Global ETD Search
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Showing 1 to 17 of 17 for “"Rimonabant"”.
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Discriminative stimulus properties of 3-substituent rimonabant analogs
… investigating analogs of the CB1 antagonist rimonabant revealed that certain alterations in the 3-substituent of rimonabant’s pyrazole core conferred agonist-like properties in the tetrad. Interestingly, these effects were present in CB1 -/- mice, and were not reversed by rimonabant in …
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Characterization of Rimonabant effects on G protein activity
… The first selective and potent CB1 antagonist Rimonabant (also known SR141716A, SR) at high micromolar concentrations behaves as an inverse agonist, i.e. decreases [35S]GTPγS binding in rodent and human cerebral cortex and in Chinese hamster ovary (CHO) cells transfected with CB1 receptors …
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Systemic Blockade of the Endocannabinoid System Alters Gene Expression and acquisition of a Hippocampus Dependent Learning Task
… and memory (Sullivan, 2000). The ability of rimonabant to reverse memory deficits induced by cannabinoid agonists lead to the hypothesis that administering it alone could induce learning and memory enhancements (Brodkin and Moerschbaecher, 1997). Rimonabant-induced memory enhancements may be …
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Cardiovascular risk reduction in insulin resistant states
… open labelled parallel study of metformin and rimonabant in obese patients with PCOS. Subsquently, an extension to this study was undertaken where patients who were on rimonabant were changed over to metformin, whereas those on metformin were continued on metformin for another 3 months. As part …
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A COMPARISION OF DELTA-9-TETRAHYDROCANNABINOL DEPENDENCE IN C57Bl/6j MICE AND FATTY ACID AMIDE HYDROLASE KNOCK OUT MICE
… and challenged with the CB1 receptor antagonist, rimonabant, to precipitate withdrawal. Following subchronic THC treatment, rimonabant precipitated a significant increase in paw flutters that was dependent on THC dose. However, FAAH-/- mice displayed a similar magnitude of withdrawal responses as …
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Ultra-Low Dose Antagonist Effects on Cannabinoids and Opioids in Models of Pain: Is Less More?
… ultra-low doses of the CB1 receptor antagonist rimonabant (SR 141716), or a combination of WIN and ultra-low dose rimonabant. Following the chronic experiment, striatal tissue was rapidly extracted and subjected to co-immunoprecipitation to analyse CB1 receptor coupling to G-protein subtypes. …
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Die Wirkung von Cannabinoiden auf das Herz-Kreislauf-System und die Atmung von Ratten
… Der CB1-Cannabinoidrezeptor-Antagonist Rimonabant hob alle respiratorischen und kardiovaskulären Wirkungen von WIN55212-2 auf. Die Wirkungen von WIN55212-2 wurden auch mit den Wirkungen des Opioidrezeptor-Agonisten DAMGO verglichen. Intracisternale Applikation von DAMGO verminderte die …
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Design, Synthesis and Biological Evaluation of Novel Cannabinoid Antagonist
… antagonist/inverse agonist SR141716 (Rimonabant) that was presumed to interact with a unique region in the CB1 receptors. Based on our preliminary results we identified a novel series of 1,2,3-triazole ester and keto derivatives as lead compounds for biological evaluation. Here in …
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Endocannabinoid Modulation of Spatial Memory in Aversively and Appetitively Motivated Barnes Maze Tasks
… Administration of the CB1 receptor antagonist, rimonabant, disrupted extinction learning under aversive conditions, but not under appetitive conditions. This is the first study to show a differential effect of rimonabant on extinction in a task that required identical motor behaviors, but only …
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Synthesis of fluorinated cannabinoid derivatives; Towards PET radiotracers for imaging the cannabinoid receptor
… mice were injected with the CB1R antagonist rimonabant (1 mg/kg) prior to administration of the radiotracer. In animals treated with rimonabant, radiotracer uptake in specific areas of the brain was reduced demonstrating CB1R-selective binding. This study underscores the dual utility of these …
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A Systematic Investigation of Whether Cannabinoids and Opioids Interact in the Nucleus Accumbens Shell to Differentially Impact Feeding Patterns on a Palatable Diet
… naltrexone and the CB1 receptor antagonist rimonabant blocked DAMGO-induced feeding. Taken together, these results imply that the nucleus accumbens shell may be one neural location of the observed synergistic effects of the opioid and cannabinoid systems on feeding.
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Investigating adipose tissue angiogenesis in obesity reveals a novel role for thrombospondin-1.
… 2007, the Scottish Medicines Consortium removed Rimonabant from use in the NHS Scotland due to risks of adverse psychiatric events (Burch et al., 2009). However, despite these setbacks, there have been considerable advancements in the treatment of obesity, achieved by combining pharmacological …
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Protein-ligand interaction studies and identification of new drug-like hits as cannabinoid receptor modulators
… or null psychiatric side effects compared to rimonabant. Chapter 4 focuses on the identification and characterization of CB2 allosteric site(s). Using known CB2 negative AMs, the binding energy of representative complexes after molecular dynamics studies validated the binding poses of AMs. …
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Cannabinoid Modulation of Reinforcement Maintained by Stimulation of the Medial Forebrain Bundle in C57Bl/6J Mice
… blocked by pre-treatment with the CB1 antagonist rimonabant, but not with the CB2 antagonist SR144528. PF-3845 also reduced ICSS, but did so independent of CB1 and CB2 receptors, and only with one dose (30.0 mg/kg) that has not been assessed previously in vivo. We showed that ICSS was more …
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The Role of MAGL Inhibition in Nicotine Withdrawal and Reward
… signs in mice. These effects were blocked by rimonabant indicating a CB1 receptor mechanism. Furthermore, repeated administration of JZL184 for 6 days did not produce tolerance to the alleviation of withdrawal and the treatment did not induce alterations in CB1 receptor levels or …
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One Size Does Not Fit All: A Qualitative Study Exploring Unlicensed Weight Loss Drug Use In Women
… of 2,4 dinitrophenol (DNP), sibutramine and rimonabant are just one method used in enhancing and improving the body in line with social expectations. However, previous research exploring the use of these drugs has been confined to male dominated bodybuilding communities, despite women …
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Possibile ruolo del sistema endocannabinoide nel disturbo d’alimentazione incontrollata (binge eating disorder): studi comportamentali, farmacologici e biochimici
… by CB1 receptors inverse agonist/antagonist rimonabant, was able to alter this behavior when given chronically. As regards the CB1 receptor density, no difference has been highlighted between animals showing binge eating behavior and control group. In conclusion, negative modulation of the …