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Alcohol addiction and the mu-opioid receptor
Progress in Neuro-Psychopharmacology and Biological Psychiatry, 2016Alcohol addiction is one of the most common and devastating diseases in the world. Given the tremendous heterogeneity of alcohol addicted individuals, it is unlikely that one medication will help nearly all patients. Thus, there is a clear need to develop predictors of response to existing medications.
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Mu-opioid receptor is associated with phosphatase activity
Biochemical and Biophysical Research Communications, 1986A preparation of purified mu opioid receptor from bovine brain hydrolyzes p-nitrophenylphosphate. This phosphatase activity has a pH optimum of 9.0, a Km of 9.0 microM, and is stimulated by Mn++ and Mg++ ions. Evidence that the observed activity is not due to a contaminant in the opioid receptor preparation includes 1) the activity is associated ...
S, Roy, N M, Lee, H H, Loh
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Mu opioid receptor: a gateway to drug addiction
Current Opinion in Neurobiology, 2004Mu opioid receptors mediate positive reinforcement following direct (morphine) or indirect (alcohol, cannabinoids, nicotine) activation, and our understanding of mu receptor function is central to the development of addiction therapies. Recent data obtained in native neurons confirm that mu receptor signaling and regulation are strongly agonist ...
Contet, Candice +2 more
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The Interaction Between the Mu Opioid Receptor and Filamin A
Neurochemical Research, 2010Our laboratory embarked on research to discover proteins the interaction of which with the mu opioid receptor (MOPr) is required for its function and regulation. We performed yeast two-hybrid screens, using the carboxy tail of the human MOPr as bait and a human brain library. This yielded a number of proteins that seemed to bind to the MOPr C-tail. The
Eric J, Simon, Irma, Onoprishvili
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Disruption of the mu–delta opioid receptor heteromer
Biochemical and Biophysical Research Communications, 2012The crystal structure of the mu and kappa opioid receptors has revealed dimeric structural arrangements. Mu-delta receptors heteromers also exist and we have identified discrete cytoplasmic regions in each receptor required for oligomer formation. In the carboxyl tail of the delta receptor we identified three glycine residues (-GGG), substitution of ...
Brian F, O'Dowd +4 more
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Mu Opioid Receptor Antagonists: Recent Developments
ChemMedChem, 2007AbstractFor thousands of years mu opioid agonists such as morphine have been utilized for their analgesic properties. Today, morphine and related compounds are still used as a first line therapy in the treatment of moderate to severe pain. However, despite the clear benefits of mu agonists in pain management, severe side effects such as dependence and ...
Allan J, Goodman +2 more
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Biased agonism in the mu-opioid receptor
2021Dr. Karina Martinez-Mayorga discuss Biased agonism in the mu-opioid receptor.
Karina Martinez-Mayorga +2 more
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Insights into mu opioid pharmacology the role of mu opioid receptor subtypes.
Life sciences, 2001Although mu opioids share many pharmacological characteristics, they also reveal many differences. Many approaches over the years have suggested the existence of multiple mu opioid receptors. The unique selectivities of naloxonazine, for example, provided a way of distinguishing mu₁from mu₂actions.
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Molecular Biology of Mu Opioid Receptors
2010The cloning of the Mu opioid receptor has led to the identification of a large series of splice variants. The gene is complex, with two independent promoters responsible for two distinct sets of splice variants. The primary promoter, associated with exon 1, encodes the majority of the variants, while a second promoter upstream of the first is ...
Ying-Xian Pan, Gavril W. Pasternak
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[Are polymorphisms in the mu-opioid receptor important for opioid therapy?].
Schmerz (Berlin, Germany), 2006Polymorphisms in the mu-opioid receptor gene may potentially alter the clinical effects of opioid analgesics. A common mu-opioid receptor polymorphism occurring at an allelic frequency of 12% decreases the potency of opioid analgesics in humans. Interestingly, in carriers of this mutation, it appears to be possible to reach analgesia by increasing the ...
J, Lötsch +2 more
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