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278 Aktuelle Fachpublikationen in The AAPS Journal

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Modulating inhibitory ligand-gated ion channels

13.05.2010 | Michael Cascio, The AAPS Journal, 2010

The glycine and γ-aminobutyric acid receptors (GlyR and GABAAR, respectively) are the major inhibitory neurotransmitter-gated receptors in the central nervous system of animals. Given the important role of these receptors in neuronal inhibition, they are prime targets of many therapeutic ...

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Role of morphine's metabolites in analgesia: Concepts and controversies

13.05.2010 | Erica Wittwer, Steven E. Kern, The AAPS Journal, 2010

The metabolites of morphine, morphine-6-glucuronide (M6G) and morphine-3-glucuronide (M3G), have been extensively studied for their contribution to clinical effects following administration of morphine. Those contributions to both the desired effect (ie, analgesia) and the undesired effects ...

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Causes and consequences of methamphetamine and MDMA toxicity

13.05.2010 | Maria S. Quinton, Bryan K. Yamamoto, The AAPS Journal, 2010

Methamphetamine (METH) and its derivative 3,4-methylenedioxymethamphetamine (MDMA; ecstasy) are 2 substituted amphetamines with very high abuse liability in the United States. These amphetamine-like stimulants have been associated with loss of multiple markers for dopaminergic and ...

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Computational methods in drug design: Modeling G protein-coupled receptor monomers, dimers, and oligomers

13.05.2010 | Patricia H. Reggio, The AAPS Journal, 2010

G protein-coupled receptors (GPCRs) are membrane proteins that serve as very important links through which cellular signal transduction mechanisms are activated. Many vital physiological events such as sensory perception, immune defense, cell communication, chemotaxis, and neuro-transmission ...

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Lipids and lipidomics in brain injury and diseases

13.05.2010 | Rao Muralikrishna Adibhatla, J. F. Hatcher, R. J. Dempsey, The AAPS Journal, 2010

Lipidomics is systems-level analysis and characterization of lipids and their interacting moieties. The amount of information in the genomic and proteomic fields is greater than that in the lipidomics field, because of the complex nature of lipids and the limitations of tools for analysis. ...

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Targeting the PDZ domains of molecular scaffolds of transmembrane ion channels

13.05.2010 | Andrea Piserchio, Mark Spaller, Dale F. Mierke, The AAPS Journal, 2010

The family of multidomain proteins known as the synaptic associated proteins (SAPs) act as molecular scaffolds, playing an important role in the signaling and maintenance of several receptors and channels. The SAPs consist of 5 individual protein domains: 3 PDZ (PSD95, Disc Large, Zol) ...

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Mechanisms of methamphetamine-induced dopaminergic neurotoxicity

13.05.2010 | Evan L. Riddle, Annette E. Fleckenstein, Glen R. Hanson, The AAPS Journal, 2010

Methamphetamine (METH) is a powerful stimulant of abuse with potent addictive and neurotoxic properties. More than 2.5 decades ago, METH-induced damage to dopaminergic neurons was described. Since then, numerous advancements have been made in the search for the underlying mechanisms whereby ...

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2-Arachidonoylglycerol (2-AG) membrane transport: History and outlook

13.05.2010 | Anita Hermann, Martin Kaczocha, Dale G. Deutsch, The AAPS Journal, 2010

Only a few studies have addressed the transport of 2-arachidonoylglycerol (2-AG), a naturally occurring agonist for cannabinoid receptors. Based upon saturation kinetics, these early reports have proposed that 2-AG enters the cell by a specific 2-AG transporter, via the putative anandamide ...

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Endocannabinoid signaling directs periimplantation events

13.05.2010 | Haibin Wang, Huirong Xie, Sudhansu K. Dey, The AAPS Journal, 2010

An emerging concept in female reproduction is the role of endocannabinoids, a group of endogenously produced lipid mediators that bind to and activate cannabinoid receptors. Although adverse effects of cannabinoids in female reproduction have been implicated for years, the mechanisms by which ...

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Developmental toxicity of prenatal exposure to toluene

13.05.2010 | Scott E. Bowen, John H. Hannigan, The AAPS Journal, 2010

Organic solvents have become ubiquitous in our environment and are essential for industry. Many women of reproductive age are incresingly exposed to solvents such as toluene in occupational settings (ie, long-term, lowconcentration exposures) or through inhalant abuse (eg, episodic, binge ...

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