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https://www.readbyqxmd.com/read/29233847/pharmacological-evidence-for-a-putative-conserved-allosteric-site-on-opioid-receptors
#1
Kathryn E Livingston, M Alexander Stanczyk, Neil Burford, Andrew Alt, Merixtell Canals, John R Traynor
Allosteric modulators of G protein-coupled receptors (GPCRs), including opioid receptors, have been proposed as possible therapeutic agents with enhanced selectivity. BMS-986122 is a positive allosteric modulator (PAM) of the mu-opioid receptor (μ-OR). BMS-986187 is a structurally distinct PAM for the delta-opioid receptor (δ-OR) that has been reported to show 100-fold selectivity in promoting δ-OR over μ-OR agonism. Here we use ligand binding and second messenger assays to show that BMS-986187 is actually an effective PAM at μ-OR and at the kappa opioid receptor (κ-OR), but is ineffective at the nociceptin receptor (NOPR)...
December 12, 2017: Molecular Pharmacology
https://www.readbyqxmd.com/read/29202454/fentanyl-related-designer-drugs-w-18-and-w-15-lack-appreciable-opioid-activity-in-vitro-and-in-vivo
#2
Xi-Ping Huang, Tao Che, Thomas J Mangano, Valerie Le Rouzic, Ying-Xian Pan, Michael D Cameron, Michael H Baumann, Gavril W Pasternak, Bryan L Roth
W-18 (4-chloro-N-[1-[2-(4-nitrophenyl)ethyl]-2-piperidinylidene]-benzenesulfonamide) and W-15 (4-chloro-N-[1-(2-phenylethyl)-2-piperidinylidene]-benzenesulfonamide) represent two emerging drugs of abuse chemically related to the potent opioid agonist fentanyl (N-(1-(2-phenylethyl)-4-piperidinyl)-N-phenylpropanamide). Here, we describe the comprehensive pharmacological profiles of W-18 and W-15, as examination of their structural features predicted that they might lack opioid activity. We found W-18 and W-15 to be without detectible activity at μ, δ, κ, and nociception opioid receptors in a variety of assays...
November 16, 2017: JCI Insight
https://www.readbyqxmd.com/read/29193080/neuroprotection-mediated-post-ischemically-by-a-non-peptidic-%C3%AE-opioid-receptor-agonist-tan-67-in-ischemic-stroke-mice-is-associated-with-altered-amyloid-precursor-protein-expression-maturation-and-processing
#3
Jia-Wei Min, Yanying Liu, David Wang, Fangfang Qiao, Hongmin Wang
Tan-67 is a selective non-peptidic δ-opioid receptor (DOR) agonist that confers neuroprotection against cerebral ischemia/reperfusion (I/R)-caused neuronal injury in pre-treated animals. In this study, we examined whether post-ischemic administration of Tan-67 in stroke mice is also neuroprotective and whether the treatment affects expression, maturation and processing of the amyloid precursor protein (APP). A focal cerebral I/R model in mice was induced by middle cerebral artery occlusion for 1 hour (h) and Tan-67 (1...
November 29, 2017: Journal of Neurochemistry
https://www.readbyqxmd.com/read/29191644/preclinical-assessment-of-utility-of-m6s-for-multimodal-acute-and-chronic-pain-treatment-in-diabetic-neuropathy
#4
Jai Shankar K Yadlapalli, Navdeep Dogra, Anqi W Walbaum, Paul L Prather, Peter A Crooks, Maxim Dobretsov
AIMS: Previous reports from our laboratory have established that morphine-6-O-sulfate (M6S) is a mixed μ/δ opioid receptor (OR) agonist and a potential improved alternative to morphine for treatment of chronic multimodal pain in non-diabetic rats. This study extends the antinociceptive effects of M6S and morphine in STZ-induced diabetic rats. MATERIALS AND METHODS: Effects of morphine and M6S were studied across a range of pain modalities, using hot plate threshold (HPT), pinprick sensitivity threshold (PST) and paw pressure threshold (PPT) tests...
November 27, 2017: Life Sciences
https://www.readbyqxmd.com/read/29174974/m-trifluoromethyl-diphenyl-diselenide-promotes-resilience-to-social-avoidance-induced-by-social-defeat-stress-in-mice-contribution-of-opioid-receptors-and-mapks
#5
Suzan Gonçalves Rosa, Ana Paula Pesarico, Cristina Wayne Nogueira
Depressive symptoms precipitated by stress are prevalent in population. In experimental models of social stress, endogenous opioids mediate different aspects of defensive and submissive behaviors. The present study investigated the opioid receptors, mitogen-activated protein kinase (MAPKs) and protein kinase B (Akt) contribution to m-trifluoromethyl-diphenyl diselenide [(m-CF3-PhSe)2] effects on social avoidance induced by social defeat stress (SDS). Adult Swiss mice were subjected to SDS and treated with (m-CF3-PhSe)2 (5 to 25mg/kg) for 7days...
November 23, 2017: Progress in Neuro-psychopharmacology & Biological Psychiatry
https://www.readbyqxmd.com/read/29152051/%C3%AF-space-screening-of-dermorphin-based-tetrapeptides-through-use-of-constrained-arylazepinone-and-quinolinone-scaffolds
#6
Olivier Van der Poorten, Robin Van Den Hauwe, Emilie Eiselt, Cecilia Betti, Karel Guillemyn, Nga N Chung, François Hallé, Frédéric Bihel, Peter W Schiller, Dirk Tourwé, Philippe Sarret, Louis Gendron, Steven Ballet
Herein, the synthesis of novel conformationally constrained amino acids, 4-amino-8-bromo-2-benzazepin-3-one (8-Br-Aba), 3-amino-3,4-dihydroquinolin-2-one, and regioisomeric 4-amino-naphthoazepinones (1- and 2-Ana), is described. Introduction of these constricted scaffolds into the N-terminal tetrapeptide of dermorphin (i.e., H-Tyr-d-Ala-Phe-Gly-NH2) induced significant shifts in binding affinity, selectivity, and in vitro activity at the μ- and δ-opioid receptors (MOP and DOP, respectively). A reported constrained μ-/δ-opioid lead tetrapeptide H-Dmt-d-Arg-Aba-Gly-NH2 was modified through application of various constrained building blocks to identify optimal spatial orientations in view of activity at the opioid receptors...
November 9, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29131554/the-pathophysiology-incidence-impact-and-treatment-of-opioid-induced-nausea-and-vomiting
#7
Theresa Mallick-Searle, Mechele Fillman
PURPOSE: Opioid medications are integral in managing acute moderate-to-severe pain. Opioid analgesics bind to μ (mu), κ (kappa), or δ (delta) opioid receptors in the brain, spinal cord, and digestive tract. However, opioids cause adverse effects that may interfere with their therapeutic use. Some adverse effects wane over time, but patients using opioids for acute pain struggle with opioid-induced nausea and vomiting (OINV) the entire time they take the opioid. This article discusses the underlying mechanisms, clinical implications, and treatment strategies of OINV...
November 2017: Journal of the American Association of Nurse Practitioners
https://www.readbyqxmd.com/read/29121571/high-throughput-%C3%AE-spe-based-elution-coupled-with-uplc-ms-ms-for-determination-of-eluxadoline-in-plasma-sample-application-in-pharmacokinetic-characterization-of-plga-nanoparticle-formulations-in-rats
#8
Muzaffar Iqbal, Essam Ezzeldin, Khalid A Al-Rashood, Ramadan Al-Shdefat, Md Khalid Anwer
Eluxadoline is a novel μ- and κ-opioid receptor (OR) agonist and δ-OR antagonist, recently approved as a first line therapy for the treatment of irritable bowel syndrome. Due to abuse potential, poor bioavailability and high intersubject variability, a sensitive and reliable assay is prerequisite for its determination in biological samples. This work first time report the development and validation of UPLC-MS/MS assay for determination of eluxadoline in rat plasma sample using risperidone as an internal standard (IS)...
October 28, 2017: Journal of Pharmaceutical and Biomedical Analysis
https://www.readbyqxmd.com/read/29097308/analysis-of-natural-product-regulation-of-opioid-receptors-in-the-treatment-of-human-disease
#9
REVIEW
S Badal, S Turfus, R Rajnarayanan, C Wilson-Clarke, S L Sandiford
Opioid receptors (ORs), μOR, δOR, κOR and ORL1 mediate numerous signaling cascades, most importantly, through the modulation of ion channels. Research demonstrates the role of OR mediated signal transduction in treating pain, cancer, neurodegenerative disorders and cardiac insults. Yet, the primary application of drugs that modulate ORs is analgesia. Current opioids like morphine that are mainly μOR orthosteric agonists attract many undesirable side-effects (constipation, urinary retention, respiratory depression and hypotension) and the existing modus operandi against these is the inclusion of a μOR antagonist (for example...
October 30, 2017: Pharmacology & Therapeutics
https://www.readbyqxmd.com/read/29097258/site-specific-o-glycosylation-of-n-terminal-serine-residues-by-polypeptide-galnac-transferase-2-modulates-human-%C3%AE-opioid-receptor-turnover-at-the-plasma-membrane
#10
Jarkko J Lackman, Christoffer K Goth, Adnan Halim, Sergey Y Vakhrushev, Henrik Clausen, Ulla E Petäjä-Repo
G protein-coupled receptors (GPCRs) are an important protein family of signalling receptors that govern a wide variety of physiological functions. The capacity to transmit extracellular signals and the extent of cellular response are largely determined by the amount of functional receptors at the cell surface that is subject to complex and fine-tuned regulation. Here, we demonstrate that the cell surface expression level of an inhibitory GPCR, the human δ-opioid receptor (hδOR) involved in pain and mood regulation, is modulated by site-specific N-acetylgalactosamine (GalNAc) -type O-glycosylation...
October 31, 2017: Cellular Signalling
https://www.readbyqxmd.com/read/29090081/eluxadoline-in-irritable-bowel-syndrome-with-diarrhea-rationale-evidence-and-place-in-therapy
#11
REVIEW
Kenneth Barshop, Kyle Staller
Irritable bowel syndrome (IBS) is the most common gastrointestinal (GI) disorder worldwide, however treatment options for diarrhea-predominant IBS (IBS-D) remain limited. Eluxadoline, a µ- and κ-opioid receptor agonist and δ-opioid receptor antagonist, was recently approved for the treatment of IBS-D. A novel compound first described in 2008, eluxadoline was shown to normalize GI transit, with a subsequent phase I demonstrating its safety and tolerability in healthy adults. In 2016, two randomized, double-blind, placebo-controlled phase III trials studying eluxadoline use at 75 mg and 100 mg twice daily over 26 weeks demonstrated a significant improvement in stool consistency and many global symptoms of IBS...
November 2017: Therapeutic Advances in Chronic Disease
https://www.readbyqxmd.com/read/29054455/dadle-enhances-viability-and-anti-inflammatory-effect-of-human-mscs-subjected-to-serum-free-apoptotic-condition-in-part-via-the-dor-pi3k-akt-pathway
#12
L Vinod Kumar Reddy, Dwaipayan Sen
AIM: Nutritional deprivation and inflammation-rich zones are the major causative reasons for poor survivability of transplanted mesenchymal stem cells (MSCs). Therefore in the present study, we demonstrated the cytoprotective and anti-inflammatory effects of activated delta (δ)-opioid receptor (DOR) with synthetic peptide [D-Ala(2), D-Leu(5)]-enkephalin (DADLE) treatment on human MSCs cultured in serum-starved condition. MAIN METHODS: Cell viability was measured using MTT and Annexin V/PI assays...
October 19, 2017: Life Sciences
https://www.readbyqxmd.com/read/29053731/determination-of-%C3%AE-%C3%AE-and-%C3%AE%C2%BA-opioid-receptors-in-forebrain-cortex-of-rats-exposed-to-morphine-for-10-days-comparison-with-animals-after-20-days-of-morphine-withdrawal
#13
COMPARATIVE STUDY
Hana Ujcikova, Martina Hlouskova, Kristina Cechova, Katerina Stolarova, Lenka Roubalova, Petr Svoboda
BACKGROUND: Chronic exposure of mammalian organism to morphine results in adaption to persistent high opioid tone through homeostatic adjustments. Our previous results indicated that in the frontal brain cortex (FBC) of rats exposed to morphine for 10 days, such a compensatory adjustment was detected as large up-regulation of adenylylcyclases I (8-fold) and II (2.5-fold). The other isoforms of AC (III-IX) were unchanged. Importantly, the increase of ACI and ACII was reversible as it disappeared after 20 days of morphine withdrawal...
2017: PloS One
https://www.readbyqxmd.com/read/29047460/computational-insights-into-the-subtype-selectivity-and-message-address-efficacy-mechanisms-of-opioid-receptors-through-jdtic-binding-and-unbinding
#14
Jian-Xin Cheng, Tao Cheng, Wei-Hua Li, Gui-Xia Liu, Wei-Liang Zhu, Yun Tang
In drug design and discovery, binding affinity and selectivity are two basic properties of a drug candidate. Opioid receptors (ORs) are the main targets of strong analgesics. Like some other class A members of G-protein-coupled receptors (GPCRs), ORs exhibit complex selectivity on their ligands. The diversity of binding activity and selectivity among opioids has deeply attracted researchers for a long time. To investigate the subtype selectivity of μ, δ and κ ORs in detail, using the κ-selective antagonist JDTic as a probe, we performed a series of computational simulations, including molecular dynamics and metadynamics, on JDTic-μ/δ/κ-OR complexes...
October 19, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/29044958/a-simple-validated-multi-method-for-detecting-drugs-in-oral-fluid-by-ultra-performance-liquid-chromatography-tandem-mass-spectrometry-uplc-ms-ms
#15
Yufang Zheng, Erik Sparve, Mats Bergström
BACKGROUND: Oral fluid sampling offers several advantages compared to other methods of detecting drugs in biological matrices due to its easy sampling procedure and simple supervision. Hence, the use of oral fluid for drug testing is increasing in workplaces and in roadside testing. As a result, more laboratories are required to perform analyses of drugs in oral fluid. METHODS: A multi-method using Ultra Performance Liquid Chromatography-Tandem Mass Spectrometry (UPLC-MS/MS) for tracing drugs in oral fluid was developed...
October 16, 2017: Drug Testing and Analysis
https://www.readbyqxmd.com/read/28966276/c-homomorphinan-derivatives-as-lead-compounds-to-obtain-safer-and-more-clinically-useful-analgesics
#16
Kyoko Ishikawa, Fumika Karaki, Kaoru Tayama, Eika Higashi, Shigeto Hirayama, Kennosuke Itoh, Hideaki Fujii
Buprenorphine shows strong analgesic effects on moderate to severe pain. Although buprenorphine can be used more safely than other opioid analgesics, it has room for improvement in clinical utility. Investigation of compounds structurally related to buprenorphine should be an approach to obtain novel analgesics with safer and improved profiles compared to buprenorphine. In the course of our previous studies, we observed that derivatives obtained by cyclizing C-homomorphinans were structurally related to buprenorphine...
2017: Chemical & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/28956418/protective-effects-of-smyrnium-cordifolium-boiss-essential-oil-on-pentylenetetrazol-induced-seizures-in-mice-involvement-of-benzodiazepine-and-opioid-antagonists
#17
N Abbasi, S Mohammadpour, E Karimi, A Aidy, P Karimi, M Azizi, K Asadollahi
Smyrnium cordifolium as a wild plant is used in traditional medicine in Iran for the treatment of anxiety and insomnia. The anticonvulsant effect of this plant has not been studied to date, therefore this study aimed to evaluate the anticonvulsant effects of its essential oil and curzerene on seizure. Essential oil of the Smyrnium cordifolium plant was prepared by the hydro-distillation method. Gas chromatography and gas chromatography-mass spectroscopy analysis of the essential oil revealed its main components...
July 2017: Journal of Biological Regulators and Homeostatic Agents
https://www.readbyqxmd.com/read/28944090/rapid-identification-of-buprenorphine-in-patient-saliva
#18
Stuart Farquharson, Kathryn Dana, Chetan Shende, Zachary Gladding, Jenelle Newcomb, Jessica Dascher, Ismene L Petrakis, Albert J Arias
Buprenorphine is becoming the medication of choice to help patients withdraw from opioid addiction. However, treatment is compromised by the inability of physicians to assess patient usage during scheduled examinations. Here we describe the development of a point-of-care (POC) analyzer that can rapidly measure both illicit and treatment drugs in patient saliva, ideally in the physician's office, and with a degree of accuracy similar to chromatography. The analyzer employs a relatively simple supported liquid extraction to isolate the drugs from the saliva and surface-enhanced Raman spectroscopy (SERS) to detect the drugs...
June 2017: Journal of Analytical & Bioanalytical Techniques
https://www.readbyqxmd.com/read/28877966/t-cell-mediation-of-pregnancy-analgesia-affecting-chronic-pain-in-mice
#19
Sarah F Rosen, Boram Ham, Shannon Drouin, Nadia Boachie, Anne-Julie Chabot-Dore, Jean-Sebastien Austin, Luda Diatchenko, Jeffrey S Mogil
It has been reported consistently that many female chronic pain sufferers have an attenuation of symptoms during pregnancy. Rats display increased pain tolerance during pregnancy due to an increase in opioid receptors in the spinal cord. Past studies did not consider the role of non-neuronal cells, which are now known to play an important role in chronic pain processing. Using an inflammatory (complete Freund's adjuvant) or neuropathic (spared nerve injury) model of persistent pain, we observed that young adult female mice in early pregnancy switch from a microglia-independent to a microglia-dependent pain hypersensitivity mechanism...
October 11, 2017: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/28857657/opioid-system-contribution-to-the-antidepressant-like-action-of-m-trifluoromethyl-diphenyl-diselenide-in-mice-a-compound-devoid-of-tolerance-and-withdrawal-syndrome
#20
Suzan G Rosa, Ana P Pesarico, Carolina F Tagliapietra, Sônia C A da Luz, Cristina W Nogueira
Animal and clinical researches indicate that the opioid system exerts a crucial role in the etiology of mood disorders and is a target for intervention in depression treatment. This study investigated the contribution of the opioid system to the antidepressant-like action of acute or repeated m-trifluoromethyl-diphenyl diselenide administration to Swiss mice. m-Trifluoromethyl-diphenyl diselenide (50 mg/kg, intragastric) produced an antidepressant-like action in the forced swimming test from 30 min to 24 h after treatment...
August 1, 2017: Journal of Psychopharmacology
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