1, EA with epidural lidocaine (1...
January 12, 2017: Veterinary Anaesthesia and Analgesia
https://www.readbyqxmd.com/read/28625489/diosmin-reduces-chronic-constriction-injury-induced-neuropathic-pain-in-mice
#10
Mariana M Bertozzi, Ana C Rossaneis, Victor Fattori, Daniela T Longhi-Balbinot, Andressa Freitas, Fernando Q Cunha, José C Alves-Filho, Thiago M Cunha, Rubia Casagrande, Waldiceu A Verri
Injury or dysfunction of somatosensory system induces a complex syndrome called neuropathic pain, which still needs adequate pharmacological control. The current pharmacological treatments were in part developed from natural compounds. Flavonoids are natural polyphenolic molecules presenting varied biological activities and low toxicity. The flavonoid diosmin is a safe compound with good tolerability and low toxicity. This study evaluated the antinociceptive effect of diosmin in the sciatic nerve chronic constriction injury (CCI)-induced neuropathic pain model...
June 15, 2017: Chemico-biological Interactions
https://www.readbyqxmd.com/read/28623711/contribution-of-dopaminergic-and-noradrenergic-systems-in-the-antinociceptive-effect-of-%C3%AE-phenylalanyl-acetophenone
#11
Fernanda S S Sousa, Roberta G Anversa, Paloma T Birmann, Maurice N de Souza, Renata Balaguez, Diego Alves, Cristiane Luchese, Ethel A Wilhelm, Lucielli Savegnago
BACKGROUND: This study evaluated the antinociceptive action of α-(phenylalanyl) acetophenone (PSAP) in mice. METHODS: Evaluated whether the serotonergic, adrenergic and dopaminergic systems are involved in PSAP antinociceptive activity. PSAP was administered intragastrically (ig) 30min prior to formalin or glutamate test and compared with a standard drug, meloxicam (10mg/kg, ig). RESULTS: The treatment with PSAP (10-50mg/kg) caused inhibition in the neurogenic phase and reduced the paw oedema caused by intraplantar (ipl) injection of formalin...
March 27, 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/28623708/isobolographic-analysis-of-the-cutaneous-antinociceptive-interaction-between-bupivacaine-co-injected-with-serotonin-in-rats
#12
Jann-Inn Tzeng, Chong-Chi Chiu, Jhi-Joung Wang, Yu-Wen Chen, Ching-Hsia Hung
BACKGROUND: The aim of this experiment was to investigate a long-lasting local anesthetic bupivacaine combined with serotonin at inducing cutaneous antinociception. METHODS: The skin antinociception, characterized by an inhibition of the cutaneous trunci muscle reflex (CTMR) following the pinprick on the dorsal skin of rats, was evaluated. The cutaneous antinociceptive effects of bupivacaine alone, serotonin alone, or bupivacaine co-injected with serotonin in a dose-dependent fashion were constructed, while the drug-drug interactions were evaluated by isobologram...
March 29, 2017: Pharmacological Reports: PR
https://www.readbyqxmd.com/read/28618070/morin-suppresses-astrocyte-activation-and-regulates-cytokine-release-in-bone-cancer-pain-rat-models
#13
Wei Jiang, Ying Wang, Wei Sun, Mengyuan Zhang
As inflammatory and immune responses are involved in pathophysiology of debilitating neuropathic pain, reagents that can modulate these two responses may have therapeutic potential. Morin, derived from the moraceae family of plants, benefits inflammation-related diseases, but its antinociceptive effects on cancer pain remain elusive. In the present study, we investigated antinociceptive effects of morin on bone cancer pain using a rat model, where rats were subject to implantation of Walker 256 mammary gland carcinoma cells into the tibia...
June 15, 2017: Phytotherapy Research: PTR
https://www.readbyqxmd.com/read/28614186/mir-34c-5p-functions-as-pronociceptive-microrna-in-cancer-pain-by-targeting-cav2-3-containing-calcium-channels
#14
Jagadeesh Gandla, Santosh Kumar Lomada, Jianning Lu, Rohini Kuner, Kiran Kumar Bali
Pathophysiological mechanisms underlying pain associated with cancer are poorly understood. microRNAs are a class of non-coding RNAs with emerging functional importance in chronic pain. In a genome-wide screen for microRNAs regulated in dorsal root ganglia (DRG) neurons in a mouse model of bone metastatic pain, we identified miR-34c-5p as a functionally important pronociceptive microRNA. Despite these functional insights and therapeutic potential for miR-34c-5p, its molecular mechanism of action in peripheral sensory neurons remains unknown...
June 9, 2017: Pain
https://www.readbyqxmd.com/read/28608248/the-analgesic-effect-of-trans-resveratrol-is-regulated-by-calcium-channels-in-the-hippocampus-of-mice
#15
Weijie Wang, Yingcong Yu, Jing Li, Lin Wang, Zhi Li, Chong Zhang, Linlin Zhen, Lianshu Ding, Gang Wang, Xiaoyang Sun, Ying Xu
Resveratrol has been widely studied in terms of it's potential to slow the progression of many diseases. But little is known about the mechanism of action in neuropathic pain. Neuropathic pain is the main type of chronic pain associated with tissue injury. Calcium channels and calcium/caffeine-sensitive pools are associated with analgesic pathway involving neuropathic pain. Our previous study suggested that the antinociceptive effect of resveratrol was involved in Ca(2+)/calmodulin-dependent signaling in the spinal cord of mice...
June 12, 2017: Metabolic Brain Disease
https://www.readbyqxmd.com/read/28608142/erratum-to-antinociceptive-interaction-of-gabapentin-with-minocycline-in-murine-diabetic-neuropathy
#16
H F Miranda, F Sierralta, V Jorquera, P Poblete, J C Prieto, V Noriega
No abstract text is available yet for this article.
June 12, 2017: Inflammopharmacology
https://www.readbyqxmd.com/read/28606856/antinociceptive-effect-of-botulinum-toxin-a-involves-alterations-in-ampa-receptor-expression-and-glutamate-release-in-spinal-dorsal-horn-neurons
#17
Bin Hong, LingLing Yao, Linhui Ni, Li Wang, XingYue Hu
The use of botulinum toxin A (BTX-A) for various clinical therapeutic applications is increasing. It is widely believed that peripheral therapeutic or toxic effects of BTX-A are exclusively mediated by SNAP-25 cleavage. There is growing evidence of long-distance retrograde axonal transport of BTX-A on entering the central nervous system, subsequent to a local injection of the toxin. However, the prevalence of central antinociceptive effects after BTX-A peripheral application and its underlying mechanisms are unclear...
June 10, 2017: Neuroscience
https://www.readbyqxmd.com/read/28606623/the-interaction-between-alpha-7-nicotinic-acetylcholine-receptor-and-nuclear-peroxisome-proliferator-activated-receptor-%C3%AE-represents-a-new-antinociceptive-signaling-pathway-in-mice
#18
Giulia Donvito, Deniz Bagdas, Wisam Toma, Elnaz Rahimpour, Asti Jackson, Julie A Meade, Shakir AlSharari, Abhijit R Kulkarni, F Ivy Carroll, Aron H Lichtman, Roger L Papke, Ganesh A Thakur, M Imad Damaj
Recently, α7 nicotinic acetylcholine receptors (nAChRs), primarily activated by binding of orthosteric agonists, represent a target for anti-inflammatory and analgesic drug development. These receptors may also be modulated by positive allosteric modulators (PAMs), ago-allosteric ligands (ago-PAMs), and α7-silent agonists. Activation of α7 nAChRs has been reported to increase the brain levels of endogenous ligands for nuclear peroxisome proliferator-activated receptors type-α (PPAR-α), palmitoylethanolamide (PEA) and oleoylethanolamide (OEA), in a Ca(2+)-dependent manner...
June 9, 2017: Experimental Neurology
https://www.readbyqxmd.com/read/28603600/synthesis-and-pharmacological-evaluation-of-novel-selective-mor-agonist-6%C3%AE-pyridinyl-amidomorphines-exhibiting-long-lasting-antinociception
#19
Ákos Urai, András Váradi, Levente Szőcs, Balázs Komjáti, Valerie Le Rouzic, Amanda Hunkele, Gavril W Pasternak, Susruta Majumdar, Sándor Hosztafi
It was previously reported that 6β-aminomorphinan derivatives show high affinity for opiate receptors. Novel 6β-heteroarylamidomorphinanes were designed based on the MOR selective antagonist NAP. The 6β-aminomorphinanes were prepared with stereoselective Mitsunobu reaction and subsequently acylated with nicotinic acid and isonicotinic acid chloride hydrochlorides. The receptor binding and efficacy were determined in vitro and the analgesic activity was studied in vivo. The in vitro studies revealed moderate selectivity for MOR...
January 1, 2017: MedChemComm
https://www.readbyqxmd.com/read/28602640/design-and-synthesis-of-novel-%C3%AE-opioid-receptor-agonists-with-an-azatricyclodecane-skeleton-for-improving-blood-brain-barrier-penetration
#20
Yoshikazu Watanabe, Kohei Hayashida, Daisuke Saito, Toshihiro Takahashi, Junichi Sakai, Eriko Nakata, Takashi Kanda, Takashi Iwai, Shigeto Hirayama, Hideaki Fujii, Tomio Yamakawa, Hiroshi Nagase
We designed and synthesized novel δ opioid receptor (DOR) agonists 3a-i with an azatricyclodecane skeleton, which was a novel structural class of DOR agonists. Among them, 3b exhibited high values of binding affinity and potent agonistic activity for the DOR that were approximately equivalent to those of 2 which bore an oxazatricyclodecane skeleton. In vitro assays using the blood-brain barrier (BBB) permeability test kit supported the idea that 3b achieved an excellent BBB permeability by converting an oxygen atom of 2 to a carbon atom (methylene group) in the core skeleton...
May 26, 2017: Bioorganic & Medicinal Chemistry Letters
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