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https://www.readbyqxmd.com/read/29017758/in-vitro-and-in-vivo-pharmacological-characterization-of-asp8477-a-novel-highly-selective-fatty-acid-amide-hydrolase-inhibitor
#1
Tomonari Watabiki, Noriko Tsuji, Tetsuo Kiso, Tohru Ozawa, Fumie Narazaki, Shuichiro Kakimoto
Although exogenous agonists for cannabinoid (CB) receptors are clinically effective for treating chronic pain, global activation of brain CB receptors causes frequent central nervous system (CNS) side-effects. Fatty acid amide hydrolase (FAAH) is a primary catabolic enzyme for anandamide (AEA), an endogenous CB. Recently, we discovered a novel FAAH inhibitor, 3-pyridyl 4-(phenylcarbamoyl)piperidine-1-carboxylate (ASP8477). In vitro studies demonstrated that ASP8477 inhibited human FAAH-1, FAAH-1 (P129T) and FAAH-2 activity with IC50 values of 3...
October 7, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28980210/photobiomodulation-therapy-improves-acute-inflammatory-response-in-mice-the-role-of-cannabinoid-receptors-atp-sensitive-k-channel-p38-mapk-signalling-pathway
#2
Laís M S Neves, Elaine C D Gonçalves, Juliana Cavalli, Graziela Vieira, Larissa R Laurindo, Róli R Simões, Igor S Coelho, Adair R S Santos, Alexandre M Marcolino, Maíra Cola, Rafael C Dutra
Although photobiomodulation therapy (PBM) has been applied clinically for the treatment of pain and inflammation, wound healing, sports and soft tissue injuries, as well as to repair injured spinal cords and peripheral nerves, it remains unclear which molecular substrates (receptor) are implicated in the cellular mechanisms of PBM. Here, we reported that PBM (660 nm, 30 mW, 0.06 cm(2), 50 J/cm(2), plantar irradiation) significantly inhibited carrageenan-induced paw oedema, but not noxious thermal response, through positive modulation to both CB1 and CB2 cannabinoid receptors...
October 4, 2017: Molecular Neurobiology
https://www.readbyqxmd.com/read/28975684/salvinorin-a-reduces-neuropathic-nociception-in-the-insular-cortex-of-the-rat
#3
U Coffeen, A Canseco-Alba, K Simón-Arceo, A Almanza, F Mercado, M León-Olea, F Pellicer
BACKGROUND: Neuropathic pain is one of the most important challenges in public health. The search for novel treatments is important for an adequate relief without adverse effects. In this sense salvinorin A (SA), the main diterpene of the medicinal plant Salvia divinorum is an important antinociceptive compound, which acts as a potent agonist of kappa opioid receptor (KOR) and cannabinoid CB1 receptors. METHODS: We evaluated nociceptive responses in a neuropathic pain model induced by the sciatic nerve ligature (SNL) in the right hind paw, after the microinjection of SA, Salvinorin B (SB), KOR and CB1 antagonists directly in the insular cortex (IC) in male wistar rats...
October 4, 2017: European Journal of Pain: EJP
https://www.readbyqxmd.com/read/28967368/is-cannabis-an-effective-treatment-for-joint-pain
#4
REVIEW
Richard J Miller, Rachel E Miller
Cannabis has been used to treat pain for thousands of years. However, since the early part of the 20th century, laws restricting cannabis use have limited its evaluation using modern scientific criteria. Over the last decade, the situation has started to change because of the increased availability of cannabis in the United States for either medical or recreational purposes, making it important to provide the public with accurate information as to the effectiveness of the drug for joint pain among other indications...
September 2017: Clinical and Experimental Rheumatology
https://www.readbyqxmd.com/read/28963716/the-monoacylglycerol-lipase-inhibitor-kml29-with-gabapentin-synergistically-produces-analgesia-in-mice
#5
Molly S Crowe, Catheryn D Wilson, Emma Leishman, Paul L Prather, Heather B Bradshaw, Matthew L Banks, Steven G Kinsey
BACKGROUND AND PURPOSE: Gabapentin (GBP) is commonly prescribed for nerve pain but may also cause dizziness, sedation, and gait disturbances. Similarly, inhibition of the endogenous cannabinoid enzyme monoacylglycerol lipase (MAGL) has antinociceptive and anti-inflammatory properties, but also induces sedation in mice at high doses. To limit these side effects, the present study investigated the analgesic effects of coadministering a MAGL inhibitor with GBP. EXPERIMENTAL APPROACH: Mice subjected to the chronic constriction injury (CCI) model of neuropathic pain were administered the MAGL inhibitor KML29 (1-40 mg kg(-1) , i...
September 29, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28952976/effects-of-morphine-cp55940-mixtures-on-an-impulsive-choice-task-in-rhesus-monkeys
#6
Vanessa Minervini, Charles P France
µ-Opioid receptor agonists are commonly used to treat pain despite their adverse effects. In preclinical studies, cannabinoid receptor agonists increase the potency of opioids for producing antinociceptive but not reinforcing effects. It is unknown whether other adverse effects of these drugs, such as impairment of complex behavior, are enhanced by their co-administration. This study characterized the effects of morphine (µ-opioid receptor agonist; 0.32-5.6 mg/kg, subcutaneously) and CP55940 (CB1/CB2 cannabinoid receptor agonist; 0...
September 25, 2017: Behavioural Pharmacology
https://www.readbyqxmd.com/read/28947487/cannabinoid-cb1-discrimination-effects-of-endocannabinoids-and-catabolic-enzyme-inhibitors
#7
Michael Z Leonard, Shakiru O Alapafuja, Lipin Ji, Vidyanand G Shukla, Yingpeng Liu, Spyros P Nikas, Alexandros Makriyannis, Jack Bergman, Brian D Kangas
An improved understanding of the endocannabinoid system has provided new avenues of drug discovery and development toward the management of pain and other behavioral maladies. Exogenous cannabinoid type-1 (CB1) receptor agonists such as Δ9-tetrahydrocannabinol are increasingly utilized for their medicinal actions; however, their utility is constrained by concern regarding abuse-related subjective effects. This has led to growing interest in the clinical benefit of indirectly enhancing the activity of the highly labile endocannabinoids N-arachidonoylethanolamine (anandamide; AEA) and/or 2-arachidonoylglycerol (2-AG) via catabolic enzyme inhibition...
September 25, 2017: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/28942644/an-endocannabinoid-uptake-inhibitor-from-black-pepper-exerts-pronounced-anti-inflammatory-effects-in-mice
#8
Inés Reynoso Moreno, Israel Najar-Guerrero, Noe Escareno, Mario Eduardo Flores, Jürg Gertsch, Juan Manuel Viveros-Paredes
Guineensine is a dietary N-isobutylamide widely present in black and long pepper (Piper nigrum and P. longum) previously shown to inhibit cellular endocannabinoid uptake. Given the role of endocannabinoids in inflammation and pain reduction, here we evaluated guineensine in mouse models of acute and inflammatory pain and endotoxemia. Significant dose-dependent anti-inflammatory effects (95.6 ± 3.1 % inhibition of inflammatory pain at 2.5 mg/kg i.p. and 50.0 ± 15.9 % inhibition of edema formation at 5 mg/kg i...
September 24, 2017: Journal of Agricultural and Food Chemistry
https://www.readbyqxmd.com/read/28930612/genetic-addiction-risk-score-gars-%C3%A2-a-predictor-of-vulnerability-to-opioid-dependence
#9
Kenneth Blum, Amanda L C Chen, Panayotis K Thanos, Marcelo Febo, Zsolt Demetrovics, Kristina Dushaj, Abraham Kovoor, David Baron, David E Smith, Alphonso Kenison Roy Iii, Lyle Fried, Thomas J H Chen, Edwin Chapman, Edward Modestino, Bruce Steinberg, Rajendra D Badgaiyan
The interaction of neurotransmitters and genes that control the release of dopamine is the Brain Reward Cascade (BRC). Variations within the BRC, whether genetic or epigenetic, may predispose individuals to addictive behaviors and altered pain tolerance. This discussion authored by a group of concerned scientists and clinicians examines the Genetic Addiction Risk Score (GARS), the first test to accurately predict vulnerability to pain, addiction, and other compulsive behaviors, defined as Reward Deficiency Syndrome (RDS)...
January 1, 2018: Frontiers in Bioscience (Elite Edition)
https://www.readbyqxmd.com/read/28917977/the-role-of-the-endocannabinoid-system-in-the-antihyperalgesic-effect-of-cedrus-atlantica-essential-oil-inhalation-in-a-mouse-model-of-postoperative-pain
#10
Aline Armiliato Emer, Nathalia Nahas Donatello, Ana Paula Batisti, Luiz Augusto Oliveira Belmonte, Adair R S Santos, Daniel F Martins
ETHNOPHARMACOLOGICAL RELEVANCE: Cedar is part of the phylum of conifers, and it's essential oil has been used for therapeutic purposes since ancient times. In our previous study, we have demonstrated that the inhalation of the Cedrus atlantica essential oil (CaEO) induces an antihyperalgesic effect in a model of postoperative pain. But the mechanism that underlies this effect is not yet fully known. AIM OF THE STUDY: This study investigates the involvement of the endocannabinoid system in the antihyperalgesic effect produced by the inhalation of CaEO in a post operative pain model...
September 14, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28914627/antinociceptive-effects-of-jwh015-in-female-and-male-rats
#11
Rebecca M Craft, Nicholas Z Greene, Alexa A Wakley
Despite greater chronic pain prevalence in females compared with males, and the analgesic potential of cannabinoid receptor type 2 (CB2) agonists, CB2 agonists have rarely been tested in females. The aim of the present study was to compare the antinociceptive effects of a CB2-preferring agonist, (2-methyl-1-propyl-1H-indol-3-yl)-1-naphthalenylmethanone (JWH015), in female and male rats against acute pain and persistent inflammatory pain. JWH015 (5-20 mg/kg, intraperitoneally) produced dose-dependent and time-dependent increases in latency to respond on the tail withdrawal and paw pressure tests that did not differ statistically between the sexes...
September 13, 2017: Behavioural Pharmacology
https://www.readbyqxmd.com/read/28771697/effects-of-centrally-administered-endocannabinoids-and-opioids-on-orofacial-pain-perception-in-rats
#12
Marek Zubrzycki, Anna Janecka, Andreas Liebold, Mechthild Ziegler, Maria Zubrzycka
BACKGROUND AND PURPOSE: Endocannabinoids and opioids play a vital role in mediating pain-induced analgesia. The specific effects of these compounds within orofacial region are largely unknown. In this study we tried to determine whether the increase of cannabinoid and opioid concentration in cerebrospinal fluid affects impulse transmission between the motor centers localized in the vicinity of the third and fourth cerebral ventricles. EXPERIMENTAL APPROACH: The study objectives were realized on rats using the method allowing to record the amplitude of evoked tongue jerks (ETJ) in response to noxious tooth pulp stimulation...
August 3, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28758232/administrations-of-thalidomide-into-the-rostral-ventromedial-medulla-produce-antinociceptive-effects-in-a-rat-model-of-postoperative-pain
#13
Tieying Song, Xiaojing Ma, Pengyu Ma, Kunfeng Gu, Jianhui Zhao, Yunliang Yang, Bo Jiang, Yuxia Li, Chunping Wang
The rostral ventromedial medulla (RVM) is highly involved in pain signal transmissions. Previous studies have shown that thalidomide is anti-nociceptive. Thus, we evaluated the neurobiological mechanisms of thalidomide in the RVM in the regulation of postoperative pain. We used a rat model of postoperative pain to investigate the effects of intra-RVM thalidomide treatments on postoperative pain, and evaluate the role of cannabinoid receptors in the effects of intra-RVM thalidomide treatments on GABAergic neurotransmission in the RVM neurons...
July 31, 2017: Journal of Neuroscience Research
https://www.readbyqxmd.com/read/28750813/methods-for-the-development-of-in-silico-gpcr-models
#14
Paula Morales, Dow P Hurst, Patricia H Reggio
The Reggio group has constructed computer models of the inactive and G-protein-activated states of the cannabinoid CB1 and CB2 receptors, as well as, several orphan receptors that recognize a subset of cannabinoid compounds, including GPR55 and GPR18. These models have been used to design ligands, mutations, and covalent labeling studies. The resultant second-generation models have been used to design ligands with improved affinity, efficacy, and subtype selectivity. Herein, we provide a guide for the development of GPCR models using the most recent orphan receptor studied in our lab, GPR3...
2017: Methods in Enzymology
https://www.readbyqxmd.com/read/28750809/assessing-allosteric-modulation-of-cb1-at-the-receptor-and-cellular-levels
#15
Caitlin E Scott, Debra A Kendall
The cannabinoid CB1 receptor is abundant in the central nervous system and regulates neuronal transmission and other key physiological processes including those leading to pain, inflammation, memory, and feeding behavior. CB1 is activated by the endogenous ligands, arachidonoyl ethanolamine and 2-arachidonoyl glycerol, by various synthetic ligands (e.g., CP55940), and by Δ(9)-tetrahydrocannabinol, the psychoactive component of Cannabis sativa. These CB1 ligands are orthosteric and transduce downstream signals by binding CB1 and primarily inducing Gi coupling, but Gs and β-arrestin coupling are also possible...
2017: Methods in Enzymology
https://www.readbyqxmd.com/read/28729222/antiallodynic-effect-of-%C3%AE-caryophyllene-on-paclitaxel-induced-peripheral-neuropathy-in-mice
#16
Gabriela C Segat, Mariane N Manjavachi, Daiane O Matias, Giselle F Passos, Cristina Setim Freitas, Robson Costa, João B Calixto
Painful peripheral neuropathy is a common side effect of paclitaxel (PTX). The use of analgesics is an important component for management of PTX-induced peripheral neuropathy (PINP). However, currently employed analgesics have several side effects and are poorly effective. β-caryophyllene (BCP), a dietary selective CB2 agonist, has shown analgesic effect in neuropathic pain models, but its role in chemotherapy-induced neuropathic pain has not yet been investigated. Herein, we used the mouse model of PINP to show the therapeutic effects of BCP in this neuropathy...
July 18, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28722246/delta-9-tetrahydrocannabinol-decreases-masticatory-muscle-sensitization-in-female-rats-through-peripheral-cannabinoid-receptor-activation
#17
H Wong, S Hossain, B E Cairns
BACKGROUND: This study investigated whether intramuscular injection of delta-9-tetrahydrocannabinol (THC), by acting on peripheral cannabinoid (CB) receptors, could decrease nerve growth factor (NGF)-induced sensitization in female rat masseter muscle; a model which mimics the symptoms of myofascial temporomandibular disorders. METHODS: Immunohistochemistry was used to explore the peripheral expression of cannabinoid receptors in the masseter muscle while behavioural and electrophysiology experiments were employed to assess the functional effects of intramuscular injection of THC...
July 18, 2017: European Journal of Pain: EJP
https://www.readbyqxmd.com/read/28695708/targeting-fatty-acid-amide-hydrolase-and-transient-receptor-potential-vanilloid-1-simultaneously-to-modulate-colonic-motility-and-visceral-sensation-in-the-mouse-a-pharmacological-intervention-with-n-arachidonoyl-serotonin-aa-5-ht
#18
M Bashashati, J Fichna, F Piscitelli, R Capasso, A A Izzo, A Sibaev, J-P Timmermans, N Cenac, N Vergnolle, V Di Marzo, M Storr
BACKGROUND: Endocannabinoid anandamide (AEA) inhibits intestinal motility and visceral pain, but it may also be proalgesic through transient receptor potential vanilloid-1 (TRPV1). AEA is degraded by fatty acid amide hydrolase (FAAH). This study explored whether dual inhibition of FAAH and TRPV1 reduces diarrhea and abdominal pain. METHODS: Immunostaining was performed on myenteric plexus of the mouse colon. The effects of the dual FAAH/TRPV1 inhibitor AA-5-HT on electrically induced contractility, excitatory junction potential (EJP) and fast (f) and slow (s) inhibitory junction potentials (IJP) in the mouse colon, colonic propulsion and visceromotor response (VMR) to rectal distension were studied...
July 11, 2017: Neurogastroenterology and Motility: the Official Journal of the European Gastrointestinal Motility Society
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
#19
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...
September 2017: Experimental Neurology
https://www.readbyqxmd.com/read/28597570/pharmaco-toxicological-effects-of-the-novel-third-generation-fluorinate-synthetic-cannabinoids-5f-adbinaca-ab-fubinaca-and-sts-135-in-mice-in-vitro-and-in-vivo-studies
#20
Isabella Canazza, Andrea Ossato, Fabrizio Vincenzi, Adolfo Gregori, Fabiana Di Rosa, Federica Nigro, Alessandro Rimessi, Paolo Pinton, Katia Varani, Pier Andrea Borea, Matteo Marti
INTRODUCTION: 5F-ADBINACA, AB-FUBINACA, and STS-135 are 3 novel third-generation fluorinate synthetic cannabinoids that are illegally marketed as incense, herbal preparations, or research chemicals for their psychoactive cannabis-like effects. METHODS: The present study aims at investigating the in vitro and in vivo pharmacological activity of 5F-ADBINACA, AB-FUBINACA, and STS-135 in male CD-1 mice, comparing their in vivo effects with those caused by the administration of Δ(9) -THC and JWH-018...
June 9, 2017: Human Psychopharmacology
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