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https://www.readbyqxmd.com/read/28893975/agonist-dependent-and-independent-kappa-opioid-receptor-phosphorylation-showed-distinct-phosphorylation-patterns-and-resulted-in-different-cellular-outcomes
#1
Yi-Ting Chiu, Chongguang Chen, Daohai Yu, Stefan Schulz, Lee-Yuan Liu-Chen
We reported previously that the selective agonist U50,488H promoted phosphorylation of the mouse kappa opioid receptor (KOPR) at residues S356, T357, T363 and S369. Here, we found that agonist (U50,488H)-dependent KOPR phosphorylation at all the residues were mediated by Gi/oα proteins and multiple protein kinases [GRKs2, 3, 5 and 6 and protein kinase C (PKC)]. In addition, PKC activation by phorbol ester induced agonist-independent KOPR phosphorylation. Compared with U50,488H, PKC activation promoted much higher S356/T357 phosphorylation, much lower T363 phosphorylation and similar levels of S369 phosphorylation...
September 11, 2017: Molecular Pharmacology
https://www.readbyqxmd.com/read/28893017/a-comparative-study-of-analgesic-effect-of-intrathecal-nalbuphine-and-fentanyl-as-adjuvant-in-lower-limb-orthopaedic-surgery
#2
Shagufta Naaz, Usha Shukla, Swati Srivastava, Erum Ozair, Adil Asghar
INTRODUCTION: Intrathecal opioids when added to local anaesthetics decrease their dosage and provide haemodynamic stability. Nalbuphine is an agonist-antagonist and acts on kappa receptors providing analgesia. AIM: The study aims to compare the analgesic efficacy of fentanyl with that of two doses of nalbuphine when used with injection bupivacaine heavy in spinal anaesthesia. MATERIALS AND METHODS: A randomised, double blinded, prospective study on 90 patients of ASA I and II undergoing lower limb orthopaedic surgery under subarachnoid block was done...
July 2017: Journal of Clinical and Diagnostic Research: JCDR
https://www.readbyqxmd.com/read/28886759/epigenetic-regulation-of-the-kappa-opioid-receptor-by-child-abuse
#3
Pierre-Eric Lutz, Jeffrey A Gross, Sabine K Dhir, Gilles Maussion, Jennie Yang, Alexandre Bramoulle, Michael J Meaney, Gustavo Turecki
BACKGROUND: Experiences of abuse and neglect during childhood are major predictors of the emergence of depressive and suicidal behaviors throughout life. The underlying biological mechanisms, however, remain poorly understood. Here, we focused on the opioid system as a potential brain substrate mediating these effects. METHODS: Postmortem samples from three brain structures regulating social bonds and emotions were analyzed. Groups were constituted of depressed individuals who died by suicide, with or without a history of severe child abuse, and of psychiatrically healthy control subjects...
July 27, 2017: Biological Psychiatry
https://www.readbyqxmd.com/read/28844812/antidepressant-like-effects-of-3-carboxamido-seco-nalmefene-3cs-nalmefene-a-novel-opioid-receptor-modulator-in-a-rat-ifn-%C3%AE-induced-depression-model
#4
Charlotte K Callaghan, Jennifer Rouine, Reginald L Dean, Brian I Knapp, Jean M Bidlack, Daniel R Deaver, Shane M O'Mara
Patients receiving the cytokine immunotherapy, interferon-alpha (IFN-α) frequently present with neuropsychiatric consequences and cognitive impairments. Patients (25-80%) report symptoms of depression, including, anhedonia, irritability, fatigue and impaired motivation. Our lab has previously demonstrated treatment (170,000IU/kg sc, 3 times per week for 4weeks) of the pro-inflammatory cytokine, IFN-α, induced a depressive phenotype in rats in the forced swim test (FST). Here, we examine the biological mechanisms underlying behavioral changes induced by IFN-α, which may be reflective of mechanisms underlying inflammation associated depression...
August 24, 2017: Brain, Behavior, and Immunity
https://www.readbyqxmd.com/read/28830758/the-medicinal-chemistry-and-neuropharmacology-of-kratom-a-preliminary-discussion-of-a-promising-medicinal-plant-and-analysis-of-its-potential-for-abuse
#5
REVIEW
Andrew C Kruegel, Oliver Grundmann
The leaves of Mitragyna speciosa (commonly known as kratom), a tree endogenous to parts of Southeast Asia, have been used traditionally for their stimulant, mood-elevating, and analgesic effects and have recently attracted significant attention due to increased use in Western cultures as an alternative medicine. The plant's active alkaloid constituents, mitragynine and 7-hydroxymitragynine, have been shown to modulate opioid receptors, acting as partial agonists at mu-opioid receptors and competitive antagonists at kappa- and delta-opioid receptors...
August 19, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28807672/pharmacological-characterization-of-novel-synthetic-opioids-nso-found-in-the-recreational-drug-marketplace
#6
REVIEW
Michael H Baumann, Susruta Majumdar, Valerie Le Rouzic, Amanda Hunkele, Rajendra Uprety, Xi Ping Huang, Jin Xu, Bryan L Roth, Ying-Xian Pan, Gavril W Pasternak
Novel synthetic opioids (NSO) are increasingly encountered in illicit heroin and counterfeit pain pills. Many NSO are resurrected from older biomedical literature or patent applications, so limited information is available about their biological effects. Here we examined the pharmacology of three structurally-distinct NSO found in the recreational drug market: N-(1-(2-phenylethyl)-4-piperidinyl)-N-phenylbutyramide (butyrylfentanyl), 3,4-dichloro-N-[(1R,2R)-2-(dimethylamino)cyclohexyl]-N-methylbenzamide (U-47700) and 1-cyclohexyl-4-(1,2-diphenylethyl)piperazine (MT-45)...
August 11, 2017: Neuropharmacology
https://www.readbyqxmd.com/read/28806860/patient-caregiver-and-provider-perceptions-of-pain-and-pain-management-in-adolescents-and-young-adults-with-bleeding-disorders
#7
Angela Lambing, Cynthia D Nichols, James E Munn, Terry L Anderson, Bartholomew J Tortella, Michelle L Witkop
INTRODUCTION: Recurrent bleeding and associated pain are critical components in the management of bleeding disorders, yet scant data describe perceptions of pain in this patient population. OBJECTIVE: This study assessed perceptions of pain and pain management in adolescents and young adults (AYAs) with haemophilia or von Willebrand disease (VWD) to determine agreement/disagreement between patients, caregivers and health care providers. METHODS: Using an online questionnaire, AYA patients (N=89), their caregivers (N=77), and providers (N=54) reported on pain perception, pain treatment and pain control...
August 14, 2017: Haemophilia: the Official Journal of the World Federation of Hemophilia
https://www.readbyqxmd.com/read/28802836/neocortical-prodynorphin-expression-is-transiently-increased-with-learning-implications-for-time-and-learning-dependent-neocortical-kappa-opioid-receptor-activation
#8
Ryan Loh, Sean Collins, Roberto Galvez
There are several lines of evidence that indicate a prominent role for the opioid system in the acquisition and consolidation of learned associations. Specifically, kappa opioid receptor (KOR) modulation has been demonstrated to alter various behavioral tasks including whisker trace eyeblink conditioning (WTEB). WTEB is an associative conditioning paradigm in which a neutral conditioned stimulus (CS; Whisker stimulation) is paired following a short stimulus free trace interval with a salient unconditioned stimulus that elicits a blink response (US; Eye shock)...
August 9, 2017: Behavioural Brain Research
https://www.readbyqxmd.com/read/28796483/placement-of-hydroxy-moiety-on-pendant-of-peptidomimetic-scaffold-modulates-mu-and-kappa-opioid-receptor-efficacy
#9
Aubrie A Harland, Irina D Pogozheva, Nicholas W Griggs, Tyler J Trask, John R Traynor, Henry I Mosberg
In an effort to expand the structure-activity relationship (SAR) studies of a series of mixed-efficacy opioid ligands, peptidomimetics that incorporate methoxy and hydroxy groups around a benzyl or 2-methylindanyl pendant on a tetrahydroquinoline (THQ) core of the peptidomimetics were evaluated. Compounds containing a methoxy or hydroxy moiety in the o- or m- positions increased binding affinity to the kappa opioid receptor (KOR), whereas compounds containing methoxy or hydroxy groups in the p- position decreased KOR affinity and reduced or eliminated efficacy at the mu opioid receptor (MOR)...
August 10, 2017: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/28770825/kappa-opioid-receptor-agonist-u50448h-protects-against-renal-ischemia-reperfusion-injury-in-rats-via-activating-the-pi3k-akt-signaling-pathway
#10
Li-Jie Liu, Jian-Jun Yu, Xiao-Lin Xu
Renal ischemia-reperfusion injury (IRI) is regarded as a leading cause of acute kidney failure and renal dysfunction. Previous studies show that kappa opioid receptor (KOR) agonists can attenuate IRI in cardiomycytes and neuronal cells. In this study we explored the effects of a KOR agonist on renal IRI and the underlying mechanisms in vivo and in vitro. An IRI model was established in SD rats, which were intravenously pretreated with a KOR agonist U50448H (1 mg/kg), a KOR antagonist Nor-BNI (2 mg/kg) followed by U50448H (1 mg/kg), or the PI3K inhibitor wortmannin (1...
August 3, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28747521/a-novel-18-f-labeled-kappa-opioid-receptor-antagonist-as-pet-radiotracer-synthesis-and-in-vivo-evaluation-of-18-f-ly2459989-in-non-human-primates
#11
Songye Li, Zhengxin Cai, Ming-Qiang Zheng, Daniel Holden, Mika Naganawa, Shu-Fei Lin, Jim Ropchan, David Labaree, Michael Kapinos, Teresa Lara-Jaime, Antonio Navarro, Yiyun Huang
The kappa opioid receptor (KOR) is implicated in depression, addictions, and other central nervous system (CNS) disorders and thus an important target for drug development. We have previously developed a number of (11)C-labeled PET radiotracers for KOR imaging in humans. Here we report the synthesis and evaluation of (18)F-LY2459989 as the first (18)F-labeled KOR antagonist radiotracer in non-human primates and its comparison with (11)C-LY2459989. Methods: The novel radioligand (18)F-LY2459989 was synthesized by (18)F-displacement of a nitro group or an iodonium ylide...
July 26, 2017: Journal of Nuclear Medicine: Official Publication, Society of Nuclear Medicine
https://www.readbyqxmd.com/read/28745394/opioids-for-chronic-non-cancer-pain-in-children-and-adolescents
#12
REVIEW
Tess E Cooper, Emma Fisher, Andrew L Gray, Elliot Krane, Navil Sethna, Miranda Al van Tilburg, Boris Zernikow, Philip J Wiffen
BACKGROUND: Pain is a common feature of childhood and adolescence around the world, and for many young people, that pain is chronic. The World Health Organization guidelines for pharmacological treatments for children's persisting pain acknowledge that pain in children is a major public health concern of high significance in most parts of the world. While in the past, pain was largely dismissed and was frequently left untreated, views on children's pain have changed over time, and relief of pain is now seen as importantWe designed a suite of seven reviews on chronic non-cancer pain and cancer pain (looking at antidepressants, antiepileptic drugs, non-steroidal anti-inflammatory drugs, opioids, and paracetamol as priority areas) in order to review the evidence for children's pain utilising pharmacological interventions in children and adolescents...
July 26, 2017: Cochrane Database of Systematic Reviews
https://www.readbyqxmd.com/read/28740609/simple-tetrahydroisoquinolines-are-potent-and-selective-kappa-opioid-receptor-antagonists
#13
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/28740600/seeking-and-finding-biased-ligands-of-the-kappa-opioid-receptor
#14
Laura M Bohn, Jeffrey Aubé
The discovery and characterization of two classes of kappa opioid receptor agonists that are biased for G protein over βarrestin signaling are described.
July 13, 2017: ACS 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
#15
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/28734766/trpv1-modulates-morphine-induced-conditioned-place-preference-via-p38-mapk-in-the-nucleus-accumbens
#16
Sa-Ik Hong, Thi-Lien Nguyen, Shi-Xun Ma, Hyoung-Chun Kim, Seok-Yong Lee, Choon-Gon Jang
Emerging evidence suggests that the transient receptor potential vanilloid type 1 channel (TRPV1) is a novel target for the treatment of drug addiction, such as cocaine and morphine. Previously we reported that TRPV1 inhibition reduced morphine reward in the dorsal striatum (DSt) of mice and morphine self-administration through a decrease in accumbal activity in rats. However, the role of TRPV1 on morphine-conditioned reward in addiction-related brain regions, such as the nucleus accumbens (NAc), has not been previously established...
July 19, 2017: Behavioural Brain Research
https://www.readbyqxmd.com/read/28721822/opioid-antagonists-for-pharmacological-treatment-of-gambling-disorder-are-they-relevant
#17
Caroline Victorri-Vigneau, Andrew Spiers, Pascal Caillet, Mélanie Bruneau, Gaëlle Challet-Bouju, Marie Grall-Bronnec
Background: To date, no drugs have been approved for gambling disorder. Numerous publications have described the value of opioid antagonists. Indeed, the mesocorticolimbic dopaminergic pathway has been suggested as the underlying cause of reward-seeking behaviour, and it is modulated by the opioid system. Objective: This study aims to evaluate the relevance of opioid antagonists for treating GD. Method A systematic literature review was conducted. A search of the PubMed electronic database, PsycINFO and the Cochrane Systematic Review Database without any limits was performed...
July 18, 2017: Current Neuropharmacology
https://www.readbyqxmd.com/read/28718638/semisynthesis-and-kappa-opioid-receptor-activity-of-derivatives-of-columbin-a-furanolactone-diterpene
#18
Anil Yilmaz, Rachel Saylor Crowley, Alexander M Sherwood, Thomas E Prisinzano
Columbin (1) is a furanolactone diterpene isolated from the roots of Jateorhiza and Tinospora species. These species generally grow in Asia and Africa and have been used in folk medicine for their apparent analgesic and antipyretic activities. Columbin (1) is of particular interest due to its structural similarity to the known kappa-opioid receptor (KOR) agonist salvinorin A. Given that the KOR is of interest in the study of many serious diseases, such as anxiety, depression, and drug addiction, obtaining natural or semisynthetic molecules with KOR activity recently has gained much interest...
July 28, 2017: Journal of Natural Products
https://www.readbyqxmd.com/read/28693915/selective-opioid-growth-factor-receptor-antagonists-based-on-a-stilbene-isostere
#19
David P Stockdale, Michelle B Titunick, Jessica M Biegler, Jessie L Reed, Alyssa M Hartung, David F Wiemer, Patricia J McLaughlin, Jeffrey D Neighbors
As part of an ongoing drug development effort aimed at selective opioid receptor ligands based on the pawhuskin natural products we have synthesized a small set of amide isosteres. These amides were centered on lead compounds which are selective antagonists for the delta and kappa opioid receptors. The amide isomers revealed here show dramatically different activity from the parent stilbene compounds. Three of the isomers synthesized showed antagonist activity for the opioid growth factor (OGF)/opioid growth factor receptor (OGFR) axis which is involved in cellular and organ growth control...
August 15, 2017: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/28674176/effects-of-chronic-social-defeat-stress-on-sleep-and-circadian-rhythms-are-mitigated-by-kappa-opioid-receptor-antagonism
#20
Audrey M Wells, Elysia Ridener, Clinton A Bourbonais, Woori Kim, Harry Pantazopoulos, F Ivy Carroll, Kwang-Soo Kim, Bruce M Cohen, William A Carlezon
Stress plays a critical role in the neurobiology of mood and anxiety disorders. Sleep and circadian rhythms are affected in many of these conditions. Here we examined the effects of chronic social defeat stress (CSDS), an ethological form of stress, on sleep and circadian rhythms. We exposed male mice implanted with wireless telemetry transmitters to a 10 day CSDS regimen known to produce anhedonia (a depressive-like effect) and social avoidance (an anxiety-like effect). EEG, EMG, body temperature, and locomotor activity data were collected continuously during the CSDS regimen and a 5 day recovery period...
August 9, 2017: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
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