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https://www.readbyqxmd.com/read/29785554/interactions-between-kappa-and-mu-opioid-receptor-agonists-effects-of-the-ratio-of-drugs-in-mixtures
#1
Vanessa Minervini, Hannah Y Lu, Jahnavi Padarti, Daniela C Osteicoechea, Charles P France
RATIONALE: Pain is the leading reason for seeking health care, and mu opioid receptor agonists continue to be prescribed despite well-documented adverse effects. Kappa opioid receptor agonists have antinociceptive effects with little to no abuse liability and might be useful for treating pain in mixtures. Kappa:mu opioid mixtures might be useful if therapeutic effects of each drug can be selectively increased while reducing or avoiding the adverse effects that occur with larger doses of each drug alone...
May 22, 2018: Psychopharmacology
https://www.readbyqxmd.com/read/29779230/role-of-mu-but-not-delta-or-kappa-opioid-receptors-in-context-induced-reinstatement-of-oxycodone-seeking
#2
Jennifer M Bossert, Jennifer K Hoots, Ida Fredriksson, Sweta Adhikary, Michelle Zhang, Marco Venniro, Yavin Shaham
Relapse to nonmedical use of prescription opioids often occurs after exposure to places previously associated with drug use. Here, we describe a rat model of context-induced reinstatement of oxycodone seeking after repeated cycles of drug self-administration and extinction-induced abstinence. We also determined the role of mu, delta, and kappa opioid receptors (MOR, DOR, KOR) in this reinstatement. We trained rats to self-administer oxycodone for 6 h/d in Context A; lever pressing was paired with a discrete cue...
May 19, 2018: European Journal of Neuroscience
https://www.readbyqxmd.com/read/29768187/activation-of-kappa-opioid-receptors-in-the-dorsal-raphe-have-sex-dependent-effects-on-social-behavior-in-california-mice
#3
Emily C Wright, Tiffany V Parks, Jonathon O Alexander, Rajesh Supra, Brian C Trainor
Kappa opioid receptor activation has been linked to stress and anxiety behavior, thus leading to kappa antagonists being popularized in research as potential anxiolytics. However, while these findings may hold true in standard models, the neuromodulatory effects of social defeat may change the behavioral outcome of kappa opioid receptor activation. Previous research has shown that social defeat can lead to hyperactivity of serotonergic neurons in the dorsal raphe nucleus, and that inhibition of this increase blocks the social deficits caused by defeat...
May 13, 2018: Behavioural Brain Research
https://www.readbyqxmd.com/read/29752444/kappa-opioid-antagonists-as-stress-resilience-medications-for-the-treatment-of-alcohol-use-disorders
#4
Charles Chavkin
No abstract text is available yet for this article.
March 27, 2018: Neuropsychopharmacology: Official Publication of the American College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/29734749/synthesis-and-structure-activity-relationships-of-cis-n-normetazocine-based-lp1-derivatives
#5
Lorella Pasquinucci, Carmela Parenti, Emanuele Amata, Zafiroula Georgoussi, Paschalina Pallaki, Valeria Camarda, Girolamo Calò, Emanuela Arena, Lucia Montenegro, Rita Turnaturi
(−)- cis - N -Normetazocine represents a rigid scaffold able to mimic the tyramine moiety of endogenous opioid peptides, and the introduction of different N -substituents influences affinity and efficacy of respective ligands at MOR (mu opioid receptor), DOR (delta opioid receptor), and KOR (kappa opioid receptor). We have previously identified LP1, a MOR/DOR multitarget opioid ligand, with an N -phenylpropanamido substituent linked to (−)- cis - N -Normetazocine scaffold. Herein, we report the synthesis, competition binding and calcium mobilization assays of new compounds 10 ⁻ 16 that differ from LP1 by the nature of the N -substituent...
May 5, 2018: Pharmaceuticals
https://www.readbyqxmd.com/read/29729777/methadone-maximizing-safety-and-efficacy-for-pain-control-in-patients-with-cancer
#6
REVIEW
Mary Lynn McPherson, Ryan C Costantino, Alexandra L McPherson
Methadone is a valuable opioid in the management of patients who have cancer with pain. Methadone is a mu-, kappa-, and delta-opioid agonist, and an N-methyl-D-aspartate receptor antagonist. These mechanisms of action make methadone an attractive option for complex pain syndromes. It is critically important that providers consider a patient's risk status before beginning methadone. Careful consideration must be given to dosing methadone in both opioid-naïve and opioid-tolerant patients, with vigilant monitoring for therapeutic effectiveness and potential toxicity until the patient achieves steady state...
June 2018: Hematology/oncology Clinics of North America
https://www.readbyqxmd.com/read/29713172/gender-specific-association-of-functional-prodynorphin-68-bp-repeats-with-cannabis-exposure-in-an-african-american-cohort
#7
Vadim Yuferov, Eduardo R Butelman, Mary Jeanne Kreek
Background: Cannabis use disorders (CUDs) cause substantial neuropsychiatric morbidity and comorbidity. There is evidence for gender-based differences in CUDs, for instance, a greater prevalence in males than in females. The main active component of cannabis is delta 9-tetrahydrocannabinol (delta 9-THC), a partial agonist of the cannabinoid type 1 receptor. Preclinical studies show that genetic or pharmacological manipulation of the kappa opioid receptor/dynorphin system modulates the effects of delta 9-THC...
2018: Neuropsychiatric Disease and Treatment
https://www.readbyqxmd.com/read/29687539/using-prescription-claims-to-detect-aberrant-behaviors-with-opioids-comparison-and-validation-of-5-algorithms
#8
Kathryn Rough, Krista F Huybrechts, Sonia Hernandez-Diaz, Rishi J Desai, Elisabetta Patorno, Brian T Bateman
OBJECTIVE: Compare and validate 5 algorithms to detect aberrant behavior with opioids: Opioid Misuse Score, Controlled Substance-Patterns of Utilization Requiring Evaluation (CS-PURE), Overutilization Monitoring System, Katz, and Cepeda algorithms. STUDY DESIGN AND SETTING: We identified new prescription opioid users from 2 insurance databases: Medicaid (2000-2006) and Clinformatics Data Mart (CDM; 2004-2013). Patients were followed 1 year, and aberrant opioid behavior was defined according to each algorithm, using Cohen's kappa to assess agreement...
April 24, 2018: Pharmacoepidemiology and Drug Safety
https://www.readbyqxmd.com/read/29673620/effects-of-opioid-and-non-opioid-analgesics-on-responses-to-psychosocial-stress-in-humans
#9
Anya K Bershad, Melissa A Miller, Greg J Norman, Harriet de Wit
Both preclinical and clinical evidence suggests that the endogenous opioid system is involved in responses to stress. For example, in animal models opioid agonists reduce isolation distress whereas opioid antagonists increase isolation distress. We recently reported that the mixed mu agonist and kappa antagonist buprenorphine dampened responses to acute psychosocial stress in humans. Now we extend this to study the effects of a pure mu-opioid agonist, hydromorphone, and a non-opioid analgesic, acetaminophen, on response to social stress...
April 16, 2018: Hormones and Behavior
https://www.readbyqxmd.com/read/29669731/involvement-of-activated-brain-stress-responsive-systems-in-excessive-and-relapse-alcohol-drinking-in-rodent-models-implications-for-therapeutics
#10
Yan Zhou, Mary Jeanne Kreek
Addictive diseases, including addiction to alcohol pose massive public health costs. Addiction is a chronic relapsing disease, caused by both the direct effects induced by drugs and persistent neuroadaptations at several (molecular, cellular and behavioral) levels. These drug-type specific neuro-adaptations are brought on largely by the reinforcing effects of drugs on the central nervous system and environment, including stress. Results from animal experiments have demonstrated important interactions between alcohol and the stress responsive systems...
April 18, 2018: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/29669290/non-canonical-opioid-signaling-inhibits-itch-transmission-in-the-spinal-cord-of-mice
#11
Admire Munanairi, Xian-Yu Liu, Devin M Barry, Qianyi Yang, Jun-Bin Yin, Hua Jin, Hui Li, Qing-Tao Meng, Jia-Hang Peng, Zhen-Yu Wu, Jun Yin, Xuan-Yi Zhou, Li Wan, Ping Mo, Seungil Kim, Fu-Quan Huo, Joseph Jeffry, Yun-Qing Li, Rita Bardoni, Michael R Bruchas, Zhou-Feng Chen
Chronic itch or pruritus is a debilitating disorder that is refractory to conventional anti-histamine treatment. Kappa opioid receptor (KOR) agonists have been used to treat chronic itch, but the underlying mechanism remains elusive. Here, we find that KOR and gastrin-releasing peptide receptor (GRPR) overlap in the spinal cord, and KOR activation attenuated GRPR-mediated histamine-independent acute and chronic itch in mice. Notably, canonical KOR-mediated Gαi signaling is not required for desensitizing GRPR function...
April 17, 2018: Cell Reports
https://www.readbyqxmd.com/read/29615341/a-review-of-salvinorin-analogs-and-their-kappa-opioid-receptor-activity
#12
REVIEW
Jeremy J Roach, Ryan A Shenvi
The plant metabolite salvinorin A potently and selectively agonizes the human kappa-opioid receptor, an emerging target for next-generation analgesics. Here we review analogs of the salvinorin chemotype and their effects on selectivity, affinity and potency. Extensive peripheral modifications using isolated salvinorin A have delivered a trove of SAR information. More deep-seated changes are now possible by advances in chemical synthesis.
March 12, 2018: Bioorganic & Medicinal Chemistry Letters
https://www.readbyqxmd.com/read/29596097/repeated-morphine-prolongs-postoperative-pain-in-male-rats
#13
Peter M Grace, Erika L Galer, Keith A Strand, Kaci Corrigan, Debra Berkelhammer, Steven F Maier, Linda R Watkins
BACKGROUND: Opioids are effective postoperative analgesics. Disturbingly, we have previously reported that opioids such as morphine can worsen inflammatory pain and peripheral and central neuropathic pain. These deleterious effects are mediated by immune mediators that promote neuronal hyperexcitability in the spinal dorsal horn. Herein, we tested whether perioperative morphine could similarly prolong postoperative pain in male rats. METHODS: Rats were treated with morphine for 7 days, beginning immediately after laparotomy, while the morphine was tapered in a second group...
March 27, 2018: Anesthesia and Analgesia
https://www.readbyqxmd.com/read/29556136/secondary-metabolites-isolated-from-pinus-roxburghii-and-interpretation-of-their-cannabinoid-and-opioid-binding-properties-by-virtual-screening-and-in-vitro-studies
#14
Rola M Labib, Radhakrishnan Srivedavyasasri, Fadia S Youssef, Samir A Ross
Pinus roxburghii is highly popular as a potent analgesic and anti-inflammatory agent; however its exact mechanism of action was not fully elucidated. We aimed to interpret the analgesic and anti-inflammatory activity of the total ethanol extract of Pinus roxburghii bark (PRE) and its isolated compounds by both in silico molecular modelling and in-vitro cannabinoid and opioid binding activities evaluation for the first time. Comprehensive phytochemical investigation of PRE resulted in the isolation of sixteen compounds that were fully elucidated using1 H NMR and13 C NMR...
March 2018: Saudi Pharmaceutical Journal: SPJ: the Official Publication of the Saudi Pharmaceutical Society
https://www.readbyqxmd.com/read/29547588/synthesis-and-structure-activity-relationships-of-lp1-derivatives-n-methyl-n-phenylethylamino-analogues-as-novel-mor-agonists
#15
Rita Turnaturi, Carmela Parenti, Orazio Prezzavento, Agostino Marrazzo, Paschalina Pallaki, Zafiroula Georgoussi, Emanuele Amata, Lorella Pasquinucci
The opioid pharmacological profile of cis -(-)- N -normetazocine derivatives is deeply affected by the nature of their N -substituents. Here, our efforts were focused on the synthesis and pharmacological evaluation of novel derivatives of the lead LP1, a multitarget opioid analgesic compound featuring an N -phenylpropanamido substituent. LP1 derivatives 5a - d and 6a - d were characterized by flexible groups at the N -substituent that allow them to reposition themselves relative to cis -(-)- N -normetazocine nucleus, thus producing different pharmacological profiles at the mu, delta and kappa opioid receptors (MOR, DOR and KOR) in in vitro and in vivo assays...
March 16, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
https://www.readbyqxmd.com/read/29528965/evaluation-of-different-drug-classes-on-transient-sciatic-nerve-injury-depressed-marble-burying-in-mice
#16
Jenny L Wilkerson, Zachary A Curry, Pamela D Kinlow, Brittany L Mason, Ku-Lung Hsu, Mario van der Stelt, Benjamin F Cravatt, Aron H Lichtman
A great need exists for the identification of new effective analgesics to treat sustained pain. However, most preclinical nociceptive assays measure behavioral responses evoked by noxious stimuli (ie, pain-stimulated behavior), which presents a challenge to distinguish between motor impairing and antinociceptive effects of drugs. Here, we demonstrate that chronic constriction injury (CCI) of the sciatic nerve elicits common pain-stimulated responses (ie, mechanical allodynia and thermal hyperalgesia) as well as reduces marble burying/digging behaviors that occur during the early stages of the neuropathy and resolve within 1 week...
June 2018: Pain
https://www.readbyqxmd.com/read/29526023/contribution-of-dynorphin-and-orexin-neuropeptide-systems-to-the-motivational-effects-of-alcohol
#17
Rachel I Anderson, David E Moorman, Howard C Becker
Understanding the neural systems that drive alcohol motivation and are disrupted in alcohol use disorders is of critical importance in developing novel treatments. The dynorphin and orexin/hypocretin neuropeptide systems are particularly relevant with respect to alcohol use and misuse. Both systems are strongly associated with alcohol-seeking behaviors, particularly in cases of high levels of alcohol use as seen in dependence. Furthermore, both systems also play a role in stress and anxiety, indicating that disruption of these systems may underlie long-term homeostatic dysregulation seen in alcohol use disorders...
March 11, 2018: Handbook of Experimental Pharmacology
https://www.readbyqxmd.com/read/29518397/levo-corydalmine-alleviates-vincristine-induced-neuropathic-pain-in-mice-by-inhibiting-an-nf-kappa-b-dependent-cxcl1-cxcr2-signaling-pathway
#18
Lin Zhou, Yahui Hu, Chengyuan Li, Yunyi Yan, Luyao Ao, Boyang Yu, Weirong Fang, Jihua Liu, Yunman Li
Vincristine is a commonly used chemotherapeutic drug that can produce painful peripheral neuropathy. The chemokine (C-X-C motif) ligand 1 (CXCL1) and its receptor chemokine (C-X-C motif) receptor 2 (CXCR2) may mediate the resolution of this inflammation. In this study, we investigated whether and how CXCL1 contributes to vincristine-induced pain and the underlying mechanisms of levo-corydalmine (l-CDL, a tetrahydroprotoberberine). Oxycodone hydrochloride (a semisynthetic opioid analgesic) was used as positive control in vivo experiments...
March 5, 2018: Neuropharmacology
https://www.readbyqxmd.com/read/29513114/antinociceptive-potency-of-a-fluorinated-cyclopeptide-dmt-c-d-lys-phe-p-cf-3-phe-asp-nh-2
#19
Justyna Piekielna-Ciesielska, Adriano Mollica, Stefano Pieretti, Jakub Fichna, Agata Szymaszkiewicz, Marta Zielińska, Radzisław Kordek, Anna Janecka
Opioid peptides and opiate drugs such as morphine, mediate their analgesic effects, but also undesired side effects, mostly through activation of the mu opioid receptor. However, delta- and kappa-opioid receptors can also contribute to the analgesic effects of opioids. Recent findings showed that simultaneous activation of multiple opioid receptors may result in additional analgesia with fewer side effects. Here, we evaluated the pharmacological profile of our formerly developed mixed mu/kappa-opioid receptor ligands, Dmt-c[D-Lys-Phe-Phe-Asp]NH2 (C-36) and Dmt-c[D-Lys-Phe-p-CF3 -Phe-Asp]NH2 (F-81)...
December 2018: Journal of Enzyme Inhibition and Medicinal Chemistry
https://www.readbyqxmd.com/read/29496608/effects-of-mesyl-salvinorin-b-alone-and-in-combination-with-naltrexone-on-alcohol-deprivation-effect-in-male-and-female-mice
#20
Yan Zhou, Rachel Crowley, Thomas Prisinzano, Mary Jeanne Kreek
Alcohol relapse plays a major role in alcohol dependence and is an important focus for the treatment of alcoholism. The alcohol deprivation effect (ADE) is a widely used paradigm in rodents to model the relapse episodes that occur in human alcoholics. Mesyl Salvinorin B (MSB) is a potent and selective kappa opioid receptor (KOP-r) full agonist, with fewer side effects (e.g., sedation or anhedonia) than classic KOP-r full agonists and a longer duration of action in mice than the structurally similar salvinorin A...
April 23, 2018: Neuroscience Letters
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