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https://www.readbyqxmd.com/read/28546566/a-diastereoselective-synthesis-of-cebranopadol-a-novel-analgesic-showing-nop-mu-mixed-agonism
#1
Anna Fantinati, Sara Bianco, Remo Guerrini, Severo Salvadori, Salvatore Pacifico, Maria Camilla Cerlesi, Girolamo Calo, Claudio Trapella
A diastereoselective synthesis of the title compound as a single E diastereomer has been efficiently accomplished by assembling the featured pyrano-indole scaffold of the spiro[cyclohexane-dihydropyrano[3,4-b]-indole]-amine framework through an oxa-Pictet-Spengler reaction, promoted by a cheap and green Zeolite catalyst. Basic pharmacological experiments demonstrate that Cebranopadol acts as a mixed nociception/orphanin FQ (NOP) and mu (MOP) opioid receptor agonist useful for treatment of chronic pain.
May 25, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28543648/making-the-choices-necessary-to-make-a-difference-the-responsibility-of-national-bioethics-commissions
#2
Christine Grady
In this essay, I offer some reflections on how the topics were identified and approached by the Presidential Commission for the Study of Bioethical Issues, on which I had the honor to serve, in the hope that the reflections may be useful to future national bioethics commissions. In the executive order that established the bioethics commission, President Obama explicitly recognized the ethical imperative to responsibly pursue science, innovation, and advances in biomedical research and health care, and the importance of national attention to these issues...
May 2017: Hastings Center Report
https://www.readbyqxmd.com/read/28541119/treatment-of-opioid-use-disorder-with-ibogaine-detoxification-and-drug-use-outcomes
#3
Thomas Kingsley Brown, Kenneth Alper
BACKGROUND: Ibogaine is a monoterpene indole alkaloid used in medical and nonmedical settings for the treatment of opioid use disorder. Its mechanism of action is apparently novel. There are no published prospective studies of drug use outcomes with ibogaine. OBJECTIVES: To study outcomes following opioid detoxification with ibogaine. METHODS: In this observational study, 30 subjects with DSM-IV Opioid Dependence (25 males, 5 females) received a mean total dose of 1,540 ± 920 mg ibogaine HCl...
May 25, 2017: American Journal of Drug and Alcohol Abuse
https://www.readbyqxmd.com/read/28537555/identification-of-a-novel-spinal-nociceptive-motor-gate-control-for-a%C3%AE-pain-stimuli-in-rats
#4
Dvir Blivis, Gal Haspel, Philip Z Mannes, Michael James O'Donovan, Michael J Iadarola
Physiological responses to nociceptive stimuli are initiated within tens of milliseconds, but the corresponding sub-second behavioral responses have not been adequately explored in awake, unrestrained animals. A detailed understanding of these responses is crucial for progress in pain neurobiology. Here, high-speed videography during nociceptive Aδ fiber stimulation demonstrated engagement of a multi-segmental motor program coincident with, or even preceding, withdrawal of the stimulated paw. The motor program included early head orientation and adjustments of the torso and un-stimulated paws...
May 24, 2017: ELife
https://www.readbyqxmd.com/read/28536900/hopes-for-the-future-of-pain-control
#5
REVIEW
Kirsty Bannister, Mateusz Kucharczyk, Anthony H Dickenson
Here we aim to present an accessible review of the pharmacological targets for pain management, and succinctly discuss the newest trends in pain therapy. A key task for current pain pharmacotherapy is the identification of receptors and channels orchestrating nociception. Notwithstanding peripheral alterations in the receptors and channels following pathophysiological events, the modulatory mechanisms in the central nervous system are also fundamental to the regulation of pain perception. Bridging preclinical and clinical studies of peripheral and central components of pain modulation, we present the different types of pain and relate these to pharmacological interventions...
May 23, 2017: Pain and Therapy
https://www.readbyqxmd.com/read/28536865/the-c-2-derivatives-of-salvinorin-a-ethoxymethyl-ether-sal-b-and-%C3%AE-tetrahydropyran-sal-b-have-anti-cocaine-properties-with-minimal-side-effects
#6
Amy W M Ewald, Peter J Bosch, Aimee Culverhouse, Rachel Saylor Crowley, Benjamin Neuenswander, Thomas E Prisinzano, Bronwyn M Kivell
RATIONALE: Kappa-opioid receptor (KOPr) agonists have pre-clinical anti-cocaine and analgesic effects. However, side effects including sedation, dysphoria, aversion, anxiety and depression limit their therapeutic development. The unique structure of salvinorin A has been used to develop longer acting KOPr agonists. OBJECTIVES: We evaluate two novel C-2 analogues of salvinorin A, ethoxymethyl ether Sal B (EOM Sal B) and β-tetrahydropyran Sal B (β-THP Sal B) alongside U50,488 for their ability to modulate cocaine-induced behaviours and side effects, pre-clinically...
May 23, 2017: Psychopharmacology
https://www.readbyqxmd.com/read/28535130/home-manufacture-of-drugs-an-online-investigation-and-a-toxicological-reality-check-of-online-discussions-on-drug-chemistry
#7
Evelyn Hearne, Emanuele Amorim Alves, Marie Claire Van Hout, Jean-Paul C Grund
Emerging trends in market dynamics and the use of new psychoactive substances are both a public health concern and a complex regulatory issue. One novel area of investigation is the availability of homemade opioids, amphetamines and dissociatives, and the potential fueling of interest in clandestine home manufacture of drugs via the Internet. We illustrate here how online communal folk pharmacology of homemade drugs on drug website forums may actually inform home manufacture practices or contribute to the reduction of harms associated with this practice...
May 23, 2017: Journal of Psychoactive Drugs
https://www.readbyqxmd.com/read/28533693/dna-methylation-at-the-mu-1-opioid-receptor-gene-oprm1-promoter-predicts-preoperative-acute-and-chronic-postsurgical-pain-after-spine-fusion
#8
Vidya Chidambaran, Xue Zhang, Lisa J Martin, Lili Ding, Matthew T Weirauch, Kristie Geisler, Bobbie L Stubbeman, Senthilkumar Sadhasivam, Hong Ji
INTRODUCTION: The perioperative pain experience shows great interindividual variability and is difficult to predict. The mu-1 opioid receptor gene (OPRM1) is known to play an important role in opioid-pain pathways. Since deoxyribonucleic acid (DNA) methylation is a potent repressor of gene expression, DNA methylation was evaluated at the OPRM1 promoter, as a predictor of preoperative, acute, and chronic postsurgical pain (CPSP). METHODS: A prospective observational cohort study was conducted in 133 adolescents with idiopathic scoliosis undergoing spine fusion under standard protocols...
2017: Pharmacogenomics and Personalized Medicine
https://www.readbyqxmd.com/read/28529168/opioids-in-gastroenterology-treating-adverse-effects-and-creating-therapeutic-benefits
#9
Michael Camilleri, Anthony Lembo, David A Katzka
The use of opioid medications on both an acute and chronic basis is ubiquitous in the U.S. As opioid receptors densely populate the gastrointestinal tract, symptoms and side effects can be expected in these patients. In the esophagus, dysmotility may result manifesting with dysphagia and a syndrome indistinguishable from primary achalasia. In the stomach, a marked delay in gastric emptying may ensue with postprandial nausea and early satiety. Postoperatively, particularly with abdominal surgery, opioid induced ileus may ensue...
May 18, 2017: Clinical Gastroenterology and Hepatology
https://www.readbyqxmd.com/read/28526152/pharmacologic-properties-of-novel-local-anesthetic-agents-in-anesthesia-practice
#10
REVIEW
Chih H King, Sascha S Beutler, Alan D Kaye, Richard D Urman
Therapeutic duration of traditional local anesthetics when used in peripheral nerve blocks is normally limited. This article describes novel approaches to extend the duration of peripheral nerve blocks currently available or in development. Three newer approaches on extending the duration of peripheral nerve blocks include site-1 sodium channel blockers, novel local anesthetics delivery systems, and novel adjuvants of local anesthetics. Compared with plain amide-based and ester-based local anesthetics, alternative approaches show significant promise in decreasing postoperative pain, rescue opioid requirement, hospital length-of-stay, and overall health care cost, without compromising the established safety profile of traditional local anesthetics...
June 2017: Anesthesiology Clinics
https://www.readbyqxmd.com/read/28525409/preserved-analgesia-with-reduction-in-opioids-through-the-use-of-an-acute-pain-protocol-in-enhanced-recovery-after-surgery-for-open-hepatectomy
#11
Michael C Grant, Philip M Sommer, Cathy He, Sylvia Li, Andrew J Page, Alexander B Stone, Deborah Hobson, Elizabeth Wick, Christopher L Wu
BACKGROUND: Enhanced recovery after surgery (ERAS) pathways are designed to restore baseline physiology, mitigate surgical stressors, and hasten recovery. Paramount to this approach is optimal pain control through multimodal analgesia and limiting reliance on opioid-based medications. Recent studies have fostered growing controversy surrounding the use of epidural analgesia in the ERAS setting, especially for higher-risk procedures. We examine the analgesic end points associated with the use of epidural within the ERAS framework for open hepatectomy...
May 18, 2017: Regional Anesthesia and Pain Medicine
https://www.readbyqxmd.com/read/28522254/novel-delta-opioid-receptor-agonists-with-oxazatricyclodecane-structure-showing-potent-agonistic-activities
#12
Kohei Hayashida, Shigeto Hirayama, Takashi Iwai, Yoshikazu Watanabe, Toshihiro Takahashi, Junichi Sakai, Eriko Nakata, Tomio Yamakawa, Hideaki Fujii, Hiroshi Nagase
We recently reported oxazatricyclodecane derivatives 1 as δ opioid receptor (DOR) agonists having a novel chemotype, but their DOR agonistic activities were relatively low. Based on the working hypothesis that the dioxamethylene moiety in 1 may be an accessory site and that it may interfere with the sufficient conformational change of the receptor required for exerting the full agonistic responses, we designed and synthesized new oxazatricyclodecane derivatives 2-4 lacking the dioxamethylene moiety. As we expected, the designed compounds 2-4 showed pronouncedly improved agonistic activities for the DOR...
April 19, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28521010/prospective-audit-of-a-pathway-for-in-patient-pain-management-of-chronic-abdominal-pain-a-novel-and-cost-effective-strategy
#13
Gopinath Niraj, Sanjay Chaudhri
Background.:  Unexplained abdominal pain is a common cause of hospital admission and utilizes significant resource. Current in-patient pain management of acute exacerbation of chronic abdominal pain is primarily directed at pharmacological and psychological management strategies in this group of complex patients. We adopted a novel approach that proved to be both clinically effective and cost-effective. Design.:  Adult patients admitted to a surgical ward with acute exacerbation of chronic abdominal pain referred to in-patient pain management were prospectively audited over a two-year period at a single tertiary centre...
May 17, 2017: Pain Medicine: the Official Journal of the American Academy of Pain Medicine
https://www.readbyqxmd.com/read/28510066/the-delta-opioid-receptor-in-pain-control
#14
Khaled Abdallah, Louis Gendron
Nowadays, the delta opioid receptor (DOPr) represents a promising target for the treatment of chronic pain and emotional disorders. Despite the fact that they produce limited antinociceptive effects in healthy animals and in most acute pain models, DOPr agonists have shown efficacy in various chronic pain models. In this chapter, we review the progresses that have been made over the last decades in understanding the role played by DOPr in the control of pain. More specifically, the distribution of DOPr within the central nervous system and along pain pathways is presented...
May 17, 2017: Handbook of Experimental Pharmacology
https://www.readbyqxmd.com/read/28509855/the-hypnotic-anxiolytic-and-antinociceptive-profile-of-a-novel-%C3%A2%C2%B5-opioid-agonist
#15
Guilherme Carneiro Montes, Bianca Nascimento Monteiro da Silva, Bismarck Rezende, Roberto Takashi Sudo, Vitor Francisco Ferreira, Fernando de Carvalho da Silva, Angelo da Cunha Pinto, Bárbara Vasconcellos da Silva, Gisele Zapata-Sudo
5'-4-Alkyl/aryl-1H-1,2,3-triazole derivatives PILAB 1-12 were synthesized and a pharmacological screening of these derivatives was performed to identify a possible effect on the Central Nervous System (CNS) and to explore the associated mechanisms of action. The mice received a peritoneal injection (100 µmol/kg) of each of the 12 PILAB derivatives 10 min prior to the injection of pentobarbital and the mean hypnosis times were recorded. The mean hypnosis time increased for the mice treated with PILAB 8, which was prevented when mice were administered CTOP, a µ-opioid antagonist...
May 16, 2017: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/28502978/the-opioid-receptor-triple-agonist-dpi-125-produces-analgesia-with-less-respiratory-depression-and-reduced-abuse-liability
#16
Shou-Pu Yi, Qing-Hong Kong, Yu-Lei Li, Chen-Ling Pan, Jie Yu, Ben-Qiang Cui, Ying-Fei Wang, Guan-Lin Wang, Pei-Lan Zhou, Li-Li Wang, Ze-Hui Gong, Rui-Bin Su, Yue-Hai Shen, Gang Yu, Kwen-Jen Chang
Opioid analgesics remain the first choice for the treatment of moderate to severe pain, but they are also notorious for their respiratory depression and addictive effects. This study focused on the pharmacology of a novel opioid receptor mixed agonist DPI-125 and attempted to elucidate the relationship between the δ-, μ- and κ-receptor potency ratio and respiratory depression and abuse liability. Five diarylmethylpiperazine compounds (DPI-125, DPI-3290, DPI-130, KUST202 and KUST13T02) were selected for this study...
May 15, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28502631/a-brain-targeted-ampakine-compound-protects-against-opioid-induced-respiratory-depression
#17
Wei Dai, Dian Xiao, Xiang Gao, Xin-Bo Zhou, Tong-Yu Fang, Zheng Yong, Rui-Bin Su
The use of opioid drugs for pain relief can induce life-threatening respiratory depression. Although naloxone effectively counteracts opioid-induced respiratory depression, it diminishes the efficacy of analgesia. Our studies indicate that ampakines, in particular, a brain-targeted compound XD-8-17C, are able to reverse respiratory depression without affecting analgesia at relatively low doses. Mice and rats were subcutaneously or intravenously injected with the opioid agonist TH-030418 to induce moderate or severe respiratory depression...
May 11, 2017: European Journal of Pharmacology
https://www.readbyqxmd.com/read/28492816/enhanced-recovery-after-surgery-program-implementation-in-2-surgical-populations-in-an-integrated-health-care-delivery-system
#18
Vincent X Liu, Efren Rosas, Judith Hwang, Eric Cain, Anne Foss-Durant, Molly Clopp, Mengfei Huang, Derrick C Lee, Alex Mustille, Patricia Kipnis, Stephen Parodi
Importance: Novel approaches to perioperative surgical care focus on optimizing nutrition, mobility, and pain management to minimize adverse events after surgical procedures. Objective: To evaluate the outcomes of an enhanced recovery after surgery (ERAS) program among 2 target populations: patients undergoing elective colorectal resection and patients undergoing emergency hip fracture repair. Design, Setting, and Participants: A pre-post difference-in-differences study before and after ERAS implementation in the target populations compared with contemporaneous surgical comparator groups (patients undergoing elective gastrointestinal surgery and emergency orthopedic surgery)...
May 10, 2017: JAMA Surgery
https://www.readbyqxmd.com/read/28490127/milk-bioactive-peptide-database-a-comprehensive-database-of-milk-protein-derived-bioactive-peptides-and-novel-visualization
#19
Søren Drud Nielsen, Robert L Beverly, Yunyao Qu, David C Dallas
During processing and digestion, milk proteins are disassembled into peptides with an array of biological functions, including antimicrobial, angiotensin-converting enzyme inhibition, antioxidant, opioid, and immunomodulation. These functions are summarized in numerous reviews, yet information on which peptides have which functions remains scattered across hundreds of research articles. We systematically searched the literature for all instances of bioactive peptides derived from milk proteins from any mammalian source...
October 1, 2017: Food Chemistry
https://www.readbyqxmd.com/read/28485408/genetic-and-pharmacological-antagonism-of-nk1-receptor-prevents-opiate-abuse-potential
#20
A J Sandweiss, M I McIntosh, A Moutal, R Davidson-Knapp, J Hu, A K Giri, T Yamamoto, V J Hruby, R Khanna, T M Largent-Milnes, T W Vanderah
Development of an efficacious, non-addicting analgesic has been challenging. Discovery of novel mechanisms underlying addiction may present a solution. Here we target the neurokinin system, which is involved in both pain and addiction. Morphine exerts its rewarding actions, at least in part, by inhibiting GABAergic input onto substance P (SP) neurons in the ventral tegmental area (VTA), subsequently increasing SP release onto dopaminergic neurons. Genome editing of the neurokinin 1 receptor (NK1R) in the VTA renders morphine non-rewarding...
May 9, 2017: Molecular Psychiatry
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