keyword
MENU ▼
Read by QxMD icon Read
search

κ opioid

keyword
https://www.readbyqxmd.com/read/29224002/the-protective-effects-of-%C3%AE-opioid-receptor-stimulation-in-hypoxic-pulmonary-hypertension-involve-inhibition-of-autophagy-through-the-ampk-mtor-pathway
#1
Yaguang Zhou, Yuanbo Wang, Xu Wang, Xin Tian, Shumiao Zhang, Fan Yang, Haitao Guo, Rong Fan, Na Feng, Min Jia, Xiaoming Gu, Yuemin Wang, Juan Li, Jianming Pei
BACKGROUND/AIMS: In a previous study, we showed that κ-opioid receptor stimulation with the selective agonist U50,488H ameliorated hypoxic pulmonary hypertension (HPH). However, the roles that pulmonary arterial smooth muscle cell (PASMC) proliferation, apoptosis, and autophagy play in κ-opioid receptor-mediated protection against HPH are still unknown. The goal of the present study was to investigate the role of autophagy in U50,488H-induced HPH protection and the underlying mechanisms...
December 8, 2017: Cellular Physiology and Biochemistry
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/29174974/m-trifluoromethyl-diphenyl-diselenide-promotes-resilience-to-social-avoidance-induced-by-social-defeat-stress-in-mice-contribution-of-opioid-receptors-and-mapks
#3
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/29131554/the-pathophysiology-incidence-impact-and-treatment-of-opioid-induced-nausea-and-vomiting
#4
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
#5
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/29119401/role-of-endogenous-agonists-of-opioid-receptors-in-the-regulation-of-heart-resistance-to-postischemic-reperfusion-injury
#6
A S Gorbunov, O E Vaizova, M V Belousov, S V Pozdnyakova, E A Nesterov, P G Madonov
Intravenous injection of nonselective antagonists of opioid receptors (OR) naltrexone (5 mg/kg) and naloxone methiodide (5 mg/kg), selective δ1-OR antagonist BNTX (0.7 mg/kg), selective δ2-OR blocker naltriben (0.3 mg/kg), selective κ-OR antagonist norbinaltorphimine (2 mg/kg), and selective blocker of ORL1 opioid receptors JTC-801 (0.1 mg/kg) produced no effect on reperfusion injury to the heart in rats narcotized with α-chloralose. In contrast, selective μ-OR antagonist CTAP (1 mg/kg) limited the infarct size, although this effect was not observed at a lower CTAP concentration of 0...
November 9, 2017: Bulletin of Experimental Biology and Medicine
https://www.readbyqxmd.com/read/29104757/effect-of-nalfurafine-hydrochloride-in-patients-with-chronic-liver-disease-with-refractory-pruritus-on-sleep-disorders-a-study-protocol-for-single-arm-prospective-interventional-study
#7
Kazunori Yoh, Hiroki Nishikawa, Hirayuki Enomoto, Yoshinori Iwata, Akio Ishii, Yukihisa Yuri, Noriko Ishii, Yuho Miyamoto, Kunihiro Hasegawa, Chikage Nakano, Ryo Takata, Takashi Nishimura, Nobuhiro Aizawa, Yoshiyuki Sakai, Naoto Ikeda, Tomoyuki Takashima, Hiroko Iijima, Shuhei Nishiguchi
Introduction: Chronic liver disease (CLD)-related pruritus manifests as cholestasis symptoms, which can cause severe itches in the whole body and significantly decrease quality of daily activities and sleep. The actigram, which documents movement by means of an accelerometer, has been demonstrated to be useful for assessing sleep quality. Nalfurafine hydrochloride, which is a selective κ-opioid receptor agonist, exerts its antipruritic efficacies through a novel mechanism. We aimed to prospectively examine the effect of nalfurafine hydrochloride on sleep quality for patients with CLD with pruritus utilising actigram...
2017: BMJ Open Gastroenterology
https://www.readbyqxmd.com/read/29093296/discovery-of-peripheral-%C3%AE%C2%BA-opioid-receptor-agonists-as-novel-analgesics
#8
Shinya Suzuki, Yuji Sugawara, Hideaki Inada, Riichiro Tsuji, Atsushi Inoue, Ryuji Tanimura, Rieko Shimozono, Mitsuhiro Konno, Tomofumi Ohyama, Eriko Higashi, Chizuka Sakai, Koji Kawai
κ-Opioid receptor agonists with high selectivity over the μ-opioid receptor and peripheral selectivity are attractive targets in the development of drugs for pain. We have previously attempted to create novel analgesics with peripheral selective κ-opioid receptor agonist on the basis of TRK-820. In this study, we elucidated the biological properties of 17-hydroxy-cyclopropylmethyl and 10α-hydroxy derivatives. These compounds were found to have better κ-opioid receptor selectivity and peripheral selectivity than TRK-820...
2017: Chemical & Pharmaceutical Bulletin
https://www.readbyqxmd.com/read/29090081/eluxadoline-in-irritable-bowel-syndrome-with-diarrhea-rationale-evidence-and-place-in-therapy
#9
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/29057665/medications-for-substance-use-disorders-sud-emerging-approaches
#10
Eduardo R Butelman, Mary Jeanne Kreek
Substance use disorders are a group of chronic relapsing disorders of the brain, which have massive public health and societal impact. In some disorders (e.g., heroin/prescription opioid addictions) approved medications have a major long-term benefit. For other substances (e.g., cocaine, amphetamines and cannabis) there are no approved medications, and for alcohol there are approved treatments, which are not in wide usage. Approved treatments for tobacco use disorders are available, and novel medications are also under study...
October 30, 2017: Expert Opinion on Emerging Drugs
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
#11
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/29052613/dynorphin-counteracts-orexin-in-the-paraventricular-nucleus-of-the-thalamus-cellular-and-behavioral-evidence
#12
Alessandra Matzeu, Marsida Kallupi, Olivier George, Paul Schweitzer, Rémi Martin-Fardon
The orexin (Orx) system plays a critical role in drug addiction and reward-related behaviors. The dynorphin (Dyn) system promotes depressive-like behavior and plays a key role in the aversive effects of stress. Orx and Dyn are co-released and have opposing functions in reward and motivation in the ventral tegmental area (VTA). Previous studies suggested that OrxA transmission in the posterior paraventricular nucleus of the thalamus (pPVT) participates in cocaine-seeking behavior. This study determined whether Orx and Dyn interact in the pPVT...
October 20, 2017: Neuropsychopharmacology: Official Publication of the American College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/29051663/%C3%AE%C2%BA-casein-as-a-source-of-short-chain-bioactive-peptides-generated-by-lactobacillus-helveticus
#13
Katarzyna Skrzypczak, Waldemar Gustaw, Dominik Szwajgier, Emilia Fornal, Adam Waśko
This paper explores the ability of Lactobacillus helveticus strains to release sequences of short biologically active peptides (containing 2-10 amino acid residues) from casein. The proteolytic enzymes of the tested strains exhibit different patterns of cleavage of CN fractions. The modification of κ-casein (κ-CN) with pyrrolidone carboxylic acid inhibits the proteolytic activity of strains L. helveticus 141 and the reference strain (DSMZ 20075), while the modification with phosphothreonine inhibits enzymes of all the tested bacteria...
October 2017: Journal of Food Science and Technology
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/28967123/antidepressant-like-effects-of-bu10119-a-novel-buprenorphine-analogue-with-mixed-kappa-mu-opioid-receptor-antagonist-properties-in-mice
#15
Abdulrahman Almatroudi, Mehrnoosh Ostovar, Christopher P Bailey, Stephen M Husbands, Sarah J Bailey
BACKGROUND AND PURPOSE: Κ-opioid receptor antagonists have potential for treating neuropsychiatric disorders. We have investigated the in vivo pharmacology of a novel buprenorphine analogue, BU10119, for the first time. EXPERIMENTAL APPROACH: To determine the opioid pharmacology of BU10119 (0.3-3 mg/kg, i.p.) in vivo, the warm-water tail withdrawal assay was used in adult male CD1 mice. A range of behavioural paradigms was used to investigate the locomotor effects, rewarding properties and antidepressant or anxiolytic potential of BU10119...
October 1, 2017: British Journal of Pharmacology
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/28930716/antinociceptive-effect-of-ghrelin-in-a-rat-model-of-irritable-bowel-syndrome-involves-trpv1-opioid-systems
#17
Yuqing Mao, Zhengyang Li, Kan Chen, Huafang Yu, Shaoren Zhang, Miao Jiang, Yuanhua Ma, Chunli Liang, Hongyan Liu, Huanqing Li, Qian Hua, Hao Zhou, Yonghong Sun, Xiaoming Fan
BACKGROUND/AIMS: Irritable bowel syndrome (IBS), defined as recurrent abdominal pain and changes in bowel habits, seriously affects quality of life and ability to work. Ghrelin is a brain-gut hormone, which has been reported to show antinociceptive effects in peripheral pain. We investigated the effect of ghrelin on visceral hypersensitivity and pain in a rat model of IBS. METHODS: Maternal deprivation (MD) was used to provide a stress-induced model of IBS in Wistar rats...
2017: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/28910112/modular-approach-to-pseudo-neoclerodanes-as-designer-%C3%AE%C2%BA-opioid-ligands
#18
Alexander M Sherwood, Samuel E Williamson, Rachel S Crowley, Logan M Abbott, Victor W Day, Thomas E Prisinzano
Informed by previous semisynthetic work on salvinorin A, a modular total synthesis has been developed capable of producing novel compounds targeting the κ-opioid receptor. The strategy has permitted the deliberate simplification and introduction of functionality about the target molecule to provide access to molecular features on salvinorin A otherwise unattainable by semisynthesis. Using this approach, a potent pseudo-neoclerodane κ-opioid receptor ligand (2) has been realized.
October 6, 2017: Organic Letters
https://www.readbyqxmd.com/read/28888771/c-terminal-hydrazide-modification-changes-the-spinal-antinociceptive-profiles-of-endomorphins-in-mice
#19
Chang-Lin Wang, Dai-Jun Yang, Bi-Yu Yuan, Yu Wang
Previously, we have demonstrated that endomorphins (EMs) analogs with C-terminal hydrazide modification retained the μ-opioid receptor affinity and selectivity, and exhibited potent antinociception after intracerebroventricular (i.c.v.) administration. In the present study, we extended our studies to evaluate the antinociceptive profiles of EMs and their analogs EM-1-NHNH2, EM-2-NHNH2 given spinally in the radiant heat paw withdrawal test. Following intrathecal (i.t.) administration, EM-1, EM-2, EM-1-NHNH2 and EM-2-NHNH2 dose-dependently increased the latency for paw withdrawal response...
September 6, 2017: Peptides
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
keyword
keyword
99914
1
2
Fetch more papers »
Fetching more papers... Fetching...
Read by QxMD. Sign in or create an account to discover new knowledge that matter to you.
Remove bar
Read by QxMD icon Read
×

Search Tips

Use Boolean operators: AND/OR

diabetic AND foot
diabetes OR diabetic

Exclude a word using the 'minus' sign

Virchow -triad

Use Parentheses

water AND (cup OR glass)

Add an asterisk (*) at end of a word to include word stems

Neuro* will search for Neurology, Neuroscientist, Neurological, and so on

Use quotes to search for an exact phrase

"primary prevention of cancer"
(heart or cardiac or cardio*) AND arrest -"American Heart Association"