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Novel olanzapine analogues presenting a reduced H₁ receptor affinity and retained 5HT_2A/D₂ binding affinity ratio

Olanzapine is an atypical antipsychotic drug with high clinical efficacy, but which can cause severe weight gain and metabolic disorders in treated patients. Blockade of the histamine 1 (H₁) receptors is believed...

Authors: Somayeh Jafari, Marc E Bouillon, Xu-Feng Huang, Stephen G Pyne and Francesca Fernandez-Enright

Citation: BMC Pharmacology 2012 12:8

Content type: Research article Published on: 22 June 2012
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Lipid phosphate phosphatase inhibitors locally amplify lysophosphatidic acid LPA₁ receptor signalling in rat brain cryosections without affecting global LPA degradation

Lysophosphatidic acid (LPA) is a signalling phospholipid with multiple biological functions, mainly mediated through specific G protein-coupled receptors. Aberrant LPA signalling is being increasingly implicat...

Authors: Niina Aaltonen, Marko Lehtonen, Katri Varonen, Gemma Arrufat Goterris and Jarmo T Laitinen

Citation: BMC Pharmacology 2012 12:7

Content type: Research article Published on: 11 June 2012
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The orthosteric agonist 2-chloro-5-hydroxyphenylglycine activates mGluR5 and mGluR1 with similar efficacy and potency

The efficacy, potency, and selectivity of the compound 2-Chloro-5-hydroxyphenylglycine (CHPG), a nominally selective agonist for metabotropic glutamate receptor 5 (mGluR5), were examined with select mGluRs by ...

Authors: Paul J Kammermeier

Citation: BMC Pharmacology 2012 12:6

Content type: Research article Published on: 29 May 2012
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Long-acting κ opioid antagonists nor-BNI, GNTI and JDTic: pharmacokinetics in mice and lipophilicity

Nor-BNI, GNTI and JDTic induce κ opioid antagonism that is delayed by hours and can persist for months. Other effects are transient. It has been proposed that these drugs may be slowly absorbed or distributed,...

Authors: Thomas A Munro, Loren M Berry, Ashlee Van’t Veer, Cécile Béguin, F Ivy Carroll, Zhiyang Zhao, William A Carlezon Jr and Bruce M Cohen

Citation: BMC Pharmacology 2012 12:5

Content type: Research article Published on: 29 May 2012
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5-hydroxytryptamine (5-HT) reduces total peripheral resistance during chronic infusion: direct arterial mesenteric relaxation is not involved

Serotonin (5-hydroxytryptamine; 5-HT) delivered over 1 week results in a sustained fall in blood pressure in the sham and deoxycorticosterone acetate (DOCA)-salt rat. We hypothesized 5-HT lowers blood pressure...

Authors: Robert Patrick Davis, Jill Pattison, Janice M Thompson, Ruslan Tiniakov, Karie E Scrogin and Stephanie W Watts

Citation: BMC Pharmacology 2012 12:4

Content type: Research article Published on: 6 May 2012
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Contrasting effects of linaclotide and lubiprostone on restitution of epithelial cell barrier properties and cellular homeostasis after exposure to cell stressors

Linaclotide has been proposed as a treatment for the same gastrointestinal indications for which lubiprostone has been approved, chronic idiopathic constipation and irritable bowel syndrome with constipation. ...

Authors: John Cuppoletti, Anthony T Blikslager, Jayati Chakrabarti, Prashant K Nighot and Danuta H Malinowska

Citation: BMC Pharmacology 2012 12:3

Content type: Research article Published on: 3 May 2012
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Potency, selectivity and prolonged binding of saxagliptin to DPP4: maintenance of DPP4 inhibition by saxagliptin in vitro and ex vivo when compared to a rapidly-dissociating DPP4 inhibitor

Dipeptidylpeptidase 4 (DPP4) inhibitors have clinical benefit in patients with type 2 diabetes mellitus by increasing levels of glucose-lowering incretin hormones, such as glucagon-like peptide -1 (GLP-1), a p...

Authors: Aiying Wang, Charles Dorso, Lisa Kopcho, Gregory Locke, Robert Langish, Eric Harstad, Petia Shipkova, Jovita Marcinkeviciene, Lawrence Hamann and Mark S Kirby

Citation: BMC Pharmacology 2012 12:2

Content type: Research article Published on: 4 April 2012
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Computational models for in-vitro anti-tubercular activity of molecules based on high-throughput chemical biology screening datasets

The emergence of Multi-drug resistant tuberculosis in pandemic proportions throughout the world and the paucity of novel therapeutics for tuberculosis have re-iterated the need to accelerate the discovery of n...

Authors: Vinita Periwal, Shireesha Kishtapuram and Vinod Scaria

Citation: BMC Pharmacology 2012 12:1

Content type: Research article Published on: 31 March 2012
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The effect of formulation vehicles on the in vitro percutaneous permeation of ibuprofen

The transdermal application of substances represents an elegant approach to overcome side effects related to injections or oral treatment. Due to benefits like a constant plasma level, no pain during applicati...

Authors: Jessica Stahl, Mareike Wohlert and Manfred Kietzmann

Citation: BMC Pharmacology 2011 11:12

Content type: Research article Published on: 14 December 2011
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Polyamidoamine (PAMAM) dendrimer conjugate specifically activates the A₃ adenosine receptor to improve post-ischemic/reperfusion function in isolated mouse hearts

When stimulated by small molecular agonists, the A₃ adenosine receptor (AR) mediates cardioprotective effects without inducing detrimental hemodynamic side effects. We have examined pharmacologically the protecti...

Authors: Tina C Wan, Dilip K Tosh, Lili Du, Elizabeth T Gizewski, Kenneth A Jacobson and John A Auchampach

Citation: BMC Pharmacology 2011 11:11

Content type: Research article Published on: 31 October 2011
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Protection of protease-activated receptor 2 mediated vasodilatation against angiotensin II-induced vascular dysfunction in mice

Under conditions of cardiovascular dysfunction, protease-activated receptor 2 (PAR2) agonists maintain vasodilatation activity, which has been attributed to increased cyclooxygenase-2, nitric oxide synthase an...

Authors: Elizabeth Chia, Satomi Kagota, Enoka P Wijekoon and John J McGuire

Citation: BMC Pharmacology 2011 11:10

Content type: Research article Published on: 28 September 2011
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Erratum to: Improvement of right heart structure and function by BAY41-8543 in pulmonary artery banded mice

Authors: Wiebke Janssen, Yves Schymura, Astrid Wietelmann, Johannes-Peter Stasch, Himal Luitel, Norbert Weissmann, Hossein Ardeschir Ghofrani, Friedrich Grimminger, Thomas Braun, Werner Seeger and Ralph Theo Schermuly

Citation: BMC Pharmacology 2011 11(Suppl 1):P80

Content type: Erratum Published on: 14 September 2011

This article is part of a Supplement: Volume 11 Supplement 1

The original article was published in BMC Pharmacology 2011 11:P79
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Properties of the transient outward, ultra-rapid delayed rectifier and acetylcholine-sensitive potassium currents in isolated atrial myocytes from dogs: sinus rhythm and tachypaced model of permanent atrial fibrillation

Authors: Zsófia Kohajda, Attila Kristóf, Péter P Kovács, Claudia Corici, László Virág, Viktor Juhász, Zoltán Husti, István Baczkó, András Varró and Norbert Jost

Citation: BMC Pharmacology 2011 11(Suppl 2):A60

Content type: Meeting abstract Published on: 5 September 2011

This article is part of a Supplement: Volume 11 Supplement 2
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The D-type prostanoid (DP) receptor enhances the signaling of chemoattractant receptor-homologous molecule expressed on Th2 cells (CRTH2)

Authors: Miriam Sedej, Ralf Schröder, Kathrin Bell, Wolfgang Platzer, Evi Kostenis, Ákos Heinemann and Maria Waldhoer

Citation: BMC Pharmacology 2011 11(Suppl 2):A58

Content type: Meeting abstract Published on: 5 September 2011

This article is part of a Supplement: Volume 11 Supplement 2
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The double-faced role of P2X₇ receptors in toxin-induced animal models of Parkinson’s disease

Authors: Beáta Sperlágh, Zsuzsanna Hracskó, Mária Baranyi, Cecília Csölle, Flóra Gölöncsér, Ágnes Kittel and Emilia Madarász

Citation: BMC Pharmacology 2011 11(Suppl 2):A56

Content type: Meeting abstract Published on: 5 September 2011

This article is part of a Supplement: Volume 11 Supplement 2
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Can the electrophysiological action of rosiglitazone explain its cardiac side effects?

Authors: Valéria Kecskeméti, Andrea Szebeni, Norbert Szentandrássy and Péter P Nánási

Citation: BMC Pharmacology 2011 11(Suppl 2):A54

Content type: Meeting abstract Published on: 5 September 2011

This article is part of a Supplement: Volume 11 Supplement 2
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Stability monitoring of some acetylcholinesterase reactivating drugs

Authors: Nazila Ram, Péter Szegi, Kamil Kuča, Farzad Hashemi and Kornélia Tekes

Citation: BMC Pharmacology 2011 11(Suppl 2):A52

Content type: Meeting abstract Published on: 5 September 2011

This article is part of a Supplement: Volume 11 Supplement 2
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Penetration of polar organic compounds through the blood-brain barrier

Authors: Huba Kalász, Kamil Musílek and Kornélia Tekes

Citation: BMC Pharmacology 2011 11(Suppl 2):A51

Content type: Meeting abstract Published on: 5 September 2011

This article is part of a Supplement: Volume 11 Supplement 2
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Capsaicin-sensitive sensory nerves, TRPV1 receptors and tachykinins play important roles in mast cell tryptase-induced arthritis and hyperalgesia

Authors: Zsuzsanna Helyes, Éva Borbély, Katalin Sándor, Adrienn Markovics, Erika Pintér, János Szolcsányi, John P Quinn and Jason J McDougall

Citation: BMC Pharmacology 2011 11(Suppl 2):A50

Content type: Meeting abstract Published on: 5 September 2011

This article is part of a Supplement: Volume 11 Supplement 2
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Salermide down-regulates sirtuin proteins to induce human cancer cell apoptosis

Authors: Asha Leisser, Michael Wolzt and Angela Storka

Citation: BMC Pharmacology 2011 11(Suppl 2):A49

Content type: Meeting abstract Published on: 5 September 2011

This article is part of a Supplement: Volume 11 Supplement 2
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Role of nitric oxide in optic nerve head blood flow regulation while experimental increase of ocular perfusion pressure

Authors: Reinhard Told, Doreen Schmidl, Michael Lasta, Agnes Boltz, Berthold Pemp, Semira Kaya, Gerhard Garhöfer, Gabriele Fuchsjäger-Mayrl and Leopold Schmetterer

Citation: BMC Pharmacology 2011 11(Suppl 2):A47

Content type: Meeting abstract Published on: 5 September 2011

This article is part of a Supplement: Volume 11 Supplement 2
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[¹¹C]Elacridar as a novel P-glycoprotein PET tracer, assessment of whole-body distribution and radiation dosimetry in humans

Authors: Martin Bauer, Markus Zeitlinger, Georg Dobrozemsky, Cécile Philippe, Markus Müller and Oliver Langer

Citation: BMC Pharmacology 2011 11(Suppl 2):A46

Content type: Meeting abstract Published on: 5 September 2011

This article is part of a Supplement: Volume 11 Supplement 2
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Effect of orally administered moxaverine on ocular haemodynamics

Authors: Stefan Palkovits, Michael Lasta, Doreen Schmidl, Agnes Boltz, Reinhard Told, Semira Kaya, Gerhard Garhöfer and Leopold Schmetterer

Citation: BMC Pharmacology 2011 11(Suppl 2):A45

Content type: Meeting abstract Published on: 5 September 2011

This article is part of a Supplement: Volume 11 Supplement 2
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Identification of a new C-terminal splice variant of Ca_V1.3 L-type calcium channels with unique functional properties

Authors: Gabriella Juhasz-Vedres, Anja Scharinger, Mathias Gebhart, Perrine Busquet, Chiara Poggiani, Simone B Sartori, Martina J Sinnegger-Brauns, Alexandra Koschak and Jörg Striessnig

Citation: BMC Pharmacology 2011 11(Suppl 2):A44

Content type: Meeting abstract Published on: 5 September 2011

This article is part of a Supplement: Volume 11 Supplement 2
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Septal urocortin 3 modulates stress-coping behaviour but not hypothalamic-pituitary-adrenal axis activity during forced swimming

Authors: Karl Ebner, Alesja Rjabokon and Nicolas Singewald

Citation: BMC Pharmacology 2011 11(Suppl 2):A43

Content type: Meeting abstract Published on: 5 September 2011

This article is part of a Supplement: Volume 11 Supplement 2
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The folding interactome of GPCRs

Authors: Christian Bergmayr, Christian Nanoff, Oliver Kudlacek, Michael Freissmuth and Christian W Gruber

Citation: BMC Pharmacology 2011 11(Suppl 2):A41

Content type: Meeting abstract Published on: 5 September 2011

This article is part of a Supplement: Volume 11 Supplement 2
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129S1/SvImJ mice display impaired contextual fear extinction, enhanced fear incubation and deficit extinction consolidation phenotypes: rescue via pharmacological and non-pharmacological treatments

Authors: Nigel Whittle, Markus Hauschild, Marguerite Camp, Andrew Holmes and Nicolas Singewald

Citation: BMC Pharmacology 2011 11(Suppl 2):A39

Content type: Meeting abstract Published on: 5 September 2011

This article is part of a Supplement: Volume 11 Supplement 2
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Differential regulation of amphetamine-induced serotonergic and dopaminergic efflux by syntaxin 1A

Authors: Therese Montgomery, Sonja Sucic, Thomas Steinkellner, Michael Freissmuth and Harald Sitte

Citation: BMC Pharmacology 2011 11(Suppl 2):A38

Content type: Meeting abstract Published on: 5 September 2011

This article is part of a Supplement: Volume 11 Supplement 2
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Autocrine signalling as cause of sensitized cAMP formation

Authors: Christian Nanoff, Qiong Yang and Edin Ibrišimović

Citation: BMC Pharmacology 2011 11(Suppl 2):A37

Content type: Meeting abstract Published on: 5 September 2011

This article is part of a Supplement: Volume 11 Supplement 2
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Teaching therapy-oriented pharmacology within a medical curriculum

Authors: Georg Wietzorrek

Citation: BMC Pharmacology 2011 11(Suppl 2):A35

Content type: Meeting abstract Published on: 5 September 2011

This article is part of a Supplement: Volume 11 Supplement 2
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Screening for serine/threonine kinases phosphorylating Stat5

Authors: Angelika Berger, Andrea Hölbl, Wolfgang Warsch and Veronika Sexl

Citation: BMC Pharmacology 2011 11(Suppl 2):A33

Content type: Meeting abstract Published on: 5 September 2011

This article is part of a Supplement: Volume 11 Supplement 2
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Characterising the interaction between the COPII component SEC24C and the human serotonin transporter

Authors: Florian Koban and Sonja Sucic

Citation: BMC Pharmacology 2011 11(Suppl 2):A31

Content type: Meeting abstract Published on: 5 September 2011

This article is part of a Supplement: Volume 11 Supplement 2
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Characterization of CPCA-induced action on isolated rat femoral artery

Authors: Miroslav Radenković, Radmila Stevanović, Milica Stojiljković, Mirko Topalović and Marko Stojanović

Citation: BMC Pharmacology 2011 11(Suppl 2):A29

Content type: Meeting abstract Published on: 5 September 2011

This article is part of a Supplement: Volume 11 Supplement 2
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Expression and differential distribution of the shaker-related voltage-gated potassium channel family (K_V1.x) in human hippocampus and neocortex

Authors: Irmgard Leitner, Georg Wietzorrek, Maria Trieb, Josef Marksteiner and Hans-Günther Knaus

Citation: BMC Pharmacology 2011 11(Suppl 2):A27

Content type: Meeting abstract Published on: 5 September 2011

This article is part of a Supplement: Volume 11 Supplement 2
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Simvastatin targets the IL-6 signalling cascade in human melanoma cells

Authors: Christine Wasinger, Christoph Minichsdorfer and Martin Hohenegger

Citation: BMC Pharmacology 2011 11(Suppl 2):A25

Content type: Meeting abstract Published on: 5 September 2011

This article is part of a Supplement: Volume 11 Supplement 2
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Statins modulate the expression profile of ATP-binding cassette transporters in human neuroblastoma cells

Authors: Bihter Atil, Evelyn Sieczkowski and Martin Hohenegger

Citation: BMC Pharmacology 2011 11(Suppl 2):A23

Content type: Meeting abstract Published on: 5 September 2011

This article is part of a Supplement: Volume 11 Supplement 2
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LRET-based intramolecular distance measurements in LeuT_Aa

Authors: Azmat Sohail, Peggy Stolt-Bergner, Gerhard F Ecker, Michael Freissmuth, Thomas Stockner, Harald H Sitte and Walter Sandtner

Citation: BMC Pharmacology 2011 11(Suppl 2):A21

Content type: Meeting abstract Published on: 5 September 2011

This article is part of a Supplement: Volume 11 Supplement 2
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Amphetamine actions rely on the availability of phosphatidylinositol-4,5-bisphosphate

Authors: Florian Buchmayer, Klaus Schicker, Gerald Stübiger, Peter J Hamilton, Petra Geier, Andreas Jurik, René Weissensteiner, Thomas Steinkellner, Heinrich J Matthies, Therese Montgomery, Marie-Therese Winkler, Jae-Won Yang, Marion Holy, Gerhard F Ecker, Aurelio Galli, Valery Bochkov…

Citation: BMC Pharmacology 2011 11(Suppl 2):A19

Content type: Meeting abstract Published on: 5 September 2011

This article is part of a Supplement: Volume 11 Supplement 2
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Neurodegeneration and histochemical plasticity in the rat subiculum after kainic acid-induced epilepsy

Authors: Meinrad Drexel, Adrian P Preidt, Elke Kirchmair and Günther Sperk

Citation: BMC Pharmacology 2011 11(Suppl 2):A17

Content type: Meeting abstract Published on: 5 September 2011

This article is part of a Supplement: Volume 11 Supplement 2
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Identification of novel ligands interacting with kappa opioid receptors

Authors: Mariana Spetea, Muhammad F Asim, Ilona P Berzetei-Gurske, Gerhard Wolber and Helmut Schmidhammer

Citation: BMC Pharmacology 2011 11(Suppl 2):A15

Content type: Meeting abstract Published on: 5 September 2011

This article is part of a Supplement: Volume 11 Supplement 2
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Bacterial peptidoglycan enhances sickness behaviour induced by bacterial lipopolysaccharide

Authors: Aitak Farzi, Evelin Painsipp and Peter Holzer

Citation: BMC Pharmacology 2011 11(Suppl 2):A14

Content type: Meeting abstract Published on: 5 September 2011

This article is part of a Supplement: Volume 11 Supplement 2
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Development of novel N-methyl and N-allyl-substituted oxazolomorphinans and their interaction with opioid receptors

Authors: Attila Sipos, Levente Girán, Sándor Berényi, Sándor Antus, Helmut Schmidhammer and Mariana Spetea

Citation: BMC Pharmacology 2011 11(Suppl 2):A13

Content type: Meeting abstract Published on: 5 September 2011

This article is part of a Supplement: Volume 11 Supplement 2
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Timothy mutation affects tightly sealing point of Ca_V1.2 activation gate

Authors: Katrin Depil, Stanislav Beyl, Anna Stary-Weinzinger, Annette Hohaus, Eugen Timin and Steffen Hering

Citation: BMC Pharmacology 2011 11(Suppl 2):A12

Content type: Meeting abstract Published on: 5 September 2011

This article is part of a Supplement: Volume 11 Supplement 2
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Structural determinants of Ca_V1.3 L-type calcium channel gating

Authors: Andreas Lieb, Anja Scharinger, Florian Hechenblaickner, Mathias Gebhart, Alexandra Koschak, Martina J Sinnegger-Brauns and Jörg Striessnig

Citation: BMC Pharmacology 2011 11(Suppl 2):A11

Content type: Meeting abstract Published on: 5 September 2011

This article is part of a Supplement: Volume 11 Supplement 2
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Activation of kappa opioid receptors reduces EEG seizure activity in a mouse model of temporal lobe epilepsy

Authors: Luca Zangrandi and Christoph Schwarzer

Citation: BMC Pharmacology 2011 11(Suppl 2):A10

Content type: Meeting abstract Published on: 5 September 2011

This article is part of a Supplement: Volume 11 Supplement 2
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Biological, pharmacological and immunological activities of novel 6-amino-acid-substituted 14-alkoxy-N-methylmorphinans

Authors: Elena Guerrieri, Valeria Follia, Dorota Garczarczyk, Silvia B Rief, Monika Fink, Muhammad F Asim, Mariana Spetea and Helmut Schmidhammer

Citation: BMC Pharmacology 2011 11(Suppl 2):A5

Content type: Meeting abstract Published on: 5 September 2011

This article is part of a Supplement: Volume 11 Supplement 2
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Efficacy of systemic HS-198, an analogue of oxymorphone, on cancer pain-related behaviour in mice

Authors: Muhammad F Asim, Catalina R Bohotin, Cristina E Constantin, Helmut Schmidhammer, Michaela Kress and Mariana Spetea

Citation: BMC Pharmacology 2011 11(Suppl 2):A4

Content type: Meeting abstract Published on: 5 September 2011

This article is part of a Supplement: Volume 11 Supplement 2
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Reduced fear conditioning after viral vector mediated neuropeptide Y administration into the basolateral amygdala

Authors: Dilip Verma, Ramon O Tasan, Mario Mietzsch, Stefan Weger, Regine Heilbronn, Herbert Herzog and Günther Sperk

Citation: BMC Pharmacology 2011 11(Suppl 2):A3

Content type: Meeting abstract Published on: 5 September 2011

This article is part of a Supplement: Volume 11 Supplement 2
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Neuropeptide Y Y₂ receptors modulate trace fear conditioning and spatial memory in the dorsal hippocampus

Authors: Ramon O Tasan, Dilip Verma, Mario Mietzsch, Stefan Weger, Regine Heilbronn, Herbert Herzog and Günther Sperk

Citation: BMC Pharmacology 2011 11(Suppl 2):A2

Content type: Meeting abstract Published on: 5 September 2011

This article is part of a Supplement: Volume 11 Supplement 2
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The anti-addictive drug ibogaine modulates voltage-gated ion channels and may trigger cardiac arrhythmias

Authors: Michael Kovar, Xaver Koenig, Ágnes Mike, René Cervenka, Péter Lukács, Hannes Todt, Walter Sandtner and Karlheinz Hilber

Citation: BMC Pharmacology 2011 11(Suppl 2):A1

Content type: Meeting abstract Published on: 5 September 2011

This article is part of a Supplement: Volume 11 Supplement 2
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