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https://www.readbyqxmd.com/read/27913257/prodynorphin-and-kappa-opioid-receptor-mrna-expression-in-the-brain-relates-to-social-status-and-behavior-in-male-european-starlings
#1
Lauren V Riters, Melissa A Cordes, Sharon A Stevenson
Numerous animal species display behavioral changes in response to changes in social status or territory possession. For example, in male European starlings only males that acquire nesting sites display high rates of sexual and agonistic behavior. Past studies show that mu and delta opioid receptors regulate behaviors associated with social ascension or defeat. Opioids also act at kappa receptors, with dynorphin binding with the highest affinity; however, the role of these opioids in social behavior has not been well studied...
November 29, 2016: Behavioural Brain Research
https://www.readbyqxmd.com/read/27903642/behavioral-characterization-of-kappa-opioid-receptor-agonist-spiradoline-and-cannabinoid-receptor-agonist-cp55940-mixtures-in-rats
#2
Vanessa Minervini, Sujata S Dahal, Charles France
Pain is a significant clinical problem and there is a need for more effective treatments with reduced adverse effects that currently limit the use of mu opioid receptor agonists. Synthetic kappa opioid receptor agonists have no abuse liability and well-documented antinociceptive effects; however, adverse effects (diuresis, dysphoria) preclude their use in the clinic. Combining kappa opioids with non-opioid drugs (cannabinoid receptor agonists) allows for smaller doses of each drug to produce antinociception...
November 30, 2016: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/27899885/interacting-cannabinoid-and-opioid-receptors-in-the-nucleus-accumbens-core-control-adolescent-social-play
#3
Antonia Manduca, Olivier Lassalle, Marja Sepers, Patrizia Campolongo, Vincenzo Cuomo, Giovanni Marsicano, Brigitte Kieffer, Louk J M J Vanderschuren, Viviana Trezza, Olivier J J Manzoni
Social play behavior is a highly rewarding, developmentally important form of social interaction in young mammals. However, its neurobiological underpinnings remain incompletely understood. Previous work has suggested that opioid and endocannabinoid neurotransmission interact in the modulation of social play. Therefore, we combined behavioral, pharmacological, electrophysiological, and genetic approaches to elucidate the role of the endocannabinoid 2-arachidonoylglycerol (2-AG) in social play, and how cannabinoid and opioid neurotransmission interact to control social behavior in adolescent rodents...
2016: Frontiers in Behavioral Neuroscience
https://www.readbyqxmd.com/read/27876117/neonatal-abstinence-syndrome-and-the-gastrointestinal-tract
#4
Denise Maguire, Maureen Gröer
Development of a healthy gut microbiome is essential in newborns to establish immunity and protection from pathogens. Recent studies suggest that infants who develop dysbiosis may be at risk for lifelong adverse health consequences. Exposure to opioid drugs during pregnancy is a factor of potential importance for microbiome health that has not yet been investigated. Since these infants are born after an entire gestation exposed to mu opioid receptor agonists and have severe gastrointestinal and neurological symptoms, we hypothesize that these infants are at risk for dysbiosis...
December 2016: Medical Hypotheses
https://www.readbyqxmd.com/read/27867511/is-tapentadol-different-from-classical-opioids-a-review-of-the-evidence
#5
Richard M Langford, Roger Knaggs, Paul Farquhar-Smith, Anthony H Dickenson
Tapentadol is a single molecule able to deliver analgesia by two distinct mechanisms, a feature which differentiates it from many other analgesics. Pre-clinical data demonstrate two mechanisms of action: mu-opioid receptor agonist activity and noradrenaline re-uptake inhibition. From these, one may predict that tapentadol would be applicable across a broad spectrum of pain from nociceptive to neuropathic. The evidence in animal models suggests that norepinephrine re-uptake inhibition (NRI) is a key mechanism and may even predominate over opioid actions in chronic (and especially neuropathic) pain states, reinforcing that tapentadol is different to classical opioids and may, therefore, be an a priori choice for the treatment of neuropathic and mixed pain...
November 2016: British Journal of Pain
https://www.readbyqxmd.com/read/27857679/bold-imaging-in-awake-wild-type-and-mu-opioid-receptor-knock-out-mice-reveals-on-target-activation-maps-in-response-to-oxycodone
#6
Kelsey Moore, Dan Madularu, Sade Iriah, Jason R Yee, Praveen Kulkarni, Emmanuel Darcq, Brigitte L Kieffer, Craig F Ferris
Blood oxygen level dependent (BOLD) imaging in awake mice was used to identify differences in brain activity between wild-type, and Mu (μ) opioid receptor knock-outs (MuKO) in response to oxycodone (OXY). Using a segmented, annotated MRI mouse atlas and computational analysis, patterns of integrated positive and negative BOLD activity were identified across 122 brain areas. The pattern of positive BOLD showed enhanced activation across the brain in WT mice within 15 min of intraperitoneal administration of 2...
2016: Frontiers in Neuroscience
https://www.readbyqxmd.com/read/27842940/nalmefene-for-the-management-of-alcohol-dependence-review-on-its-pharmacology-mechanism-of-action-and-meta-analysis-on-its-clinical-efficacy
#7
Karl Mann, Lars Torup, Per Sørensen, Antoni Gual, Robert Swift, Brendan Walker, Wim van den Brink
Nalmefene, a mu- and delta-opioid receptor (MOR, DOR) antagonist and a partial kappa-opioid receptor (KOR) agonist, is approved in the European Union and other countries for the reduction of alcohol consumption in alcohol dependent patients with a high drinking risk level according to WHO ("target population"). This review presents an overview of nalmefene׳s pharmacology, its mechanisms of action and a meta-analysis on its efficacy in reducing alcohol consumption. The review was based on a systematic search of the literature...
December 2016: European Neuropsychopharmacology: the Journal of the European College of Neuropsychopharmacology
https://www.readbyqxmd.com/read/27825896/activation-of-mu-opioid-receptors-in-the-ventral-pallidum-decreases-the-negative-hedonic-evaluation-of-a-conditioned-aversive-taste-in-rats
#8
Tadashi Inui, Tsuyoshi Shimura
Conditioned taste aversion (CTA) causes a shift in the hedonic evaluation of a conditioned stimulus (CS) from positive to negative, and reduces the CS intake. Mu-opioid receptors (MORs) in the ventral pallidum (VP) are known to be involved in the hedonic evaluation of positive rewarding stimuli; however, their involvement in evaluation of a negative aversive stimulus is still unclear. To explore the neural mechanisms of the negative hedonic evaluation of the CS in CTA, we examined the effects of the activation of VP MORs on the behavioral responses of rats to a CS...
November 5, 2016: Behavioural Brain Research
https://www.readbyqxmd.com/read/27824891/exploring-flexibility-of-progesterone-receptor-ligand-binding-domain-using-molecular-dynamics
#9
Liangzhen Zheng, Valerie Chunling Lin, Yuguang Mu
Progesterone receptor (PR), a member of nuclear receptor (NR) superfamily, plays a vital role for female reproductive tissue development, differentiation and maintenance. PR ligand, such as progesterone, induces conformation changes in PR ligand binding domain (LBD), thus mediates subsequent gene regulation cascades. PR LBD may adopt different conformations upon an agonist or an antagonist binding. These different conformations would trigger distinct transcription events. Therefore, the dynamics of PR LBD would be of general interest to biologists for a deep understanding of its structure-function relationship...
2016: PloS One
https://www.readbyqxmd.com/read/27818236/a-role-for-the-mu-opioid-receptor-in-the-antidepressant-effects-of-buprenorphine
#10
Shivon A Robinson, Rebecca L Erickson, Caroline A Browne, Irwin Lucki
Buprenorphine (BPN), a mixed opioid drug with high affinity for mu (MOR) and kappa (KOR) opioid receptors, has been shown to produce behavioral responses in rodents that are similar to those of antidepressant and anxiolytic drugs. Although recent studies have identified KORs as a primary mediator of BPN's effects in rodent models of depressive-like behavior, the role of MORs in BPN's behavioral effects has not been as well explored. The current studies investigated the role of MORs in mediating conditioned approach behavior in the novelty-induced hypophagia (NIH) test, a behavioral measure previously shown to be sensitive to chronic treatment with antidepressant drugs...
November 3, 2016: Behavioural Brain Research
https://www.readbyqxmd.com/read/27743985/mu-opioid-receptor-inhibition-decreases-voluntary-wheel-running-in-a-dopamine-dependent-manner-in-rats-bred-for-high-voluntary-running
#11
Gregory N Ruegsegger, Jacob D Brown, M Cathleen Kovarik, Dennis K Miller, Frank W Booth
The mesolimbic dopamine and opioid systems are postulated to influence the central control of physical activity motivation. We utilized selectively bred rats for high (HVR) or low (LVR) voluntary running behavior to examine (1) inherent differences in mu-opioid receptor (Oprm1) expression and function in the nucleus accumbens (NAc), (2) if dopamine-related mRNAs, wheel-running, and food intake are differently influenced by intraperitoneal (i.p.) naltrexone injection in HVR and LVR rats, and (3) if dopamine is required for naltrexone-induced changes in running and feeding behavior in HVR rats...
December 17, 2016: Neuroscience
https://www.readbyqxmd.com/read/27743812/mu-opioid-receptors-in-the-caudomedial-nts-are-critical-for-respiratory-responses-to-stimulation-of-bronchopulmonary-c-fibers-and-carotid-body-in-conscious-rats
#12
Jianguo Zhuang, Xiuping Gao, Franklin Gao, Fadi Xu
We tested the hypothesis that mu-opioid receptors (MORs) in the caudomedial nucleus tractus solitarius (cmNTS) are important for the ventilatory responses to stimulation of bronchopulmonary C-fibers (PCFs), the carotid body-mediated hypoxia, and hypercapnia independent of the carotid body. First, we used immunohistochemistry to map MORs distribution in the caudal medulla. Then we compared the effects of intra-cmNTS microinjection of DAMGO (a MOR agonist) with or without a combination of CTAP (a MOR antagonist) on the ventilatory responses to: 1) right atrial injection of capsaicin (to stimulation of PCFs) and 2) acute hypoxia (HVR, to stimulate the carotid body) in awake intact rats; and 3) hypercapnia (HCVR) in the carotid body ablated rats...
January 2017: Respiratory Physiology & Neurobiology
https://www.readbyqxmd.com/read/27736284/continuous-perioperative-sublingual-buprenorphine
#13
Marcelina Jasmine Silva, Andrea Rubinstein
Buprenorphine, a semisynthetic thebaine derivative, is a unique opioid, as it has activity at multiple receptors, including mu (partial agonist), kappa (antagonist), OLR-1 (agonist), and delta (antagonist). Because buprenorphine's pharmacology is relatively complex, misconceptions about its actions are common. Most other opioids act solely or predominately as full mu receptor agonists. Common practice at many institutions calls for the cessation of regular buprenorphine use 48-72 hours prior to surgery. This practice is based on three foundational theories that have come from scant data about the properties of buprenorphine: (1) that buprenorphine is only a partial mu agonist and therefore is not a potent analgesic; (2) because buprenorphine has a ceiling effect on respiratory depression, it also has a ceiling effect on analgesia; and (3) that buprenorphine acts as a "blockade" to the analgesic effects of other opiates when coadministered due to its strong binding affinity...
October 13, 2016: Journal of Pain & Palliative Care Pharmacotherapy
https://www.readbyqxmd.com/read/27725218/opioid-subtype-and-cell-type-dependent-regulation-of-inhibitory-synaptic-transmission-in-the-rat-insular-cortex
#14
Eiko Yokota, Yuko Koyanagi, Kiyofumi Yamamoto, Yoshiyuki Oi, Noriaki Koshikawa, Masayuki Kobayashi
The insular cortex (IC) plays a principal role in the regulation of pain processing. Although opioidergic agonists depress cortical excitatory synaptic transmission, little is known about opioidergic roles in inhibitory synaptic transmission. In the IC, the opioid receptors differentially regulate the excitatory propagation: agonists of the mu (MOR), delta (DOR), and kappa (KOR) exhibit suppressive, facilitative, and little effects, respectively. Thus, we aimed to examine the effects of opioid receptor agonists on unitary inhibitory postsynaptic currents (uIPSCs) in the IC...
December 17, 2016: Neuroscience
https://www.readbyqxmd.com/read/27707973/t394a-mutation-at-the-%C3%AE-opioid-receptor-blocks-opioid-tolerance-and-increases-vulnerability-to-heroin-self-administration-in-mice
#15
Xiao-Fei Wang, Elisabeth Barbier, Yi-Ting Chiu, Yi He, Jia Zhan, Guo-Hua Bi, Hai-Ying Zhang, Bo Feng, Lee-Yuan Liu-Chen, Jia Bei Wang, Zheng-Xiong Xi
: The etiology and pathophysiology underlying opioid tolerance and dependence are still unknown. Because mu opioid receptor (MOR) plays an essential role in opioid action, many vulnerability-related studies have focused on single nucleotide polymorphisms of MOR, particularly on A118G. In this study, we found that a single-point mutation at the MOR T394 phosphorylation site could be another important susceptive factor in the development of opioid tolerance and dependence in mice. T394A mutation, in which a threonine at 394 was replaced by an alanine, did not alter agonist binding to MOR and opioid analgesia, but resulted in loss of etorphine-induced MOR internalization in spinal dorsal horn neurons and opioid analgesic tolerance induced by either morphine or etorphine...
October 5, 2016: Journal of Neuroscience: the Official Journal of the Society for Neuroscience
https://www.readbyqxmd.com/read/27660244/constitutive-desensitization-of-opioid-receptors-in-peripheral-sensory-neurons
#16
Laura C Sullivan, Teresa S Chavera, Raehannah J Jamshidi, Kelly A Berg, William P Clarke
Opioid receptors expressed by peripheral pain-sensing neurons are functionally inactive for antinociceptive signaling under most basal conditions; however, tissue damage or exposure to inflammatory mediators (e.g., bradykinin) converts these receptors from a nonresponsive state to a functionally competent state. Here we tested the hypothesis that the basal, nonresponsive state of the mu- and delta-opioid receptors (MOR and DOR, respectively) is the result of constitutive receptor activity that activates desensitization mechanisms, resulting in MOR and DOR receptor systems that are constitutively desensitized...
December 2016: Journal of Pharmacology and Experimental Therapeutics
https://www.readbyqxmd.com/read/27639959/decreased-cb-receptor-binding-and-cannabinoid-signaling-in-three-brain-regions-of-a-rat-model-of-schizophrenia
#17
Edina Szűcs, Szabolcs Dvorácskó, Csaba Tömböly, Alexandra Büki, Gabriella Kékesi, Gyöngyi Horváth, Sándor Benyhe
Schizophrenia is a serious mental health disorder characterized by several behavioral and biochemicel abnormalities. In a previous study we have shown that mu-opioid (MOP) receptor signaling is impaired in specific brain regions of our three-hit animal model of schizophrenia. Since the cannabinoid system is significantly influenced in schizophrenic patients, in the present work we investigated cannabinoid (CB) receptor binding and G-protein activation in cortical, subcortical and cerebellar regions of control and 'schizophrenic' rats...
October 28, 2016: Neuroscience Letters
https://www.readbyqxmd.com/read/27639082/exenatide-improves-both-hepatic-and-adipose-tissue-insulin-resistance-a-dynamic-pet-study
#18
Amalia Gastaldelli, Melania Gaggini, Giuseppe Daniele, Demetrio Ciociaro, Eugenio Cersosimo, Devjit Tripathy, Curtis Triplitt, Peter Fox, Nicolas Musi, Ralph DeFronzo, Patricia Iozzo
: GLP-1 receptor agonists (GLP-1-RAs) act on multiple tissues, in addition to the pancreas. Recent studies suggest that GLP-1-RAs act on liver and adipose tissue to reduce insulin resistance (IR). Thus, we evaluated the acute effects of exenatide (EX) on hepatic (Hep-IR) and adipose (Adipo-IR) insulin resistance and glucose uptake. 15 male subjects (age=56±8 y, BMI=29±1 kg/m(2) , A1c=5.7±0.1%) were studied on two occasions, with a double blind subcutaneous injection of exenatide (5 mcg) or placebo (PLC) 30 min before a 75-gram oral glucose tolerance test (OGTT)...
September 17, 2016: Hepatology: Official Journal of the American Association for the Study of Liver Diseases
https://www.readbyqxmd.com/read/27637375/antinociceptive-effects-of-the-6-o-sulfate-ester-of-morphine-in-normal-and-diabetic-rats-comparative-role-of-mu-and-delta-opioid-receptors
#19
Jai Shankar K Yadlapalli, Benjamin M Ford, Amit Ketkar, Anqi Wan, Narasimha R Penthala, Robert L Eoff, Paul L Prather, Maxim Dobretsov, Peter A Crooks
: This study determined the antinociceptive effects of morphine and morphine-6-O-sulfate (M6S) in both normal and diabetic rats, and evaluated the comparative role of mu-opioid receptors (mu-ORs) and delta-opioid receptors (delta-ORs) in the antinociceptive action of these opioids. In vitro characterization of mu-OR and delta-OR-mediated signaling by M6S and morphine in stably transfected Chinese hamster ovary (CHO-K1) cells showed that M6S exhibited a 6-fold higher affinity for delta-ORs and modulated G-protein and adenylyl cyclase activity via delta-ORs more potently than morphine...
November 2016: Pharmacological Research: the Official Journal of the Italian Pharmacological Society
https://www.readbyqxmd.com/read/27605628/long-term-reduction-of-kappa-opioid-receptor-function-by-the-biased-ligand-norbinaltorphimine-requires-c-jun-n-terminal-kinase-activity-and-new-protein-synthesis-in-peripheral-sensory-neurons
#20
Raehannah J Jamshidi, Laura C Sullivan, Blaine A Jacobs, Teresa A Chavera, Kelly A Berg, William P Clarke
A single administration of the κ opioid receptor (KOR) antagonist, norbinaltorphimine (norBNI), produces long-term reduction in KOR function in heterologous expression systems and brain that is mediated by activation of c-Jun N-terminal kinase (JNK). In this study, we examined the long-term effects of norBNI on adult rat peripheral sensory neurons in vivo and ex vivo. Following a single intraplantar (i.pl.) injection of norBNI into the hind paw, peripheral KOR-mediated antinociception in the ipsilateral, but not the contralateral, hindpaw was abolished for at least 9 days...
November 2016: Journal of Pharmacology and Experimental Therapeutics
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