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Opioid antagonism

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https://www.readbyqxmd.com/read/29864972/oxycodone-and-macrogol-3350-treatment-reduces-anal-sphincter-relaxation-compared-to-combined-oxycodone-and-naloxone-tablets
#1
Jakob Lykke Poulsen, Christina Brock, Debbie Grønlund, Klaus Krogh, Asbjørn Mohr Drewes
Background Opioid analgesics inhibit anal sphincter function and contribute to opioid-induced bowel dysfunction. However, it is unknown if the inhibition can be reduced by opioid antagonism with oral naloxone, and how this compares to osmotic laxative treatment. Aims To compare the effects of oxycodone and macrogol 3350 treatment (OX + PEG) versus combined oral oxycodone and naloxone (OXN) on anal sphincter function and gastrointestinal symptoms. Methods A randomised, double-blind, crossover trial was conducted in 20 healthy, male volunteers...
December 29, 2017: Scandinavian Journal of Pain
https://www.readbyqxmd.com/read/29844727/the-possible-mechanisms-of-protocatechuic-acid-induced-central-analgesia
#2
Rana Arslan, Sule Aydin, Dilara Nemutlu Samur, Nurcan Bektas
It is aimed to investigate the central antinociceptive effect of protocatechuic acid and the involvement of stimulation of opioidergic, serotonin 5-HT2A/2C , α2-adrenergic and muscarinic receptors in protocatechuic acid-induced central analgesia in mice. Time-dependent antinociceptive effects of protocatechuic acid at the oral doses of 75, 150 and 300 mg/kg were tested in hot-plate (integrated supraspinal response) and tail-immersion (spinal reflex) tests in mice. To investigate the mechanisms of action; the mice administered 300 mg/kg protocatechuic acid (p...
May 2018: Saudi Pharmaceutical Journal: SPJ: the Official Publication of the Saudi Pharmaceutical Society
https://www.readbyqxmd.com/read/29780163/heteromerization-of-%C3%AE-opioid-receptor-and-cholecystokinin-b-receptor-through-the-third-transmembrane-domain-of-the-%C3%AE-opioid-receptor-contributes-to-the-anti-opioid-effects-of-cholecystokinin-octapeptide
#3
Yin Yang, Qian Li, Qi-Hua He, Ji-Sheng Han, Li Su, You Wan
Activation of the cholecystokinin type B receptor (CCKBR) by cholecystokinin octapeptide (CCK-8) inhibits opioid analgesia. Chronic opiate treatment leads to an increase in the CCK-8 concentration and thus enhances the antagonism of CCK-8 against opioid analgesia; the underlying molecular mechanisms remain of great interest. In the present study, we validated the colocalization of the μ-opioid receptor (MOR) and CCKBR in pain signal transmission-related spinal cord dorsal horn and dorsal root ganglion neurons of rats...
May 21, 2018: Experimental & Molecular Medicine
https://www.readbyqxmd.com/read/29772497/the-role-of-the-vasopressin-system-and-dopamine-d1-receptors-in-the-effects-of-social-housing-condition-on-morphine-reward
#4
M L Shawn Bates, Rebeca S Hofford, Michael A Emery, Paul J Wellman, Shoshana Eitan
BACKGROUND: The association with opioid-abusing individuals or even the perception of opioid abuse by peers are risk factors for the initiation and escalation of abuse. Similarly, we demonstrated that morphine-treated animals housed with only morphine-treated animals (referred to as morphine only) acquire morphine conditioned place-preference (CPP) more readily than morphine-treated animals housed with drug-naïve animals (referred to as morphine cage-mates). However, the molecular mechanisms underlying these effects are still elusive...
April 22, 2018: Drug and Alcohol Dependence
https://www.readbyqxmd.com/read/29766045/post-stroke-intranasal-naloxone-delivery-reduces-microglial-activation-and-improves-behavioral-recovery-from-ischemic-injury
#5
Jenni E Anttila, Katrina Albert, Emily S Wires, Kert Mätlik, Lisa C Loram, Linda R Watkins, Kenner C Rice, Yun Wang, Brandon K Harvey, Mikko Airavaara
Ischemic stroke is the leading cause of disability, and effective therapeutic strategies are needed to promote complete recovery. Neuroinflammation plays a significant role in stroke pathophysiology, and there is limited understanding of how it affects recovery. The aim of this study was to characterize the spatiotemporal expression profile of microglial activation and whether dampening microglial/macrophage activation post-stroke facilitates the recovery. For dampening microglial/macrophage activation, we chose intranasal administration of naloxone, a drug that is already in clinical use for opioid overdose and is known to decrease microglia/macrophage activation...
March 2018: ENeuro
https://www.readbyqxmd.com/read/29710079/neurobiology-of-opioid-use-disorder-and-comorbid-traumatic-brain-injury
#6
Thomas R Kosten, David P Graham, David A Nielsen
Importance: Treating patients with opioid use disorder (OUD) and traumatic brain injury illustrates 6 neurobiological principles about the actions of 2 contrasting opioid analgesics, morphine and fentanyl, as well as pharmacotherapies for OUD, methadone, naltrexone, and buprenorphine. Observations: This literature review focused on a patient with traumatic brain injury who developed OUD from chronic morphine analgesia. His treatment is described in a neurobiological framework of 6 opioid action principles...
June 1, 2018: JAMA Psychiatry
https://www.readbyqxmd.com/read/29708942/a-bifunctional-biased-mu-opioid-agonist-neuropeptide-ff-receptor-antagonist-as-analgesic-with-improved-acute-and-chronic-side-effects
#7
Armand Drieu la Rochelle, Karel Guillemyn, Maria Dumitrascuta, Charlotte Martin, Valérie Utard, Raphaëlle Quillet, Séverine Schneider, François Daubeuf, Tom Willemse, Pieter Mampuys, Bert U W Maes, Nelly Frossard, Frédéric Bihel, Mariana Spetea, Frédéric Simonin, Steven Ballet
Opioid analgesics, such as morphine, oxycodone and fentanyl, are the cornerstones for treating moderate to severe pain. However, upon chronic administration, their efficiency is limited by prominent side effects such as analgesic tolerance and dependence liability. Neuropeptide FF (NPFF) and its receptors (NPFF1R and NPFF2R) are recognized as an important pronociceptive system involved in opioid-induced hyperalgesia and analgesic tolerance. Herein, we report the design of multitarget peptidomimetic compounds that show high affinity binding to the mu opioid receptor (MOPr) and NPFFRs...
April 26, 2018: Pain
https://www.readbyqxmd.com/read/29693947/use-of-sugammadex-in-a-patient-with-myotonic-dystrophy-undergoing-laparoscopic-cholecystectomy
#8
Rieko Uno, Shoko Matsuda, Kohei Murao, Kumiko Nakamura, Michiyo Shirakawa, Koh Shingu
A 37-year-old female patient with myotonic dystrophy was scheduled for laparoscopic cholecystectomy for gall stone under general anesthesia with continuous propofol infusion. Rocuronium was administered with careful monitoring using TOF- Watch®, measuring train-of-four count (Tc), TOF ratio (Tr), and posttetanic count The total amount of rocuronium was 70 mg ; 0.6 mg .kg⁻1 for anesthetic induction and 0.3 mg .kg⁻1 when Tc exceeded 1. When the operation was completed, Tc was 4, Tr was uncountable and she showed reaction to calling her name...
May 2017: Masui. the Japanese Journal of Anesthesiology
https://www.readbyqxmd.com/read/29674333/intravenous-and-intratracheal-thyrotropin-releasing-hormone-and-its-analog-taltirelin-reverse-opioid-induced-respiratory-depression-in-isoflurane-anesthetized-rats
#9
James D Boghosian, Anita Luethy, Joseph F Cotten
Thyrotropin releasing hormone (TRH) is a tripeptide hormone and a neurotransmitter widely expressed in the central nervous system that regulates thyroid function and maintains physiologic homeostasis. Following injection in rodents, TRH has multiple effects including increased blood pressure and breathing. We tested the hypothesis that TRH and its long-acting analog, taltirelin, will reverse morphine-induced respiratory depression in anesthetized rats following intravenous or intratracheal (IT) administration...
July 2018: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/29663315/pro-region-engineering-of-nerve-growth-factor-by-deep-mutational-scanning-enables-a-yeast-platform-for-conformational-epitope-mapping-of-anti-ngf-monoclonal-antibodies
#10
Angélica V Medina-Cucurella, Yaqi Zhu, Scott J Bowen, Lisa M Bergeron, Timothy A Whitehead
Nerve growth factor (NGF) plays a central role in multiple chronic pain conditions. As such, anti-NGF monoclonal antibodies (mAbs) that function by antagonizing NGF downstream signaling are leading drug candidates for non-opioid pain relief. To evaluate anti-canine NGF (cNGF) mAbs we sought a yeast surface display platform of cNGF. Both mature cNGF and pro-cNGF displayed on the yeast surface but bound conformationally sensitive mAbs at most 2.5-fold in mean fluorescence intensity above background, suggesting that cNGF was mostly misfolded...
April 16, 2018: Biotechnology and Bioengineering
https://www.readbyqxmd.com/read/29644656/pro-region-engineering-of-nerve-growth-factor-by-deep-mutational-scanning-enables-a-yeast-platform-for-conformational-epitope-mapping-of-anti-ngf-monoclonal-antibodies
#11
Angélica V Medina-Cucurella, Yaqi Zhu, Scott J Bowen, Lisa M Bergeron, Timothy A Whitehead
Nerve growth factor (NGF) plays a central role in multiple chronic pain conditions. As such, anti-NGF monoclonal antibodies (mAbs) that function by antagonizing NGF downstream signaling are leading drug candidates for non-opioid pain relief. To evaluate anti-canine NGF (cNGF) mAbs we sought a yeast surface display platform of cNGF. Both mature cNGF and pro-cNGF displayed on the yeast surface but bound conformationally sensitive mAbs at most 2.5-fold in mean fluorescence intensity above background, suggesting that cNGF was mostly misfolded...
April 12, 2018: Biotechnology and Bioengineering
https://www.readbyqxmd.com/read/29596152/upregulation-of-p2x2-and-p2x3-receptors-in-rats-with-hyperalgesia-induced-by-heroin-withdrawal
#12
Changlong Leng, Lin Chen, Xiaokang Gong, Baomiao Ma, Weimin Gan, Yuanren Si, Huaqiao Xiao, Chaoying Li
Drug dependence and withdrawal syndrome induced by abrupt cessation of opioid administration remain a severe obstacle in the clinical treatment of chronic pain and opioid drug addiction. One of the key symptoms during opioid withdrawal is hyperalgesia. The mechanism of opioid withdrawal-induced hyperalgesia remains unclear. P2X2 and P2X3 receptors, members of P2X receptor subunits, act as the integrator of multiple forms of noxious stimuli and play an important role in nociception transduction of chronic neuropathic and inflammatory pain...
May 23, 2018: Neuroreport
https://www.readbyqxmd.com/read/29580951/modality-specific-peripheral-antinociceptive-effects-of-%C3%AE-opioid-agonists-on-heat-and-mechanical-stimuli-contribution-of-sigma-1-receptors
#13
Ángeles Montilla-García, Gloria Perazzoli, Miguel Á Tejada, Rafael González-Cano, Cristina Sánchez-Fernández, Enrique J Cobos, José M Baeyens
Morphine induces peripherally μ-opioid-mediated antinociception to heat but not to mechanical stimulation. Peripheral sigma-1 receptors tonically inhibit μ-opioid antinociception to mechanical stimuli, but it is unknown whether they modulate μ-opioid heat antinociception. We hypothesized that sigma-1 receptors might play a role in the modality-specific peripheral antinociceptive effects of morphine and other clinically relevant μ-opioid agonists. Mechanical nociception was assessed in mice with the paw pressure test (450 g), and heat nociception with the unilateral hot plate (55 °C) test...
June 2018: Neuropharmacology
https://www.readbyqxmd.com/read/29568976/pharmacokinetics-and-dynamics-of-intramuscular-and-intranasal-naloxone-an-explorative-study-in-healthy-volunteers
#14
Arne Kristian Skulberg, Ida Tylleskar, Turid Nilsen, Sissel Skarra, Øyvind Salvesen, Trond Sand, Thorsteinn Loftsson, Ola Dale
PURPOSE: This study aimed to develop a model for pharmacodynamic and pharmacokinetic studies of naloxone antagonism under steady-state opioid agonism and to compare a high-concentration/low-volume intranasal naloxone formulation 8 mg/ml to intramuscular 0.8 mg. METHODS: Two-way crossover in 12 healthy volunteers receiving naloxone while receiving remifentanil by a target-controlled infusion for 102 min. The group were subdivided into three different doses of remifentanil...
March 22, 2018: European Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/29530590/in-vitro-and-in-vivo-functional-profile-characterization-of-17-cyclopropylmethyl-3-14%C3%AE-dihydroxy-4-5%C3%AE-epoxy-6%C3%AE-isoquinoline-3-carboxamido-morphinan-naq-as-a-low-efficacy-mu-opioid-receptor-modulator
#15
Samuel Obeng, Yunyun Yuan, Abdulmajeed Jali, Dana E Selley, Yan Zhang
Evidence has shown that downstream signaling by mu opioid receptor (MOR) agonists that recruit β-arrestin2 may lead to the development of tolerance. Also, it has been suggested that opioid receptor desensitization and cyclic AMP overshoot contributes to the development of tolerance and occurrence of withdrawal, respectively. Therefore, studies were conducted with 17-cyclopropylmethyl-3,14β-dihydroxy-4,5α-epoxy-6α-(isoquinoline-3-carboxamido)morphinan (NAQ), a MOR selective partial agonist discovered in our laboratory, to characterize its effect on β-arrestin2 recruitment and precipitation of a cyclic AMP overshoot...
May 15, 2018: European Journal of Pharmacology
https://www.readbyqxmd.com/read/29528698/opioids-in-cardiovascular-disease-therapeutic-options
#16
Hemangi Rawal, Bhoomika M Patel
The World Health Organization suggests that the cardiovascular diseases (CVDs) are the major cause of mortality and account for two-thirds of the deaths all over the world. These diseases kill about 17 million people every year and 3 in every 10 deaths are due to these diseases. The past decade has seen considerable improvements in diagnosis as well as treatment of various heart diseases. Various new therapeutic targets are being identified through in-depth knowledge of the disease mechanisms which has favored the testing of new strategies leading to newer treatment options...
January 1, 2018: Journal of Cardiovascular Pharmacology and Therapeutics
https://www.readbyqxmd.com/read/29528663/naltrexone-maintenance-fails-to-alter-amphetamine-effects-on-intracranial-self-stimulation-in-rats
#17
Farhana Sakloth, S Stevens Negus
Pharmacotherapy to treat stimulant use disorders continues to be an unmet medical need. Some evidence supports both the role of opioids in mediating abuse-related amphetamine effects and the potential utility of opioid antagonists as therapeutic candidates for treating amphetamine abuse. This study used intracranial self-stimulation (ICSS) to evaluate effects of exposure to and termination of naltrexone maintenance on rewarding amphetamine effects in an ICSS procedure in rats. Morphine and cocaine were included as positive and negative controls, respectively...
April 2018: Experimental and Clinical Psychopharmacology
https://www.readbyqxmd.com/read/29524385/selectivity-profiling-of-nop-mop-dop-and-kop-receptor-antagonists-in-the-rat-spinal-nerve-ligation-model-of-mononeuropathic-pain
#18
Kris Rutten, Wolfgang Schröder, Thomas Christoph, Thomas Koch, Thomas M Tzschentke
Agonists selectively acting at NOP, MOP, DOP and KOP receptors as well as mixed opioid receptor agonists are known to exert anti-hypersensitive efficacy in the rat spinal nerve ligation (SNL) model of neuropathic pain. To investigate the relative contribution of individual opioid receptor activation to the overall efficacy of mixed opioid receptor agonists, selective doses of respective opioid receptor antagonists have to be employed. In order to identify such selective antagonist doses, doses of the selective NOP, MOP, DOP and KOP receptor agonists Ro65-6570, morphine, SNC-80 and U50488H, that produced maximum efficacy without apparent side effects, were challenged by each of the receptor antagonists J-113397 (NOP receptor), naloxone (MOP receptor), naltrindole (DOP receptor) and nor-binaltorphimine (KOP receptor)...
May 15, 2018: European Journal of Pharmacology
https://www.readbyqxmd.com/read/29499274/role-of-dorsal-hippocampus-%C3%AE%C2%BA-opioid-receptors-in-contextual-aversive-memory-consolidation-in-rats
#19
Felipe Vanz, Maíra Assunção Bicca, Vagner Fagnani Linartevichi, Marcelo Giachero, Leandro José Bertoglio, Thereza C Monteiro de Lima
The main κ opioid receptors (κORs) subtypes already described (κ1 ORs and κ2 ORs) are expressed in brain regions involved in aversive memory consolidation, including the dorsal hippocampus (DH). However, the role of DH κORs in consolidation of aversive memories with varied intensity and specificity is still uncertain. The present study aimed to investigate this question using pharmacological agents in rats subjected to a weak, moderate or strong contextual aversive conditioning (CAC) protocol. Antagonizing DH κORs with nor-binaltorphimine (nor-BNI), immediately after, but not 6 h later, a moderate CAC leads to intensified freezing behavior in the re-exposure to the paired context...
February 27, 2018: Neuropharmacology
https://www.readbyqxmd.com/read/29477761/concurrent-assessment-of-the-antinociceptive-and-behaviorally-disruptive-effects-of-opioids-in-squirrel-monkeys
#20
Sarah L Withey, Carol A Paronis, Jack Bergman
Although the clinical application of opioids for pain management is often hindered by undesired behavioral impairment, preclinical assays of antinociception typically do not provide information regarding the behaviorally disruptive effects of opioids that may accompany their antinociceptive effects. To address this, we modified a warm water tail withdrawal procedure to determine concurrently the effects of opioids on tail withdrawal latency (antinociception) and indices of food-maintained operant behavior (rates of responding and reinforcement density) in squirrel monkeys...
March 2, 2018: Journal of Pain: Official Journal of the American Pain Society
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