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Novel olanzapine analogues presenting a reduced H1 receptor affinity and retained 5HT2A/D2 binding affinity ratio
Somayeh Jafari, Marc E Bouillon, Xu-Feng Huang, Stephen G Pyne, Francesca Fernandez-Enright BMC Pharmacology 2012, 12:8 (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
Niina Aaltonen, Marko Lehtonen, Katri Varonen, Gemma Goterris, Jarmo T Laitinen BMC Pharmacology 2012, 12:7 (11 June 2012)
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The orthosteric agonist 2-chloro-5-hydroxyphenylglycine activates mGluR5 and mGluR1 with similar efficacy and potency
Paul J Kammermeier BMC Pharmacology 2012, 12:6 (29 May 2012)
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Long-acting κ opioid antagonists nor-BNI, GNTI and JDTic: pharmacokinetics in mice and lipophilicity
Thomas A Munro, Loren M Berry, Ashlee Van’t Veer, Cécile Béguin, F Carroll, Zhiyang Zhao, William A Carlezon, Bruce M Cohen BMC Pharmacology 2012, 12:5 (29 May 2012)
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Editor’s summary
Plasma levels of kappa opioid antagonists in mice following intraperitoneal administration show a strong negative correlation with the prolonged time-course of antagonism, consistent with an irreversible mechanism of action such as receptor desensitisation.
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5-hydroxytryptamine (5-HT) reduces total peripheral resistance during chronic infusion: direct arterial mesenteric relaxation is not involved
Robert Davis, Jill Pattison, Janice M Thompson, Ruslan Tiniakov, Karie E Scrogin, Stephanie W Watts BMC Pharmacology 2012, 12:4 (6 May 2012)
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Editor’s summary
Chronic infusion with 5-hydroxytryptamine (5-HT) reduces total peripheral resistance, and this effect is not due to direct arterial mesenteric relaxation since 5-HT receptors present in the superior mesenteric artery are not functional.
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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
John Cuppoletti, Anthony T Blikslager, Jayati Chakrabarti, Prashant K Nighot, Danuta H Malinowska BMC Pharmacology 2012, 12:3 (3 May 2012)
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Editor’s summary
Comparison of linaclotide with lubiprostone in experimental models of epithelial barrier function and repair suggests that patients with compromised barrier function, such as in irritable bowel syndrome may benefit more from treatment with lubiprostone.
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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
Aiying Wang, Charles Dorso, Lisa Kopcho, Gregory Locke, Robert Langish, Eric Harstad, Petia Shipkova, Jovita Marcinkeviciene, Lawrence Hamann, Mark S Kirby BMC Pharmacology 2012, 12:2 (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
Vinita Periwal, Shireesha Kishtapuram, Open Source Drug Discovery Consortium, Vinod Scaria BMC Pharmacology 2012, 12:1 (31 March 2012)
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Editor’s summary
Computational methods based on Machine Learning tools and supervised classifiers generate accurate predictive models for virtual high-throughput screens of large libraries of anti-tubercular molecules, allowing prioritization of good candidates for drug discovery.
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The effect of formulation vehicles on the in vitro percutaneous permeation of ibuprofen
Jessica Stahl, Mareike Wohlert, Manfred Kietzmann BMC Pharmacology 2011, 11:12 (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
Tina C Wan, Dilip K Tosh, Lili Du, Elizabeth T Gizewski, Kenneth A Jacobson, John A Auchampach BMC Pharmacology 2011, 11:11 (31 October 2011)
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Editor’s summary
A Polyamidoamine (PAMAM) dendrimer conjugated to 64 moieties of a nucleoside agonist binds to the mouse A3 adenosine receptor with enhanced potency and selectivity, and mediates cardioprotective effects in an isolated heart model of ischemia/reperfusion injury.
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Protection of protease-activated receptor 2 mediated vasodilatation against angiotensin II-induced vascular dysfunction in mice
Elizabeth Chia, Satomi Kagota, Enoka P Wijekoon, John J McGuire BMC Pharmacology 2011, 11:10 (28 September 2011)
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Editor’s summary
Vasodilatation mediated by protease-activated receptor 2 (PAR2) is retained in a mouse model of Angiotensin-II induced hypertension and mesenteric arterial vascular dysfunction, through a mechanism dependent on the calcium-activated potassium channel SK3.1.
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Towards the development of novel Trypanosoma brucei RNA editing ligase 1 inhibitors
Jacob D Durrant, J Andrew McCammon BMC Pharmacology 2011, 11:9 (30 August 2011)
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Dexamethasone restrains ongoing expression of interleukin-23p19 in peripheral blood-derived human macrophages
Linda Palma, Carla Sfara, Antonella Antonelli, Mauro Magnani BMC Pharmacology 2011, 11:8 (26 July 2011)
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Editor’s summary
The glucocorticoid analogue dexamethasone reduces the expression of interleukin-23p19 in human monocyte-derived macrophages via a distinct cascade of down-modulation, secondary to the suppression of p38 MAPK activity and likely involving MAPK phosphatase-1 (MKP-1).
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Enhanced sensitivity to cisplatin and gemcitabine in Brca1-deficient murine mammary epithelial cells
Elizabeth Alli, Vandana B Sharma, Anne-Renee Hartman, Patrick S Lin, Lisa McPherson, James M Ford BMC Pharmacology 2011, 11:7 (19 July 2011)
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Differential effects of TRPV1 receptor ligands against nicotine-induced depression-like behaviors
Tamaki Hayase BMC Pharmacology 2011, 11:6 (18 July 2011)
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A web server for predicting inhibitors against bacterial target GlmU protein
Deepak Singla, Meenakshi Anurag, Debasis Dash, Gajendra PS Raghava BMC Pharmacology 2011, 11:5 (6 July 2011)
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Editor’s summary
A Quantitative Structure Activity Relationship (QSAR) model based on docking energy descriptors predicts potential inhibitors of the Mycobacterium tuberculosis drug target GlmU, that could be used in the development of drugs against tuberculosis.
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Synthesis of 86 species of 1,5-diaryl-3-oxo-1,4-pentadienes analogs of curcumin can yield a good lead in vivo
Chieko Kudo, Hiroyuki Yamakoshi, Atsuko Sato, Hiroshi Nanjo, Hisatsugu Ohori, Chikashi Ishioka, Yoshiharu Iwabuchi, Hiroyuki Shibata BMC Pharmacology 2011, 11:4 (28 May 2011)
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Synthetic analogs of natural curcumin, found in the popular Indian spice turmeric, overcome the compound's low bioavailability and display enhanced chemotherapeutic potential both in vitro and in a mouse model of colorectal carcinogenesis.
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Altered 5-HT2C receptor agonist-induced responses and 5-HT2C receptor RNA editing in the amygdala of serotonin transporter knockout mice
Pablo R Moya, Meredith A Fox, Catherine L Jensen, Justin L Laporte, Helen T French, Jens R Wendland, Dennis L Murphy BMC Pharmacology 2011, 11:3 (7 April 2011)
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Knock-out mice for the serotonin transporter (SERT) are impaired in the anxiogenic response induced by serotonin receptor agonists and display an increased editing of the serotonin 5-HT2C receptor RNA compared to wild-type.
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Effects of rasagiline, its metabolite aminoindan and selegiline on glutamate receptor mediated signalling in the rat hippocampus slice in vitro
W Dimpfel, JA Hoffmann BMC Pharmacology 2011, 11:2 (21 February 2011)
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Editor’s summary
The new Parkinson`s disease drug rasagiline and its metabolite aminoindan, affect the glutamate receptor mediated signaling pathway and display dose-dependent neuroprotective activity in the rat hippocampus.
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The boron-oxygen core of borinate esters is responsible for the store-operated calcium entry potentiation ability
Olivier Dellis, Pierre Mercier, Christine Chomienne BMC Pharmacology 2011, 11:1 (26 January 2011)
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Editor’s summary
The Boron-oxygen core present in 2-aminoethyl diphenylborinate (2-APB) and other borinate ester analogues is required for the dual potentiation and inhibition of Store-Operated Calcium Entry (SOCE) in leukocyte cell lines.
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Pharmacokinetic and pharmacodynamic comparison of two "pegylated" interferon alpha-2 formulations in healthy male volunteers: a randomized, crossover, double-blind study
Idrian García-García, Carlos A González-Delgado, Carmen M Valenzuela-Silva, Alina Díaz-Machado, Marisol Cruz-Díaz, Hugo Nodarse-Cuní, Orlando Pérez-Pérez, Cimara H Bermúdez-Badell, Joel Ferrero-Bibilonia, Rolando Páez-Meireles, Iraldo Bello-Rivero, Fidel R Castro-Odio, Pedro A López-Saura, for the FarmaPEG Study Group BMC Pharmacology 2010, 10:15 (23 November 2010)
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Histopathology and biochemistry analysis of the interaction between sunitinib and paracetamol in mice
Adeline YL Lim, Ignacio Segarra, Srikumar Chakravarthi, Sufyan Akram, John P Judson BMC Pharmacology 2010, 10:14 (15 October 2010)
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Protective efficacy of natansnin, a dibenzoyl glycoside from Salvinia natans against CCl4 induced oxidative stress and cellular degeneration in rat liver
Polimetla Srilaxmi, Gangadhara Sareddy, Polavarapu kishor, Oruganti Setty, Phanithi Babu BMC Pharmacology 2010, 10:13 (12 October 2010)
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Hematopoietic stem cells exhibit a specific ABC transporter gene expression profile clearly distinct from other stem cells
Leilei Tang, Saskia M Bergevoet, Christian Gilissen, Theo de Witte, Joop H Jansen, Bert A van der Reijden, Reinier AP Raymakers BMC Pharmacology 2010, 10:12 (13 September 2010)
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Beneficial effect of agmatine on brain apoptosis, astrogliosis, and edema after rat transient cerebral ischemia
Che-Chuan Wang, Chung-Ching Chio, Ching-Hong Chang, Jinn-Rung Kuo, Ching-Ping Chang BMC Pharmacology 2010, 10:11 (6 September 2010)
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