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Opioid antagonism

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https://www.readbyqxmd.com/read/27900410/-%C3%AE-bisabolol-reduces-orofacial-nociceptive-behavior-in-rodents
#1
Luana Torres Melo, Mariana Araújo Braz Duailibe, Luciana Moura Pessoa, Flávio Nogueira da Costa, Antonio Eufrásio Vieira-Neto, Ana Paula de Vasconcellos Abdon, Adriana Rolim Campos
The purposes of this study were to evaluate the anti-nociceptive effect of oral and topical administration of (-)-α-bisabolol (BISA) in rodent models of formalin- or cinnamaldehyde-induced orofacial pain and to explore the inhibitory mechanisms involved. Orofacial pain was induced by injecting 1.5% formalin into the upper lip of mice (20 μL) or into the temporomandibular joint (TMJ) of rats (50 μL). In another experiment, orofacial pain was induced with cinnamaldehyde (13.2 μg/lip). Nociceptive behavior was proxied by time (s) spent rubbing the injected area and by the incidence of head flinching...
November 29, 2016: Naunyn-Schmiedeberg's Archives of Pharmacology
https://www.readbyqxmd.com/read/27899885/interacting-cannabinoid-and-opioid-receptors-in-the-nucleus-accumbens-core-control-adolescent-social-play
#2
Antonia Manduca, Olivier Lassalle, Marja Sepers, Patrizia Campolongo, Vincenzo Cuomo, Giovanni Marsicano, Brigitte Kieffer, Louk J M J Vanderschuren, Viviana Trezza, Olivier J J Manzoni
Social play behavior is a highly rewarding, developmentally important form of social interaction in young mammals. However, its neurobiological underpinnings remain incompletely understood. Previous work has suggested that opioid and endocannabinoid neurotransmission interact in the modulation of social play. Therefore, we combined behavioral, pharmacological, electrophysiological, and genetic approaches to elucidate the role of the endocannabinoid 2-arachidonoylglycerol (2-AG) in social play, and how cannabinoid and opioid neurotransmission interact to control social behavior in adolescent rodents...
2016: Frontiers in Behavioral Neuroscience
https://www.readbyqxmd.com/read/27891289/nor-bni-antagonism-of-kappa-opioid-agonist-induced-reinstatement-of-ethanol-seeking-behavior
#3
Erin Harshberger, Emily A Gilson, Kelli Gillett, Jasmine H Stone, Laila El Amrani, Glenn R Valdez
Recent work suggests that the dynorphin (DYN)/kappa opioid receptor (KOR) system may be a key mediator in the behavioral effects of alcohol. The objective of the present study was to examine the ability of the KOR antagonist norbinaltorphimine (nor-BNI) to attenuate relapse to ethanol seeking due to priming injections of the KOR agonist U50,488 at time points consistent with KOR selectivity. Male Wistar rats were trained to self-administer a 10% ethanol solution, and then responding was extinguished. Following extinction, rats were injected with U50,488 (0...
2016: Journal of Addiction
https://www.readbyqxmd.com/read/27890601/tramadol-effects-on-sexual-behavior-in-male-rats-are-mainly-caused-by-its-5-ht-reuptake-blocking-effects
#4
Jocelien D A Olivier, Diana C Esquivel Franco, Ronald Oosting, Marcel Waldinger, Zoltan Sarnyai, Berend Olivier
Tramadol is a well-known and effective analgesic. Recently it was shown that tramadol is also effective in human premature ejaculation. The inhibitory effect of tramadol on the ejaculation latency is probably due to its mechanism of action as a μ-opioid receptor agonist and noradrenaline/serotonin (5-HT) reuptake inhibitor. In order to test this speculation, we tested several doses of tramadol in a rat model of male sexual behavior and investigated two types of drugs interfering with the μ-opioid and the 5-HT system...
November 24, 2016: Neuropharmacology
https://www.readbyqxmd.com/read/27818236/a-role-for-the-mu-opioid-receptor-in-the-antidepressant-effects-of-buprenorphine
#5
Shivon A Robinson, Rebecca L Erickson, Caroline A Browne, Irwin Lucki
Buprenorphine (BPN), a mixed opioid drug with high affinity for mu (MOR) and kappa (KOR) opioid receptors, has been shown to produce behavioral responses in rodents that are similar to those of antidepressant and anxiolytic drugs. Although recent studies have identified KORs as a primary mediator of BPN's effects in rodent models of depressive-like behavior, the role of MORs in BPN's behavioral effects has not been as well explored. The current studies investigated the role of MORs in mediating conditioned approach behavior in the novelty-induced hypophagia (NIH) test, a behavioral measure previously shown to be sensitive to chronic treatment with antidepressant drugs...
November 3, 2016: Behavioural Brain Research
https://www.readbyqxmd.com/read/27799813/local-analgesic-effect-of-tramadol-is-mediated-by-opioid-receptors-in-late-postoperative-pain-after-plantar-incision-in-rats
#6
José Oswaldo de Oliveira Junior, Milena Fernandes de Freitas, Carolina Bullara de Andrade, Marucia Chacur, Hazem Adel Ashmawi
Tramadol is a drug used to treat moderate to severe pain. It is known to present a peripheral effect, but the local mechanisms underlying its actions remain unclear. The role of peripheral opioid receptors in postoperative pain is not well understood. In the present study, we examined the peripheral opioid receptors to determine the local effect of tramadol in a plantar incision pain model. Rats were subjected to plantar incision and divided into four groups on postoperative day (POD) 1: SF_SF, 0.9% NaCl injected into the right hindpaw; SF_TraI, 0...
2016: Journal of Pain Research
https://www.readbyqxmd.com/read/27725218/opioid-subtype-and-cell-type-dependent-regulation-of-inhibitory-synaptic-transmission-in-the-rat-insular-cortex
#7
Eiko Yokota, Yuko Koyanagi, Kiyofumi Yamamoto, Yoshiyuki Oi, Noriaki Koshikawa, Masayuki Kobayashi
The insular cortex (IC) plays a principal role in the regulation of pain processing. Although opioidergic agonists depress cortical excitatory synaptic transmission, little is known about opioidergic roles in inhibitory synaptic transmission. In the IC, the opioid receptors differentially regulate the excitatory propagation: agonists of the mu (MOR), delta (DOR), and kappa (KOR) exhibit suppressive, facilitative, and little effects, respectively. Thus, we aimed to examine the effects of opioid receptor agonists on unitary inhibitory postsynaptic currents (uIPSCs) in the IC...
December 17, 2016: Neuroscience
https://www.readbyqxmd.com/read/27715007/dopamine-d3-d2-receptor-antagonist-pf-4363467-attenuates-opioid-drug-seeking-behavior-without-concomitant-d2-side-effects
#8
Travis T Wager, Thomas A Chappie, David Horton, Ramalakshmi Y Chandrasekaran, Brian M Samas, Elizabeth Dunn-Sims, Cathleen Hsu, Nawshaba Nawreen, Michelle A Vanase-Frawley, Rebecca E O'Connor, Christopher Schmidt, Keith Dlugolenski, Nancy C Stratman, Mark J Majchrzak, Bethany L Kormos, David Nguyen, Aarti Sawant-Basak, Andy N Mead
Dopamine receptor antagonism is a compelling molecular target for the treatment of a range of psychiatric disorders, including substance use disorders. From our corporate compound file we identified a structurally unique D3 receptor (D3R) antagonist scaffold, 1. Through a hybrid approach, we merged key pharmacophore elements from 1 and D3 agonist 2 to yield the novel D3R/D2R antagonist PF-4363467 (3). Compound 3 was designed to possess CNS drug-like properties as defined by its CNS MPO desirability score (≥4/6)...
October 7, 2016: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/27700049/pharmacodynamic-relationships-between-duration-of-action-of-jdtic-like-kappa-opioid-receptor-antagonists-and-their-brain-and-plasma-pharmacokinetics-in-rats
#9
S Michael Owens, Gerald T Pollard, James L Howard, Timothy R Fennell, Rodney W Snyder, F Ivy Carroll
JDTic is a potent and selective κ-opioid receptor (KOR) antagonist that reverses U50,488-induced diuresis in rats. It partitions into brain with a duration of action lasting for weeks. In a search for KOR antagonists that do not accumulate in the brain, we compared single doses of five methylated JDTic analogs (RTI-97, -194, -212, -240, and -241) for reversal of U50,488 diuresis and pharmacokinetic (PK) properties. All six compounds showed potent and selective KOR antagonism in a [(35)S]GTPγS binding assay...
October 4, 2016: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/27659699/opioid-receptor-antagonism-increases-pain-and-decreases-pleasure-in-obese-and-non-obese-individuals
#10
Rebecca C Price, Nicolas V Christou, Steven B Backman, Laura Stone, Petra Schweinhardt
RATIONALE: Endogenous opioids inhibit nociceptive processing and promote the experience of pleasure. It has been proposed that pain and pleasure lie at opposite ends of an affective spectrum, but the relationship between pain and pleasure and the role of opioids in mediating this relationship has not been tested. OBJECTIVES: Here, we used obese individuals as a model of a dysfunctional opioid system to assess the role of the endogenous opioid peptide, beta-endorphin, on pain and pleasure sensitivity...
September 22, 2016: Psychopharmacology
https://www.readbyqxmd.com/read/27638296/opioid-use-after-propofol-or-sevoflurane-anesthesia-a-randomized-trial
#11
Marita Windpassinger, Olga Plattner, Jana Gemeiner, Kornelia Böhler, Robert Luntzer, Walter Klimscha, Dongsheng Yang, Edward J Mascha, Daniel I Sessler
BACKGROUND: The intravenous anesthetic propofol is a gamma-aminobutyric acid A receptor agonist. Propofol promotes analgesia by depressing nociceptive transmission in peripheral neurons, antagonizing N-methyl-D-aspartate receptors, and activating gamma-aminobutyric acid A receptors in dorsal root ganglion receptor cells. Nevertheless, it remains unclear whether intraoperative propofol causes clinically meaningful postoperative analgesia. We therefore tested the hypothesis that patients anesthetized with sevoflurane require a greater quantity of postoperative opioids (from the end of surgery until the next postoperative morning) than those anesthetized with propofol...
November 2016: Canadian Journal of Anaesthesia, Journal Canadien D'anesthésie
https://www.readbyqxmd.com/read/27637375/antinociceptive-effects-of-the-6-o-sulfate-ester-of-morphine-in-normal-and-diabetic-rats-comparative-role-of-mu-and-delta-opioid-receptors
#12
Jai Shankar K Yadlapalli, Benjamin M Ford, Amit Ketkar, Anqi Wan, Narasimha R Penthala, Robert L Eoff, Paul L Prather, Maxim Dobretsov, Peter A Crooks
: This study determined the antinociceptive effects of morphine and morphine-6-O-sulfate (M6S) in both normal and diabetic rats, and evaluated the comparative role of mu-opioid receptors (mu-ORs) and delta-opioid receptors (delta-ORs) in the antinociceptive action of these opioids. In vitro characterization of mu-OR and delta-OR-mediated signaling by M6S and morphine in stably transfected Chinese hamster ovary (CHO-K1) cells showed that M6S exhibited a 6-fold higher affinity for delta-ORs and modulated G-protein and adenylyl cyclase activity via delta-ORs more potently than morphine...
November 2016: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
https://www.readbyqxmd.com/read/27634339/epoxy-fatty-acids-mediate-analgesia-in-murine-diabetic-neuropathy
#13
K Wagner, K S S Lee, J Yang, B D Hammock
BACKGROUND: Neuropathic pain is a debilitating condition with no adequate therapy. The health benefits of omega-3 fatty acids are established, however, the role of docosahexaenoic acid (DHA) in limiting pain has only recently been described and the mechanisms of this action remain unknown. DHA is metabolized into epoxydocosapentanoic acids (EDPs) via cytochrome P450 (CYP450) enzymes which are substrates for the soluble epoxide hydrolase (sEH) enzyme. Here, we tested several hypotheses; first, that the antinociceptive action of DHA is mediated by the EDPs...
September 15, 2016: European Journal of Pain: EJP
https://www.readbyqxmd.com/read/27607020/versatile-picklocks-to-access-all-opioid-receptors-tuning-the-selectivity-and-functional-profile-of-the-cyclotetrapeptide-c-phe-d-pro-phe-trp-cj-15-208
#14
Rossella De Marco, Andrea Bedini, Santi Spampinato, Lorenzo Cavina, Edoardo Pirazzoli, Luca Gentilucci
Recently, the tryptophan-containing noncationizable opioid peptides emerged with atypical structure and unexpected in vivo activity. Herein, we describe analogs of the naturally occurring mixed κ/μ-ligand c[Phe-d-Pro-Phe-Trp] 1 (CJ-15,208). Receptor affinity, selectivity, and agonism/antagonism varied upon enlarging macrocycle size, giving the μ-agonist 9 or the δ-antagonist 10 characterized by low nanomolar affinity. In particular, the μ-agonist c[β-Ala-d-Pro-Phe-Trp] 9 was shown to elicit potent antinociception in a mouse model of visceral pain upon systemic administration...
October 13, 2016: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27606669/take-home-naloxone-treatment-for-opioid-emergencies-a-comparison-of-routes-of-administration-and-associated-delivery-systems
#15
Mark J Elzey, Jeffrey Fudin, Eric S Edwards
INTRODUCTION: Naloxone reversal of opioid-induced respiratory depression outside of medical facilities has become more prevalent because of the escalating opioid epidemic in the USA. Take-home naloxone for treatment of opioid emergencies is now being recommended by numerous federal, state, and professional organizations. AREAS COVERED: The scope of the opioid overdose epidemic is reviewed along with practical, clinical, regulatory, and usability considerations for take-home naloxone routes of administration currently available and associated delivery systems...
September 8, 2016: Expert Opinion on Drug Delivery
https://www.readbyqxmd.com/read/27600945/the-%C3%AE-1-opioid-receptor-and-5-ht2a-and-5ht2c-serotonergic-receptors-of-the-locus-coeruleus-are-critical-in-elaborating-hypoalgesia-induced-by-tonic-and-tonic-clonic-seizures
#16
Renato Leonardo de Freitas, Priscila Medeiros, Juliana Almeida da Silva, Rithiele Cristina de Oliveira, Ricardo de Oliveira, Farhad Ullah, Asmat Ullah Khan, Norberto Cysne Coimbra
It has been proposed that the post-ictal state is associated with the expression of hypoalgesia. It is clear that the projections among the periaqueductal gray matter (PAG), dorsal raphe nucleus (DRN) and locus coeruleus (LC) play a role in pain management. These mesencephalic structures have direct reciprocal opioid and monoaminergic projections to the LC that can possibly modulate post-ictal hypoalgesia. The goal of this study was to examine if LC-opioid and serotonergic/noradrenergic mechanisms signal the post-ictal hypoalgesic responses to tonic-clonic seizures produced by intraperitoneal administration of pentylenetetrazole (PTZ at 64mg/kg), causing an ionophore γ-aminobutyric acid (GABA)-mediated Cl(-) influx antagonism...
November 12, 2016: Neuroscience
https://www.readbyqxmd.com/read/27582887/the-role-of-naloxegol-in-the-management-of-opioid-induced-bowel-dysfunction
#17
REVIEW
Wojciech Leppert, Jaroslaw Woron
Opioid-induced constipation (OIC) and other gastrointestinal (GI) symptoms of opioid-induced bowel dysfunction (OIBD) significantly deteriorate patients' quality of life and may lead to noncompliance with opioid schedule and undertreatment of pain. Although traditional oral laxatives are the first-line treatment of OIC, they do not address OIBD pathophysiology, and display numerous adverse effects. OIC treatment includes prokinetics (lubiprostone), opioid switch, and changing route of opioid administration...
September 2016: Therapeutic Advances in Gastroenterology
https://www.readbyqxmd.com/read/27576790/challenges-to-develop-novel-anti-inflammatory-and-analgesic-drugs
#18
Bálint Botz, Kata Bölcskei, Zsuzsanna Helyes
Chronic inflammatory diseases and persistent pain of different origin represent common medical, social, and economic burden, and their pharmacotherapy is still an unresolved issue. Therefore, there is a great and urgent need to develop anti-inflammatory and analgesic agents with novel mechanisms of action, but it is a very challenging task. The main problem is the relatively large translational gap between the preclinical experimental data and the clinical results due to characteristics of the models, difficulties with the investigational techniques particularly for pain, as well as species differences in the mechanisms...
August 31, 2016: Wiley Interdisciplinary Reviews. Nanomedicine and Nanobiotechnology
https://www.readbyqxmd.com/read/27556704/mitragynine-corynantheidine-pseudoindoxyls-as-opioid-analgesics-with-mu-agonism-and-delta-antagonism-which-do-not-recruit-%C3%AE-arrestin-2
#19
András Váradi, Gina F Marrone, Travis C Palmer, Ankita Narayan, Márton R Szabó, Valerie Le Rouzic, Steven G Grinnell, Joan J Subrath, Evelyn Warner, Sanjay Kalra, Amanda Hunkele, Jeremy Pagirsky, Shainnel O Eans, Jessica M Medina, Jin Xu, Ying-Xian Pan, Attila Borics, Gavril W Pasternak, Jay P McLaughlin, Susruta Majumdar
Natural products found in Mitragyna speciosa, commonly known as kratom, represent diverse scaffolds (indole, indolenine, and spiro pseudoindoxyl) with opioid activity, providing opportunities to better understand opioid pharmacology. Herein, we report the pharmacology and SAR studies both in vitro and in vivo of mitragynine pseudoindoxyl (3), an oxidative rearrangement product of the corynanthe alkaloid mitragynine. 3 and its corresponding corynantheidine analogs show promise as potent analgesics with a mechanism of action that includes mu opioid receptor agonism/delta opioid receptor antagonism...
September 22, 2016: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/27556438/antinociceptive-effect-of-3-2-3-dimethoxyphenyl-1-5-methylfuran-2-yl-prop-2-en-1-one-in-mice-models-of-induced-nociception
#20
Nur Izzati Ismail, Lee Ming-Tatt, Nordin Lajis, Muhammad Nadeem Akhtar, Ahmad Akira, Enoch Kumar Perimal, Daud Ahmad Israf, Mohd Roslan Sulaiman
The antinociceptive effects produced by intraperitoneal administration of a novel synthetic chalcone, 3-(2,3-dimethoxyphenyl)-1-(5-methylfuran-2-yl)prop-2-en-1-one (DMFP), were investigated in several mouse models of induced nociception. The administration of DMFP (0.1, 0.5, 1.0 and 5.0 mg/kg) produced significant attenuation on the acetic acid-induced abdominal-writhing test. It also produced a significant increase in response latency time in the hot-plate test and a marked reduction in time spent licking the injected paw in both phases of the formalin-induced paw-licking test...
2016: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
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