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Opioid antagonism

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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
#1
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
#2
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
#3
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...
March 28, 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
#4
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...
March 23, 2018: Neuropharmacology
https://www.readbyqxmd.com/read/29568976/pharmacokinetics-and-dynamics-of-intramuscular-and-intranasal-naloxone-an-explorative-study-in-healthy-volunteers
#5
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
#6
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...
March 9, 2018: European Journal of Pharmacology
https://www.readbyqxmd.com/read/29528698/opioids-in-cardiovascular-disease-therapeutic-options
#7
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
#8
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...
March 12, 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
#9
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)...
March 7, 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
#10
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
#11
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...
February 22, 2018: Journal of Pain: Official Journal of the American Pain Society
https://www.readbyqxmd.com/read/29461271/endothelin-signaling-contributes-to-modulation-of-nociception-in-early-stage-tongue-cancer-in-rats
#12
Akihiko Furukawa, Masamichi Shinoda, Asako Kubo, Kuniya Honda, Ryuta Akasaka, Yoshiyuki Yonehara, Koichi Iwata
BACKGROUND: Patients with early stage tongue cancer do not frequently complain of tongue pain. Endothelin-1 signaling is upregulated in the cancerous tongue at the early stage. We tested the hypothesis that endothelin-1 signaling contributes to the modulation of tongue nociception. METHODS: Squamous cell carcinoma cells were inoculated into the tongue under general anesthesia. Lingual mechanical sensitivity under light anesthesia using forceps from days 1 to 21 (n = 8) and the amounts of endothelin-1 and β-endorphin in the tongue on days 6, 14, and 21 (n = 5 to 7) were examined after the inoculation...
February 15, 2018: Anesthesiology
https://www.readbyqxmd.com/read/29453978/venlafaxine-prevents-morphine-antinociceptive-tolerance-the-role-of-neuroinflammation-and-the-l-arginine-nitric-oxide-pathway
#13
Mohammad Taghi Mansouri, Bahareh Naghizadeh, Behnam Ghorbanzadeh, Soheila Alboghobeish, Neda Amirgholami, Gholamreza Houshmand, Omar Cauli
Opioid-induced neuroinflammation and the nitric oxide (NO) signal-transduction pathway are involved in the development of opioid analgesic tolerance. The antidepressant venlafaxine (VLF) modulates NO in nervous tissues, and so we investigated its effect on induced tolerance to morphine, neuroinflammation, and oxidative stress in mice. Tolerance to the analgesic effects of morphine were induced by injecting mice with morphine (50 mg/kg) once a day for three consecutive days; the effect of co-administration of VLF (5 or 40 mg/kg) with morphine was similarly tested in a separate group...
February 14, 2018: Experimental Neurology
https://www.readbyqxmd.com/read/29274880/cb-1-cannabinoid-receptor-agonist-mouse-vd-hemopressin-%C3%AE-produced-supraspinal-analgesic-activity-in-the-preclinical-models-of-pain
#14
Ting Zheng, Run Zhang, Ting Zhang, Meng-Na Zhang, Biao Xu, Jing-Jing Song, Ning Li, Hong-Hai Tang, Pei Wang, Rui Wang, Quan Fang
Mouse VD-hemopressin(α) (VD-Hpα) is an undecapeptide that selectively activates CB1 cannabinoid receptor in in vitro functional tests, and exerts CB1 -mediated central antinociception in the mouse tail-flick assay. The aim of the present study was to further investigate the analgesic properties of supraspinal mouse VD-Hpα in a range of preclinical pain models. Our results indicated that the classical cannabinoid agonist WIN 55,212-2 produced supraspinal analgesia in preclinical pain models, which was selectively antagonized by the CB1 antagonist/inverse agonist AM251, but not by the CB2 antagonist AM630...
February 1, 2018: Brain Research
https://www.readbyqxmd.com/read/29273415/design-synthesis-and-opioid-activity-of-arodyn-analogs-cyclized-by-ring-closing-metathesis-involving-tyr-allyl
#15
Wei-Jie Fang, Thomas F Murray, Jane V Aldrich
Kappa (κ) opioid receptor selective antagonists are useful pharmacological tools in studying κ opioid receptors and have potential to be used as therapeutic agents for the treatment of a variety of diseases including mood disorders and drug addiction. Arodyn (Ac[Phe1-3 ,Arg4 ,d-Ala8 ]Dyn A-(1-11)NH2 ) is a linear acetylated dynorphin A (Dyn A) analog that is a potent and selective κ opioid receptor antagonist (Bennett et al. J Med Chem 2002;45:5617-5619) and prevents stress-induced reinstatement of cocaine-seeking behavior following central administration (Carey et al...
March 15, 2018: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/29155273/mu-opioid-peptide-mop-and-nociceptin-orphanin-fq-peptide-nop-receptor-activation-both-contribute-to-the-discriminative-stimulus-properties-of-cebranopadol-in-the-rat
#16
Thomas M Tzschentke, Kris Rutten
The novel potent analgesic cebranopadol is an agonist at nociceptin/orphanin FQ peptide (NOP) and classical opioid receptors, with the highest in-vitro activity at NOP and mu-opioid peptide (MOP) receptors, and somewhat lower activity at kappa-opioid peptide (KOP) and delta-opioid peptide (DOP) receptors. We addressed the question of which of these pharmacological activities contribute to the stimulus properties of cebranopadol using a rat drug discrimination procedure. First, cebranopadol was tested in generalization tests against a morphine cue, including receptor-specific antagonism...
February 2018: Neuropharmacology
https://www.readbyqxmd.com/read/29146290/sustained-opioid-antagonism-modulates-striatal-sensitivity-to-baby-schema-in-opioid-use-disorder
#17
An-Li Wang, Steven B Lowen, Igor Elman, Zhenhao Shi, Victoria P Fairchild, Alexander Bouril, Ruben C Gur, Daniel D Langleben
BACKGROUND: Chronic opioid misuse is associated with reduced sensitivity to natural rewards and social motivation deficits that include impaired caregiving. The neurobiological mechanisms underlying these deficits and their response to treatment are not well understood. Baby schema (Kindchenschema) is a set of juvenile physical features, which is perceived as "cute" and triggers motivation for caregiving. Recent studies suggest that the "baby schema effect" is mediated by the brain "reward" network...
February 2018: Journal of Substance Abuse Treatment
https://www.readbyqxmd.com/read/29100992/antagonism-of-the-kappa-opioid-receptor-attenuates-thc-induced-place-aversions-in-adult-male-sprague-dawley-rats
#18
Matthew M Clasen, Shaun M Flax, Briana J Hempel, Kejun Cheng, Kenner C Rice, Anthony L Riley
RATIONALE: Prior research with transgenic mice in which the kappa opioid receptor (KOR) has been suppressed or activated suggests that the aversive effects of THC are mediated by activity of this receptor subtype. If the activity of the KOR system is responsible for mediating the THC's aversive effects, then selective antagonism of the KOR by norBNI should block such aversive effects. To test this hypothesis, rats were pretreated with norBNI 24h prior to place conditioning with THC to assess its effect on the acquisition of THC-induced place aversions...
October 31, 2017: Pharmacology, Biochemistry, and Behavior
https://www.readbyqxmd.com/read/29042247/murine-genetic-variance-in-muscarinic-cholinergic-receptor-antagonism-of-sucrose-and-saccharin-solution-intakes-in-three-inbred-mouse-strains
#19
Faye Bourie, Kerstin Olsson, Ben Iskhakov, Agata Buras, Gabriela Fazilov, Merna Shenouda, Julia Zhezherya, Richard J Bodnar
Nutritive (e.g., sucrose) and non-nutritive (e.g., saccharin) sweeteners stimulate intake in inbred mouse strains. BALB/c, SWR and C57BL/6 mice differ in the ability of dopamine (DA) D1 (SCH23390) and opioid (naltrexone) receptor antagonism to alter sucrose intake. Whereas SCH23390 comparably reduced cumulative sucrose intake in all three strains, naltrexone reduced cumulative sucrose intake maximally in C57/BL/6 mice, in intermediate fashion in BALB/c mice, but not in SWR mice. Whereas cumulative saccharin intake was reduced by DA D1 receptor antagonism in BALB/c and SWR mice, naltrexone was more potent in SWR relative to BALB/c mice...
October 16, 2017: Pharmacology, Biochemistry, and Behavior
https://www.readbyqxmd.com/read/28991118/truncated-%C3%AE-opioid-receptors-with-6-transmembrane-domains-are-essential-for-opioid-analgesia
#20
Zhigang Lu, Jin Xu, Mingming Xu, Grace C Rossi, Susruta Majumdar, Gavril W Pasternak, Ying-Xian Pan
BACKGROUND: Most clinical opioids act through μ-opioid receptors. They effectively relieve pain but are limited by side effects, such as constipation, respiratory depression, dependence, and addiction. Many efforts have been made toward developing potent analgesics that lack side effects. Three-iodobenzoyl-6β-naltrexamide (IBNtxA) is a novel class of opioid active against thermal, inflammatory, and neuropathic pain, without respiratory depression, physical dependence, and reward behavior...
March 2018: Anesthesia and Analgesia
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