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https://www.readbyqxmd.com/read/28819234/transcriptome-of-neonatal-preb%C3%A3-tzinger-complex-neurones-in-dbx1-reporter-mice
#1
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
#2
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
#3
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
#4
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
#5
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
#6
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...
July 4, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28738113/estrogen-status-gates-effects-of-kappa-opioid-receptor-on-temporomandibular-joint-responsive-neurons-at-the-spinomedullary-junction-in-female-rats
#7
Akimasa Tashiro, David A Bereiter, Yasuhiro Nishida
AIMS: To determine whether estrogen status alters κ-opioid inhibition of nociceptive processing by affecting temporomandibular joint (TMJ) input to neurons in the trigeminal subnucleus caudalis [Vc]/C1-2 region at the spinomedullary junction in female rats. METHODS: TMJ-responsive neurons were recorded in laminae I-II of the Vc/C1-2 region at the spinomedullary junction of ovariectomized female rats treated for 2 days with low-dose estradiol (LE group; 2 mg/day) or high-dose estradiol (HE group; 20 mg/day)...
July 2017: Journal of Oral & Facial Pain and Headache
https://www.readbyqxmd.com/read/28726190/effect-of-peripheral-%C3%AE-%C3%AE-and-%C3%AE%C2%BA-opioid-ligands-on-the-development-of-tolerance-to-ethanol-induced-analgesia
#8
S K Sudakov, E V Alekseeva, G A Nazarova
We studied the rate of development of tolerance to the ethanol-induced analgesia under the effect of μ-, δ-, and κ-opioid agonists and antagonists not crossing the blood-brain barrier and rapidly inactivated by gastric and duodenal proteolytic enzymes. Activation of gastric κ-opioid receptors eliminated the analgesic effect of ethanol and accelerated the development of tolerance to ethanol-induced analgesia. In contrast, activation of gastric μ-opioid receptors decelerated the development of this tolerance...
June 2017: Bulletin of Experimental Biology and Medicine
https://www.readbyqxmd.com/read/28693156/detection-of-opcml-methylation-a-possible-epigenetic-marker-from-free-serum-circulating-dna-to-improve-the-diagnosis-of-early-stage-ovarian-epithelial-cancer
#9
Bi Wang, Lei Yu, Xin Luo, Lin Huang, Qin-Shan Li, Xiao-Shan Shao, Yi Liu, Yu Fan, Guo-Zhen Yang
The aim of the present study was to identify the appropriate DNA sequence and design high-quality primers for methylation-specific polymerase chain reaction (MSP). These primers may be used to examine and identify patients with early-stage epithelial ovarian carcinoma (EOC). Opioid binding protein/cell adhesion molecule like (OPCML), Runt-related transcription factor 3 and tissue factor pathway inhibitor 2 were selected as possible molecular markers. MSP primer sets were designed to monitor the methylation of the three markers...
July 2017: Oncology Letters
https://www.readbyqxmd.com/read/28688957/discovery-of-highly-selective-%C3%AE%C2%BA-opioid-receptor-agonists-10%C3%AE-hydroxy-trk-820-derivatives
#10
Shinya Suzuki, Yuji Sugawara, Riichiro Tsuji, Ryuji Tanimura, Chihiro Kaneko, Natsumi Yuzawa, Mai Yagi, Koji Kawai
κ-Opioid receptor agonists with high selectivity over the μ-opioid receptor are attractive targets in the development of drugs for pain and pruritus. We previously reported the synthesis of 10α-hydroxy TRK-820 (1). In this study, we elucidated the biological properties of 1 and optimized its 6-acyl unit by modifying our synthetic route. Among the 10α-hydroxy TRK-820 derivatives prepared, 26 showed the most potent κ-opioid agonist activity (EC50=0.00466nM) and excellent selectivity and 22 was the most κ-selective agonist...
June 12, 2017: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/28647729/analgesic-effects-of-diluted-bee-venom-acupuncture-mediated-by-%C3%AE-opioid-and-%C3%AE-2-adrenergic-receptors-in-osteoarthritic-rats
#11
Jeong-Eun Huh, Byung-Kwan Seo, Jung-Woo Lee, Chanyoung Kim, Yeon-Cheol Park, Jae-Dong Lee, Yong-Hyeon Baek
Context • Pain from osteoarthritis is associated with peripheral nociception and central pain processing. Given the unmet need for innovative, effective, and well-tolerated therapies, many patients, after looking for more satisfactory alternatives, decide to use complementary and alternative modalities. The analgesic mechanism of subcutaneous injections of diluted bee venom into an acupoint is thought to be part of an anti-inflammatory effect and the central modulation of pain processing. Objectives • Using the rat model of collagenase-induced osteoarthritis (CIOA), the study intended to investigate the analgesic effects of bee venom acupuncture (BVA) as they are related to the acupuncture points and dosage used and to determine whether the analgesic mechanisms of BVA for pain were mediated by opioid or adrenergic receptors...
June 23, 2017: Alternative Therapies in Health and Medicine
https://www.readbyqxmd.com/read/28640078/prospective-observational-pharmacogenetic-study-of-side-effects-induced-by-intravenous-morphine-for-postoperative-analgesia
#12
Li-Kuei Chen, Mao-Hsien Wang, Hong-Jyh Yang, Shou-Zen Fan, Shiou-Sheng Chen
Nausea and vomiting are probably the most unpleasant side effects that occur when morphine used. A number of studies have investigated the effect on pain relief of single nucleotide polymorphisms (SNPs) in genes involved in morphine's metabolism, distribution, binding, and cellular action. The mechanism through which morphine causes nausea and vomiting has not been elucidated clearly. We examined all the reported SNPs which are associated with the complications of morphine, including SNPs in genes for phase I and phase II metabolic enzymes, ABC binding cassette drug transporters, κ and δ opioid receptors, and ion channels implicated in the postreceptor action of morphine...
June 2017: Medicine (Baltimore)
https://www.readbyqxmd.com/read/28606631/restraint-stress-enhances-alcohol-intake-in-adolescent-female-rats-but-reduces-alcohol-intake-in-adolescent-male-and-adult-female-rats
#13
Aranza Wille-Bille, Ana Ferreyra, Martina Sciangula, Florencia Chiner, Michael E Nizhnikov, Ricardo Marcos Pautassi
Adolescents may be more sensitive to stress-induced alcohol drinking than adults, which would explain the higher prevalence of alcohol abuse and dependence in late adolescence than in adulthood. The present study analyzed the impact of restraint stress on the initiation of alcohol intake across 2 weeks of intermittent, two-bottle choice intake in male and female adolescent rats and adult female rats. Restraint stress significantly increased alcohol intake and preference in female adolescent rats but decreased alcohol intake and preference in male adolescent and female adult rats...
June 10, 2017: Behavioural Brain Research
https://www.readbyqxmd.com/read/28604788/long-term-efficacy-and-safety-of-nalfurafine-hydrochloride-on-pruritus-in-chronic-liver-disease-patients-patient-reported-outcome-based-analyses
#14
Kenya Kamimura, Takeshi Yokoo, Hiroteru Kamimura, Akira Sakamaki, Satoshi Abe, Atsunori Tsuchiya, Masaaki Takamura, Hirokazu Kawai, Satoshi Yamagiwa, Shuji Terai
BACKGROUND AND AIM: Among various symptoms accompanied with chronic liver disease, pruritus affects the quality of life of patients, causing physical and mental stress, and worsens hepatic function. Recently, κ-opioid receptor agonist, nalfurafine hydrochloride was approved to treat central pruritus in patients with liver disease in Japan. This study aimed to assess the long-term efficacy and safety of nalfurafine hydrochloride on pruritus in chronic liver disease patients. METHODS: A patient-reported outcome using questionnaire-based methods was used for 41 liver disease patients with or without pruritus symptoms...
2017: PloS One
https://www.readbyqxmd.com/read/28590304/antinociceptive-effect-of-epicatechin-in-inflammatory-and-neuropathic-pain-in-rats
#15
Geovanna N Quiñonez-Bastidas, Jorge B Pineda-Farias, Francisco J Flores-Murrieta, Juan Rodríguez-Silverio, Juan G Reyes-García, Beatriz Godínez-Chaparro, Vinicio Granados-Soto, Héctor I Rocha-González
The aim of this study was to investigate the antinociceptive potential of (-)-epicatechin and the possible mechanisms of action involved in its antinociceptive effect. The carrageenan and formalin tests were used as inflammatory pain models. A plethysmometer was used to measure inflammation and L5/L6 spinal nerve ligation as a neuropathic pain model. Oral (-)-epicatechin reduced carrageenan-induced inflammation and nociception by about 59 and 73%, respectively, and reduced formalin- induced and nerve injury-induced nociception by about 86 and 43%, respectively...
June 5, 2017: Behavioural Pharmacology
https://www.readbyqxmd.com/read/28571505/buprenorphine-implants-in-medical-treatment-of-opioid-addiction
#16
REVIEW
Steven Chavoustie, Michael Frost, Ole Snyder, Joel Owen, Mona Darwish, Ryan Dammerman, Victoria Sanjurjo
Opioid use disorder is a chronic, relapsing disease that encompasses use of both prescription opioids and heroin and is associated with a high annual rate of overdose deaths. Medical treatment has proven more successful than placebo treatment or psychosocial intervention, and the partial µ-opioid receptor agonist and κ-opioid receptor antagonist buprenorphine is similar in efficacy to methadone while offering lower risk of respiratory depression. However, frequent dosing requirements and potential for misuse and drug diversion contribute to significant complications with treatment adherence for available formulations...
August 2017: Expert Review of Clinical Pharmacology
https://www.readbyqxmd.com/read/28512665/involvement-of-%C3%A2%C2%B5-opioid-receptors-and-%C3%AE%C2%BA-opioid-receptors-in-itch-related-scratching-behaviour-of-imiquimod-induced-psoriasis-like-dermatitis-in-mice
#17
Nobuaki Takahashi, Mitsutoshi Tominaga, Ryohei Kosaka, Yayoi Kamata, Yoshie Umehara, Hironori Matsuda, Azumi Sakaguchi, Hideoki Ogawa, Kenji Takamori
The pathogenesis of psoriatic itch is poorly understood. The aim of this study was to investigate the involvement of opioid receptors in scratching behaviour of imiquimod-induced psoriasis-like dermatitis model mice. Topical application of 5% imiquimod cream to the rostral back skin of mice induced antihistamine-resistant scratching behaviour. The expression of µ-opioid receptor (MOR) protein increased in the epidermis, dorsal root ganglia (DRG) and spinal cord of imiquimod-treated mice. In contrast, the expression of κ-opioid receptor (KOR) protein decreased in the DRG and spinal cord of imiquimod-treated mice, and was undetectable in the epidermis of both groups...
May 17, 2017: Acta Dermato-venereologica
https://www.readbyqxmd.com/read/28502978/the-opioid-receptor-triple-agonist-dpi-125-produces-analgesia-with-less-respiratory-depression-and-reduced-abuse-liability
#18
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...
July 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28502907/neuropathic-and-inflammatory-antinociceptive-effects-and-electrocortical-changes-produced-by-salvia-divinorum-in-rats
#19
Karina Simón-Arceo, Ma Eva González-Trujano, Ulises Coffeen, Rodrigo Fernández-Mas, Francisco Mercado, Angélica Almanza, Bernardo Contreras, Orlando Jaimes, Francisco Pellicer
ETHNOPHARMACOLOGICAL RELEVANCE: Salvia divinorum is a medicinal plant traditionally used in hallucinogenic ethnopharmacological practices and for its analgesic and antinflammatory properties. Its active compounds include diterpenes known as salvinorins which act as potent κ opioid receptor agonists. AIM OF THE STUDY: Given its effects in acute animal models of pain, as well as its antinflammatory attributes, we decided to investigate the analgesic effects of an SD extract in neuropathic (sciatic loose nerve ligature) and inflammatory (intra plantar carrageenan) pain models in rats...
July 12, 2017: Journal of Ethnopharmacology
https://www.readbyqxmd.com/read/28502630/new-opioid-receptor-antagonist-naltrexone-14-o-sulfate-synthesis-and-pharmacology
#20
Ferenc Zádor, Kornél Király, András Váradi, Mihály Balogh, Ágnes Fehér, Dóra Kocsis, Anna I Erdei, Erzsébet Lackó, Zoltán S Zádori, Sándor Hosztafi, Béla Noszál, Pál Riba, Sándor Benyhe, Susanna Fürst, Mahmoud Al-Khrasani
Opioid antagonists, naloxone and naltrexone have long been used in clinical practice and research. In addition to their low selectivity, they easily pass through the blood-brain barrier. Quaternization of the amine group in these molecules, (e.g. methylnaltrexone) results in negligible CNS penetration. In addition, zwitterionic compounds have been reported to have limited CNS access. The current study, for the first time gives report on the synthesis and the in vitro [competition binding, G-protein activation, isolated mouse vas deferens (MVD) and mouse colon assay] pharmacology of the zwitterionic compound, naltrexone-14-O-sulfate...
May 11, 2017: European Journal of Pharmacology
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