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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
#1
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
#2
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
#3
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
#4
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
#5
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
#6
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
#7
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...
September 20, 2017: Cellular Physiology and Biochemistry
https://www.readbyqxmd.com/read/28910112/modular-approach-to-pseudo-neoclerodanes-as-designer-%C3%AE%C2%BA-opioid-ligands
#8
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
#9
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
#10
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
https://www.readbyqxmd.com/read/28838808/characterization-of-structurally-novel-g-protein-biased-cb1-agonists-implications-for-drug-development
#11
Benjamin M Ford, Lirit N Franks, Sherrica Tai, William E Fantegrossi, Edward L Stahl, Michael D Berquist, Christian V Cabanlong, Catheryn D Wilson, Narsimha R Penthala, Peter A Crooks, Paul L Prather
The human cannabinoid subtype 1 receptor (hCB1R) is highly expressed in the CNS and serves as a therapeutic target for endogenous ligands as well as plant-derived and synthetic cannabinoids. Unfortunately, acute use of hCB1R agonists produces unwanted psychotropic effects and chronic administration results in development of tolerance and dependence, limiting the potential clinical use of these ligands. Studies in β-arrestin knockout mice suggest that interaction of certain GPCRs, including μ-, δ-, κ-opioid and hCB1Rs, with β-arrestins might be responsible for several adverse effects produced by agonists acting at these receptors...
August 23, 2017: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
https://www.readbyqxmd.com/read/28836839/antinociceptive-efficacy-of-intramuscular-administration-of-morphine-sulfate-and-butorphanol-tartrate-in-tegus-salvator-merianae
#12
William P Leal, Adriano B Carregaro, Thais F Bressan, Shayne P Bisetto, Cristiano F Melo, Kurt K Sladky
OBJECTIVE To evaluate the antinociceptive efficacy of IM morphine sulfate or butorphanol tartrate administration in tegus (Salvator merianae). ANIMALS 6 healthy juvenile (12- to 24-month-old) tegus (mean ± SD body weight, 1,484 ± 473 g). PROCEDURES In a crossover study design, tegus were randomly assigned to treatment order, with a minimum washout period of 15 days between treatments. Each of 5 treatments was administered IM in a forelimb: saline (0.9% NaCl) solution (0.5 mL), morphine sulfate (5 or 10 mg/kg), or butorphanol tartrate (5 or 10 mg/kg)...
September 2017: American Journal of Veterinary Research
https://www.readbyqxmd.com/read/28825813/highly-potent-and-selective-new-diphenethylamines-interacting-with-the-%C3%AE%C2%BA-opioid-receptor-synthesis-pharmacology-and-structure-activity-relationships
#13
Filippo Erli, Elena Guerrieri, Tanila Ben Haddou, Aquilino Lantero, Michael Mairegger, Helmut Schmidhammer, Mariana Spetea
We previously reported on a series of small molecules targeting the κ-opioid (KOP) receptor featuring a diphenethylamine scaffold and showed the promise of these ligands as effective analgesics with reduced liability for adverse effects. This study expands the structure-activity relationships on our original series by presenting several modifications in the lead compounds 1 (HS665) and 2 (HS666). A library of new diphenethylamines was designed, synthesized, and pharmacologically evaluated. In comparison with 1 and 2, the KOP receptor affinity, selectivity, and agonist activity were modulated by introducing bulkier N-substituents, a 2-fluoro substitution, and additional hydroxyl groups at positions 3' and 4'...
September 14, 2017: Journal of Medicinal Chemistry
https://www.readbyqxmd.com/read/28821282/down-regulation-of-the-tumour-suppressor-%C3%AE%C2%BA-opioid-receptor-predicts-poor-prognosis-in-hepatocellular-carcinoma-patients
#14
Dongtai Chen, Yonghua Chen, Yan Yan, Jiahao Pan, Wei Xing, Qiang Li, Weian Zeng
BACKGROUND: Opioid receptors have become increasingly implicated in cancer progression and long-term patient outcomes. However, the expression and significance of the κ-opioid receptor (KOR) in hepatocellular carcinoma (HCC) remain unclear. METHODS: In this study, KOR mRNA expression was analysed by real-time quantitative PCR in 64 pairs of HCC tumour tissues and adjacent non-tumour tissues, and KOR protein expression was analysed by immunohistochemistry in 174 HCC patients...
August 18, 2017: BMC Cancer
https://www.readbyqxmd.com/read/28819234/transcriptome-of-neonatal-preb%C3%A3-tzinger-complex-neurones-in-dbx1-reporter-mice
#15
John A Hayes, Andrew Kottick, Maria Cristina D Picardo, Andrew D Halleran, Ronald D Smith, Gregory D Smith, Margaret S Saha, Christopher A Del Negro
We sequenced the transcriptome of brainstem interneurons in the specialized respiratory rhythmogenic site dubbed preBötzinger Complex (preBötC) from newborn mice. To distinguish molecular characteristics of the core oscillator we compared preBötC neurons derived from Dbx1-expressing progenitors that are respiratory rhythmogenic to neighbouring non-Dbx1-derived neurons, which support other respiratory and non-respiratory functions. Results in three categories are particularly salient. First, Dbx1 preBötC neurons express κ-opioid receptors in addition to μ-opioid receptors that heretofore have been associated with opiate respiratory depression, which may have clinical applications...
August 17, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28762747/enantioselective-direct-synthesis-of-free-cyclic-amines-via-intramolecular-reductive-amination
#16
Ying Zhang, Qiaozhi Yan, Guofu Zi, Guohua Hou
Chiral cyclic amines can be prepared via intramolecular reductive amination of N-Boc-protected amino ketones in a one-pot process. With the complex of iridium and f-spiroPhos as the catalyst, a range of N-Boc-protected amino ketones are smoothly transformed into chiral cyclic free amines in high yields and excellent enantioselectivities (up to 97% ee). Moreover, this method can also be successfully applied to the synthesis of a κ-opioid receptor selective antagonist, (S)-1.
August 1, 2017: Organic Letters
https://www.readbyqxmd.com/read/28758123/peripheral-antinociception-induced-by-aripiprazole-is-mediated-by-the-opioid-system
#17
Renata Cristina Mendes Ferreira, Ana Flávia Almeida-Santos, Igor Dimitri Gama Duarte, Daniele C Aguiar, Fabricio A Moreira, Thiago Roberto Lima Romero
BACKGROUND: Aripiprazole is an antipsychotic drug used to treat schizophrenia and related disorders. Our previous study showed that this compound also induces antinociceptive effects. The present study aimed to assess the participation of the opioid system in this effect. METHODS: Male Swiss mice were submitted to paw pressure test and hyperalgesia was induced by intraplantar injection of prostaglandin E2 (PGE2, 2 μg). Aripiprazole was injected 10 min before the measurement...
2017: BioMed Research International
https://www.readbyqxmd.com/read/28745076/effects-of-ici204-448-naloxone-methiodide-and-levocetirizine-on-the-scratching-behavior-induced-by-a-%C3%AE%C2%BA-opioid-antagonist-nor-bni-in-icr-mice
#18
Tasuku Nakasone, Hirokazu Wakuda, Yumi Sugimoto, Chiaki Kamei
OBJECTIVE: In this study, we aimed to study the effects of ICI204,448, naloxone methiodide and levocetirizine on the scratching behavior induced by intradermal injection of a ?-opioid antagonist, nor-binaltorphimine (nor-BNI), into the rostral back of ICR mice were investigated. MATERIALS AND METHODS: Male ICR mice weighing 30?35 g were used. The number of scratching episodes were counted for 60 min after i.d. injection of nor-BNI. RESULTS: nor-BNI dose dependently increased in the number of scratching episodes in ICR mice...
July 26, 2017: Immunopharmacology and Immunotoxicology
https://www.readbyqxmd.com/read/28740609/simple-tetrahydroisoquinolines-are-potent-and-selective-kappa-opioid-receptor-antagonists
#19
Chad M Kormos, Pauline W Ondachi, Scott P Runyon, James B Thomas, S Wayne Mascarella, Ann M Decker, Hernán A Navarro, F Ivy Carroll
Potent and selective κ opioid receptor antagonists have been derived from the N-substituted trans-3,4-dimethyl-4-(3-hydroxyphenyl)piperidine class of pure opioid receptor antagonists. In order to determine if the 3-hydroxyphenyl and/or the piperidine amino groups are required for obtaining the pure opioid antagonists, (3R)-7-hydroxy-N-[(1S)-2-methyl-1-(piperidine-1-ylmethyl)propyl]-1,2,3,4-tetrahydroiosquinoline-3-carboxamide (1), which does not have a 4-(3-hydroxyphenyl) group, and (3R)-N-(1R)-1-(cyclohexylmethyl)-2-methylpropyl]-7-hydroxy-1,2,3,4-tetrahydroisoquinoline-3-carboxamide (2), which does not have a 4-hydroxylphenyl or a piperidine amino group, were synthesized and evaluated for their [(35)S]GTPγS binding properties at the μ, δ, and κ opioid receptors...
July 13, 2017: ACS Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28739044/essential-structure-of-orexin-1-receptor-antagonist-ynt-707-part-i-role-of-the-4-5-epoxy-ring-for-binding-with-orexin-1-receptor
#20
Naoshi Yamamoto, Sayaka Ohrui, Takahiro Okada, Masahiro Yata, Tsuyoshi Saitoh, Noriki Kutsumura, Yasuyuki Nagumo, Yoko Irukayama-Tomobe, Yasuhiro Ogawa, Yukiko Ishikawa, Yurie Watanabe, Daichi Hayakawa, Hiroaki Gouda, Masashi Yanagisawa, Hiroshi Nagase
The essential structure of the orexin 1 receptor (OX1R) antagonist YNT-707 (2) was clarified, particularly the roles to OX1R antagonist activities of the 3-OMe, the 4,5-epoxy ring, the 14-hydroxy group, and the orientation of the 6-amide side chain. The 3-OMe and 17-sulfonamide group were shown to be essential for the OX1R antagonistic activity. The 4,5-epoxy ring plays an important role for the active orientation of the 6-amide group. The 14-hydroxy group could lower the activity of the 6β-amide isomer by the interaction of the 14-hydroxy group with the 6-amide group, which could orient the 6-amide group toward the upper side of the C-ring...
September 1, 2017: Bioorganic & Medicinal Chemistry Letters
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