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https://www.readbyqxmd.com/read/29917243/sex-specific-activation-of-sk-current-by-isoproterenol-facilitates-action-potential-triangulation-and-arrhythmogenesis-in-rabbit-ventricles
#1
Mu Chen, Dechun Yin, Shuai Guo, Dong-Zhu Xu, Zhuo Wang, Zhenhui Chen, Michael Rubart-von der Lohe, Shien-Fong Lin, Thomas H Everett, James N Weiss, Peng-Sheng Chen
KEY POINTS: It is unknown if sex difference exists in cardiac apamin sensitive small conductance Ca2+ activated K+ (SK) current (IKAS ). There is no sex difference in IKAS at basal condition. However, there is larger IKAS in female rabbit ventricles than in males during isoproterenol infusion. IKAS activation by isoproterenol leads to action potential triangulation in females, indicating its abundant activation at early phases of repolarization. IKAS activation in females induces negative Ca2+ -voltage coupling and promotes electromechanical discordant phase 2 repolarization alternans...
June 19, 2018: Journal of Physiology
https://www.readbyqxmd.com/read/29913911/buprenorphine-clinically-useful-but-often-misunderstood
#2
Stephen Butler
Background There are a number of false myths about buprenorphine based on unconfirmed animal data, even from isolated animal organs, and early clinical research. These myths came into textbooks on pharmacology and pain about 30 years ago and have been difficult to eradicate. Animal models of pain and pain relief are notoriously unreliable as predictors of human clinical effects. The fact is that in clinical practice there is NO bell-shaped dose-response curve, there is NO plateau on the dose-response curve, and there is NO antagonist effect from buprenorphine on other mu-opioid agonists...
December 29, 2017: Scandinavian Journal of Pain
https://www.readbyqxmd.com/read/29872601/serotonin-syndrome-presenting-with-concomitant-tramadol-and-diphenhydramine-use-a-case-report-of-an-unlikely-side-effect
#3
Salman Khan, Shakir Saud, Imran Khan, Muhammad Asif, Osama Ismail, Arqam Salam, Tsu Jung Yang, Kim J Norville
Serotonin syndrome is a condition that occurs following the administration of serotonergic drugs. Interestingly, on rare occasions, it can occur with various drug combinations that can secondarily affect the serum levels of 5-hydroxytryptamin. Tramadol is an analgesic that has mu opioid receptor agonist activity and has also been shown to inhibit the reuptake of serotonin and noradrenaline. Diphenhydramine is a first-generation histamine antagonist prescribed to treat or prevent allergic reactions and can also be used as a sleeping aid...
April 4, 2018: Curēus
https://www.readbyqxmd.com/read/29860612/reinforcing-effects-of-opioid-cannabinoid-mixtures-in-rhesus-monkeys-responding-under-a-food-drug-choice-procedure
#4
David R Maguire, Charles P France
OBJECTIVE: Cannabinoid receptor agonists such as delta-9-tetrahydrocannabinol (Δ9 -THC) enhance the antinociceptive potency of mu opioid receptor agonists such as morphine, indicating that opioid/cannabinoid mixtures might be effective for treating pain. However, such enhancement will be beneficial only if cannabinoids do not also enhance adverse effects of opioids, including those related to abuse. In rhesus monkeys, cannabinoids fail to enhance and often decrease self-administration of the mu opioid receptor agonist heroin, suggesting that opioid/cannabinoid mixtures do not have greater reinforcing effects (abuse potential) compared with opioids alone...
June 3, 2018: Psychopharmacology
https://www.readbyqxmd.com/read/29858157/cyclic-biphalin-analogues-with-a-novel-linker-lead-to-potent-agonist-activities-at-mu-delta-and-kappa-opioid-receptors
#5
Michael Remesic, Giorgia Macedonio, Adriano Mollica, Frank Porreca, Victor Hruby, Yeon Sun Lee
In an effort to improve biphalin's potency and efficacy at the µ-(MOR) and δ-opioid receptors (DOR), a series of cyclic biphalin analogues 1-5 with a cystamine or piperazine linker at the C-terminus were designed and synthesized by solution phase synthesis using Boc-chemistry. Interestingly, all of the analogues showed balanced opioid agonist activities at all opioid receptor subtypes due to enhanced κ-opioid receptor (KOR) activity. Our results indicate that C-terminal flexible linkers play an important role in KOR activity compared to that of the other cyclic biphalin analogues with a hydrazine linker...
May 26, 2018: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/29849948/additive-analgesic-effect-of-dexmedetomidine-and-dezocine-administered-intrathecally-in-a-mouse-pain-model
#6
Ya-Qin Huang, Shao-Hui Guo, Renyu Liu, Sheng-Mei Zhu, Jian-Liang Sun, Yong-Xing Yao
Background: It is known that dexmedetomidine can reduce opioid requirements and that there is a synergistic effect when dexmedetomidine and morphine (a full mu opioid receptor agonist) are administered together. However, it was unclear whether a synergistic or additive effect would be observed when dexmedetomidine was co-administered with a partial mu opioid receptor agonist. The present study was designed to elucidate such effects by intrathecally co-administering dexmedetomidine and dezocine, a partial mu receptor agonist, in a mouse pain model...
May 11, 2018: Oncotarget
https://www.readbyqxmd.com/read/29785888/the-impact-of-oprm1-s-genetic-polymorphisms-on-methadone-maintenance-treatment-in-opioid-addicts-a-systematic-review
#7
Bilel Oueslati, Olfa Moula, Rim Ghachem
AIM: Methadone is a long-acting opioid receptor agonist. It is prescribed to patients with opioid-related use disorders. The OPRM1 gene encodes for methadone's main receptor. It appears that polymorphisms in OPRM1 may affect the efficacy of methadone maintenance treatment (MMT). OBJECTIVE: Our purpose was to identify all relevant published papers dealing with the impact ofOPRM1's SNPs  on MMT's efficacy and to summarize results in order to evaluate the relevance of conducting pretherapeutic genotyping in opioid addicts prior to the onset of MMT...
June 1, 2018: Pharmacogenomics
https://www.readbyqxmd.com/read/29785554/interactions-between-kappa-and-mu-opioid-receptor-agonists-effects-of-the-ratio-of-drugs-in-mixtures
#8
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/29757938/piezo1-channel-is-a-potential-regulator-of-synovial-sarcoma-cell-viability
#9
Takahisa Suzuki, Yukiko Muraki, Noriyuki Hatano, Hiroka Suzuki, Katsuhiko Muraki
Detection of mechanical stress is essential for diverse biological functions including touch, audition, and maintenance of vascular myogenic tone. PIEZO1, a mechano-sensing cation channel, is widely expressed in neuronal and non-neuronal cells and is expected to be involved in important biological functions. Here, we examined the possibility that PIEZO1 is involved in the regulation of synovial sarcoma cell-viability. Application of a PIEZO1 agonist Yoda1 effectively induced Ca2+ response and cation channel currents in PIEZO1 -expressing HEK (HEK-Piezo1) cells and synovial sarcoma SW982 (SW982) cells...
May 14, 2018: International Journal of Molecular Sciences
https://www.readbyqxmd.com/read/29740093/differential-contributions-of-peripheral-and-central-mechanisms-to-pain-in-a-rodent-model-of-osteoarthritis
#10
Adrian R Haywood, Gareth J Hathway, Victoria Chapman
The mechanisms underlying the transition from acute nociceptive pain to centrally maintained chronic pain are not clear. We have studied the contributions of the peripheral and central nervous systems during the development of osteoarthritis (OA) pain. Male Sprague-Dawley rats received unilateral intra-articular injections of monosodium iodoacetate (MIA 1 mg) or saline, and weight-bearing (WB) asymmetry and distal allodynia measured. Subgroups of rats received intra-articular injections of, QX-314 (membrane impermeable local anaesthetic) + capsaicin, QX-314, capsaicin or vehicle on days 7, 14 or 28 post-MIA and WB and PWT remeasured...
May 8, 2018: Scientific Reports
https://www.readbyqxmd.com/read/29734749/synthesis-and-structure-activity-relationships-of-cis-n-normetazocine-based-lp1-derivatives
#11
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
#12
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/29725582/circulating-thyrotropin-is-upregulated-by-estradiol
#13
Salvatore Benvenga, Flavia Di Bari, Roberta Granese, Irene Borrielli, Grazia Giorgianni, Loredana Grasso, Maria Le Donne, Roberto Vita, Alessandro Antonelli
After encountering two women with serum thyrotropin (TSH) levels greater in periovulatory phase than in other days of the menstrual cycle, we hypothesized that TSH levels could be sensitive to changes in circulating estrogens in women. The objective of this study was to evaluate whether serum TSH increases after an induced acute increase of serum estradiol, and compare serum TSH increase with that of prolactin (PRL) which is a classic estradiol-upregulated pituitary hormone. In this retrospective study, we resorted to stored frozen sera from 55 women who had undergone the GnRH agonist (buserelin)-acute stimulation test of ovarian steroidogenesis...
March 2018: Journal of Clinical & Translational Endocrinology
https://www.readbyqxmd.com/read/29708942/a-bifunctional-biased-mu-opioid-agonist-neuropeptide-ff-receptor-antagonist-as-analgesic-with-improved-acute-and-chronic-side-effects
#14
Armand Drieu la Rochelle, Karel Guillemyn, Maria Dumitrascuta, Charlotte Martin, Valérie Utard, Raphaëlle Quillet, Séverine Schneider, François Daubeuf, Tom Willemse, Pieter Mampuys, Bert U W Maes, Nelly Frossard, Frédéric Bihel, Mariana Spetea, Frédéric Simonin, Steven Ballet
Opioid analgesics, such as morphine, oxycodone and fentanyl, are the cornerstones for treating moderate to severe pain. However, upon chronic administration, their efficiency is limited by prominent side effects such as analgesic tolerance and dependence liability. Neuropeptide FF (NPFF) and its receptors (NPFF1R and NPFF2R) are recognized as an important pronociceptive system involved in opioid-induced hyperalgesia and analgesic tolerance. Herein, we report the design of multitarget peptidomimetic compounds that show high affinity binding to the mu opioid receptor (MOPr) and NPFFRs...
April 26, 2018: Pain
https://www.readbyqxmd.com/read/29684591/in-vitro-and-in-vivo-activity-of-cyclopeptide-dmt-c-d-lys-phe-asp-nh-2-a-mu-opioid-receptor-agonist-biased-toward-%C3%AE-arrestin
#15
Katarzyna Gach-Janczak, Justyna Piekielna-Ciesielska, Anna Adamska-Bartłomiejczyk, Karol Wtorek, Federica Ferrari, Girolamo Calo', Agata Szymaszkiewicz, Joanna Piasecka-Zelga, Anna Janecka
Morphine and related drugs, which are the most effective analgesics for the relief of severe pain, act through activating opioid receptors. The endogenous ligands of these receptors are opioid peptides which cannot be used as antinociceptive agents due to their low bioactivity and stability in biological fluids. The major goal of opioid research is to understand the mechanism of action of opioid receptor agonists in order to improve therapeutic utility of opioids. Analgesic effects of morphine are mediated mostly through activation of the mu opioid receptor...
July 2018: Peptides
https://www.readbyqxmd.com/read/29677442/synthesis-and-pharmacological-evaluation-of-novel-c-8-substituted-tetrahydroquinolines-as-balanced-affinity-mu-delta-opioid-ligands-for-the-treatment-of-pain
#16
Anthony F Nastase, Nicholas W Griggs, Jessica P Anand, Thomas J Fernandez, Aubrie A Harland, Tyler J Trask, Emily M Jutkiewicz, John R Traynor, Henry I Mosberg
The use of opioids for the treatment of pain, while largely effective, is limited by detrimental side effects including analgesic tolerance, physical dependence, and euphoria, which may lead to opioid abuse. Studies have shown that compounds with a μ-opioid receptor (MOR) agonist/δ-opioid receptor (DOR) antagonist profile reduce or eliminate some of these side effects including the development of tolerance and dependence. Herein we report the synthesis and pharmacological evaluation of a series of tetrahydroquinoline-based peptidomimetics with substitutions at the C-8 position...
May 2, 2018: ACS Chemical Neuroscience
https://www.readbyqxmd.com/read/29677019/mu-opioid-receptors-in-nociceptive-afferents-produce-a-sustained-suppression-of-hyperalgesia-in-chronic-pain
#17
Amie Severino, Wenling Chen, Joshua K Hakimian, Brigitte L Kieffer, Claire Gaveriaux-Ruff, Wendy Walwyn, Juan Carlos Marvizon
The latent sensitization model of chronic pain reveals that recovery from some types of long-term hyperalgesia is an altered state in which nociceptive sensitization persists but is suppressed by the ongoing activity of analgesic receptors such as µ-opioid receptors (MORs). To determine whether these MORs are the ones present in nociceptive afferents, we bred mice expressing Cre-recombinase under the Nav1.8 channel promoter (Nav1.8cre) with MOR-floxed mice (flMOR). These Nav1.8cre/flMOR mice had reduced MOR expression in primary afferents, as revealed by quantitative PCR, in situ hybridization and immunofluorescence colocalization with the neuropeptide CGRP...
April 17, 2018: Pain
https://www.readbyqxmd.com/read/29673620/effects-of-opioid-and-non-opioid-analgesics-on-responses-to-psychosocial-stress-in-humans
#18
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 24, 2018: Hormones and Behavior
https://www.readbyqxmd.com/read/29663822/the-effect-of-intrathecal-sufentanil-preconditioning-against-myocardial-ischemia-reperfusion-injury
#19
Y Tire, G Sarkilar, H Esen, R Onoglu, S T Uzun
OBJECTIVES: We aimed to investigate the cardioprotective effect and hemodynamic response of intrathecally administered sufentanil on myocardial IR injury. BACKGROUND: Sufentanil, mu opioid receptor agonist, intravenously administered during clinical and experimental studies, has been shown to have a cardioprotective effect on myocardial ischemia-reperfusion injury. METHODS: Thirty-two New Zealand type rabbits, which were anesthetized, were divided into four equal groups: sham, ischemia-reperfusion, sufentanil and ischemia-reperfusion+sufentanil...
2018: Bratislavské Lekárske Listy
https://www.readbyqxmd.com/read/29626639/assessing-the-real-time-activation-of-the-cannabinoid-cb1-receptor-and-the-associated-structural-changes-using-a-fret-biosensor
#20
Ying Liu, Lu-Yao Chen, Hong Zeng, Richard Ward, Nan Wu, Li Ma, Xi Mu, Qiu-Lan Li, Yang Yang, Su An, Xiao-Xi Guo, Qian Hao, Tian-Rui Xu
The cannabinoid receptor 1 (CB1) is mainly expressed in the nervous system and regulates learning, memory processes, pain and energy metabolism. However, there is no way to directly measure its activation. In this study, we constructed a CB1 intramolecular fluorescence resonance energy transfer (FRET) sensor, which could measure CB1 activation by monitoring structural changes between the third intracellular loop and the C-terminal tail. CB1 agonists induced a time- and concentration-dependent increase in the FRET signal, corresponding to a reduction in the distance between the third intracellular loop and the C-terminal tail...
June 2018: International Journal of Biochemistry & Cell Biology
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