Bibliografias temáticas / Receptors; Irreversible antagonist; Drug abuse

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Literatura científica selecionada sobre o tema "Receptors; Irreversible antagonist; Drug abuse"

Autor: Grafiati

Publicado: 4 de junho de 2021

Última modificação: 6 de fevereiro de 2022

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Artigos de revistas sobre o assunto "Receptors; Irreversible antagonist; Drug abuse"

Burroughs, SF, and GJ Johnson. "Beta-lactam antibiotic-induced platelet dysfunction: evidence for irreversible inhibition of platelet activation in vitro and in vivo after prolonged exposure to penicillin." Blood 75, no. 7 (1990): 1473–80. http://dx.doi.org/10.1182/blood.v75.7.1473.1473.

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Abstract beta-Lactam antibiotics cause platelet dysfunction with bleeding complications. Previous in vitro studies documented reversible inhibition of agonist-receptor interaction. This mechanism is inadequate to explain the effect of beta-lactam antibiotics in vivo. Platelet function does not return to normal immediately after drug treatment, implying irreversible inhibition of platelet function. We report here evidence of irreversible platelet functional and biochemical abnormalities after in vitro and in vivo exposure to beta-lactam antibiotics. Irreversible binding of [14C]-penicillin (Pen

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beta-Lactam antibiotics cause platelet dysfunction with bleeding complications. Previous in vitro studies documented reversible inhibition of agonist-receptor interaction. This mechanism is inadequate to explain the effect of beta-lactam antibiotics in vivo. Platelet function does not return to normal immediately after drug treatment, implying irreversible inhibition of platelet function. We report here evidence of irreversible platelet functional and biochemical abnormalities after in vitro and in vivo exposure to beta-lactam antibiotics. Irreversible binding of [14C]-penicillin (Pen) occurre

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Vieira-Coelho, M., J. Azevedo, and M. Esteves. "New Potential Molecular Targets for Cannabis Addition." European Psychiatry 24, S1 (2009): 1. http://dx.doi.org/10.1016/s0924-9338(09)70703-5.

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Cannabis is considerer the most widely abused illicit drug in the world. The recent rising prevalence of cannabis use by young adults and increasing evidence of adverse health effects makes the search for new pharmacotherapy to reduce cannabis abuse extremely important. To date no medication has been approved for the treatment of cannabis addition.This study reviews recent results with potential interest for future pharmacological treatment of Cannabis dependence. Most of the relevant data obtained for treatment of cannabis dependence target the endocannabinoid or the central cholinergic syste

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Althobaiti, Yusuf S. "Quetiapine-Induced Place Preference in Mice: Possible Dopaminergic Pathway." Pharmaceuticals 14, no. 2 (2021): 156. http://dx.doi.org/10.3390/ph14020156.

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Quetiapine, an atypical antipsychotic, is effective in the management of schizophrenia, depression, and anxiety. Although quetiapine overdosage and misuse have been reported, its abuse potential has not been investigated in animals. In this study, the abuse potential of quetiapine was assessed based on the conditioned place preference (CPP) paradigm of drug addiction in a mouse model. First, mice received intraperitoneal injections of quetiapine (40, 80, or 120 mg/kg) every other day during the conditioning phase. In the second experiment, mice were pretreated with 0.03 mg/kg SKF-35866, a D1 r

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Lebedev, Andrei Andreevich, Eugeny Grigorievich Shumilov, Eugeny Rudolfovich Bychkov, Vitaly Ivanovich Morozov, and Petr Dmitriyevich Shabanov. "Orexin A role in mechanisms of reinforcement in the bed nucleus of stria terminalis." Reviews on Clinical Pharmacology and Drug Therapy 13, no. 2 (2015): 20–26. http://dx.doi.org/10.17816/rcf13220-26.

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The orexin family of hypothalamic neuropeptides has been implicated in reinforcement mechanisms relevant to both food and drug reward. Previous behavioral studies with antagonists at the orexin A-selective receptor OX(1), have demonstrated its involvement in behavioral sensitization, conditioned place-preference, self-administration and reinstatement of drugs abuse. There are dense concentrations of hypocretin receptors, in brain regions implicated in drug reinforcement processes, such as the nucleus accumbens, ventral tegmental area and bed nucleus of the stria terminalis Adult male Wistar ra

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Davis, Corey, Damika Webb, and Scott Burris. "Changing Law from Barrier to Facilitator of Opioid Overdose Prevention." Journal of Law, Medicine & Ethics 41, S1 (2013): 33–36. http://dx.doi.org/10.1111/jlme.12035.

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Drug overdose has recently surpassed motor vehicle accidents to become the leading cause of unintentional injury death in the United States. The epidemic is largely driven by opioids such as oxycodone, hydrocodone, and methadone, which kill more Americans than heroin and cocaine combined. The demographics of overdose have changed over the past few decades as well: according to the latest data, the average overdose victim is now a non-Hispanic white man aged 45-54.These deaths — over 16,000 per year — are almost entirely preventable. Opioid overdose kills by slowly depressing respiration, a pro

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Altarifi, Ahmad A., Megan J. Moerke, Mohammad I. Alsalem, and S. Stevens Negus. "Preclinical assessment of tramadol abuse potential: Effects of acute and repeated tramadol on intracranial self-stimulation in rats." Journal of Psychopharmacology 34, no. 11 (2020): 1316–25. http://dx.doi.org/10.1177/0269881120944153.

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Background: Tramadol is a widely used analgesic that activates mu-opioid receptors (MOR) and inhibits serotonin and norepinephrine transporters. This mixed pharmacology may limit both its own abuse potential and its modulation of abuse potential of other MOR agonists. Aims: This study used an intracranial self-stimulation (ICSS) procedure to compare abuse-related effects produced by acute or repeated treatment with tramadol or morphine in rats. Abuse potential in ICSS procedures is indicated by a drug-induced increase (or ‘facilitation’) of ICSS responding. Methods: Adult male Sprague–Dawley r

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Marszalek-Grabska, Marta, Kinga Gawel, Dariusz Matosiuk, Ewa Gibula-Tarlowska, Joanna Listos, and Jolanta H. Kotlinska. "Effects of the Positive Allosteric Modulator of Metabotropic Glutamate Receptor 5, VU-29, on Maintenance Association between Environmental Cues and Rewarding Properties of Ethanol in Rats." Biomolecules 10, no. 5 (2020): 793. http://dx.doi.org/10.3390/biom10050793.

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Metabotropic glutamate subtype 5 (mGlu5) receptors are implicated in various forms of synaptic plasticity, including drugs of abuse. In drug-addicted individuals, associative memories can drive relapse to drug use. The present study investigated the potential of the mGlu5 receptor positive allosteric modulator (PAM), VU-29 (30 mg/kg, i.p.), to inhibit the maintenance of a learned association between ethanol and environmental context by using conditioned place preference (CPP) in rats. The ethanol-CPP was established by the administration of ethanol (1.0 g/kg, i.p. ×10 days) using an unbiased p

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Helm II, Standiford. "Opioid Antagonists, Partial Agonists, and Agonists/Antagonists: The Role of OfficeBased Detoxification." Pain Physician 2;11, no. 3;2 (2008): 225–35. http://dx.doi.org/10.36076/ppj.2008/11/225.

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Background: The opioid receptor antagonists naloxone and naltrexone are competitive antagonists at the mu, kappa, and sigma receptors with a higher affinity for the mu receptor and lacking any mu receptor efficacy. Buprenorphine is classified as a partial agonist. It has a high affinity, but low efficacy at the mu receptor where it yields a partial effect upon binding. It also, however, possesses kappa receptor antagonist activity making it useful not only as an analgesic, but also in opioid abuse deterrence, detoxification, and maintenance therapies. Naloxone is added to sublingual buprenorph

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Colman, Atalie S., та John H. Miller. "μ-1 Opioid Receptor Stimulation Decreases Body Temperature in Conscious, Unrestrained Neonatal Rats". Experimental Biology and Medicine 227, № 6 (2002): 377–81. http://dx.doi.org/10.1177/153537020222700602.

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The influence of μ-selective opioid agonists on neonatal thermoregulatory mechanisms has received little attention. Opioid treatment in adult subjects can cause either hyper- or hypothermia, depending on the experimental conditions, the strain of rat used, and the dose and route of administration of the drug. The present study assessed the effect of two μ opioid agonists on body temperature in neonatal Wistar rats aged 2 to 13 days. Rat pups were administered either saline or one of the two μ-selective opioid agonists, dermorphin (0.4 mg/kg) or fentanyl (0.06 mg/kg), by subcutaneous injection.

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Mais fontes

Teses / dissertações sobre o assunto "Receptors; Irreversible antagonist; Drug abuse"

Neilan, Claire L. "In vitro and in vivo characterisation of buprenorphine and other long-lasting opioids." Thesis, Loughborough University, 1999. https://dspace.lboro.ac.uk/2134/14129.

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Buprenorphine is a promising medication for the treatment of opiate abuse. The pharmacology of buprenorphine has been studied in vitro using radioligand binding and [³⁵S]GTPγS assays, and in vivo using assays of antinociception in rodents. A number of compounds with potential similar pharmacology have also been characterised. These are an iso-morphinan pyrrolidine derivative, and long-lasting 14-aminomorphinones and codeinones, in particular clocinnamox (C-CAM), a pure μ-antagonist and methoclocinnamox (MC-CAM), which has some agonist properties.

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Livros sobre o assunto "Receptors; Irreversible antagonist; Drug abuse"

Lambert, David G. Mechanisms and determinants of anaesthetic drug action. Edited by Michel M. R. F. Struys. Oxford University Press, 2017. http://dx.doi.org/10.1093/med/9780199642045.003.0013.

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This chapter is broken into two main sections: a general description of the principles of ligand receptor interaction and a discussion of the main groups of ‘targets’; and explanation of some common pharmacological interactions in anaesthesia, critical care, and pain management. Agonists bind to and activate receptors while antagonists bind to receptors and block the effects of agonists. Antagonists can be competitive (most common) or non-competitive/irreversible. The main classes of drug target are enzymes, carriers, ion channels, and receptors with examples of anaesthetic relevance interacti

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Capítulos de livros sobre o assunto "Receptors; Irreversible antagonist; Drug abuse"

Negus, S. Stevens. "Opioid Antagonist Effects in Animal Models Related to Opioid Abuse: Drug Discrimination and Drug Self-Administration." In Opiate Receptors and Antagonists. Humana Press, 2009. http://dx.doi.org/10.1007/978-1-59745-197-0_11.

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