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BMC Pharmacology

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https://www.readbyqxmd.com/read/22686545/lipid-phosphate-phosphatase-inhibitors-locally-amplify-lysophosphatidic-acid-lpa1-receptor-signalling-in-rat-brain-cryosections-without-affecting-global-lpa-degradation
#1
Niina Aaltonen, Marko Lehtonen, Katri Varonen, Gemma Arrufat Goterris, Jarmo T Laitinen
BACKGROUND: 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 implicated in the pathology of common human diseases, such as arteriosclerosis and cancer. The lifetime of the signalling pool of LPA is controlled by the equilibrium between synthesizing and degradative enzymatic activity. In the current study, we have characterized these enzymatic pathways in rat brain by pharmacologically manipulating the enzymatic machinery required for LPA degradation...
June 11, 2012: BMC Pharmacology
https://www.readbyqxmd.com/read/22642416/long-acting-%C3%AE%C2%BA-opioid-antagonists-nor-bni-gnti-and-jdtic-pharmacokinetics-in-mice-and-lipophilicity
#2
Thomas A Munro, Loren M Berry, Ashlee Van't Veer, Cécile Béguin, F Ivy Carroll, Zhiyang Zhao, William A Carlezon, Bruce M Cohen
BACKGROUND: 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, and may dissolve in cell membranes, thus slowing elimination and prolonging their effects. Recent evidence suggests, instead, that they induce prolonged desensitization of the κ opioid receptor. METHODS: To evaluate these hypotheses, we measured relevant physicochemical properties of nor-BNI, GNTI and JDTic, and the timecourse of brain and plasma concentrations in mice after intraperitoneal administration (using LC-MS-MS)...
May 29, 2012: BMC Pharmacology
https://www.readbyqxmd.com/read/22559843/5-hydroxytryptamine-5-ht-reduces-total-peripheral-resistance-during-chronic-infusion-direct-arterial-mesenteric-relaxation-is-not-involved
#3
Robert Patrick Davis, Jill Pattison, Janice M Thompson, Ruslan Tiniakov, Karie E Scrogin, Stephanie W Watts
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 through direct receptor-mediated vascular relaxation. In vivo, 5-HT reduced mean arterial pressure (MAP), increased heart rate, stroke volume, cardiac index, and reduced total peripheral resistance during a 1 week infusion of 5-HT (25 µg/kg/min) in the normotensive Sprague Dawley rat. The mesenteric vasculature was chosen as an ideal candidate for the site of 5-HT receptor mediated vascular relaxation given the high percentage of cardiac output the site receives...
May 6, 2012: BMC Pharmacology
https://www.readbyqxmd.com/read/22726212/novel-olanzapine-analogues-presenting-a-reduced-h1-receptor-affinity-and-retained-5ht2a-d2-binding-affinity-ratio
#4
Somayeh Jafari, Marc E Bouillon, Xu-Feng Huang, Stephen G Pyne, Francesca Fernandez-Enright
BACKGROUND: 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 to play a crucial role in olanzapine induced weight gain, whereas the therapeutic effects of this drug are mainly attributed to its favourable serotoninergic 2A and dopamine 2 (5HT2A/D2) receptor binding affinity ratios. RESULTS: We have synthesized novel olanzapine analogues 8a and 8b together with the already known derivative 8c and we have examined their respective in vitro affinities for the 5HT2A, D2, and H1 receptors...
2012: BMC Pharmacology
https://www.readbyqxmd.com/read/22642439/the-orthosteric-agonist-2-chloro-5-hydroxyphenylglycine-activates-mglur5-and-mglur1-with-similar-efficacy-and-potency
#5
COMPARATIVE STUDY
Paul J Kammermeier
BACKGROUND: 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 examining their ability to induce modulation of the native voltage dependent ion channels in isolated sympathetic neurons from the rat superior cervical ganglion (SCG). SCG neurons offer a null mGluR-background in which specific mGluR subtypes can be made to express via intranuclear cDNA injection...
2012: BMC Pharmacology
https://www.readbyqxmd.com/read/22553939/contrasting-effects-of-linaclotide-and-lubiprostone-on-restitution-of-epithelial-cell-barrier-properties-and-cellular-homeostasis-after-exposure-to-cell-stressors
#6
John Cuppoletti, Anthony T Blikslager, Jayati Chakrabarti, Prashant K Nighot, Danuta H Malinowska
BACKGROUND: 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. Stressors damage the epithelial cell barrier and cellular homeostasis leading to loss of these functions. Effects of active linaclotide on repair of barrier and cell function in pig jejunum after ischemia and in T84 cells after treatment with proinflammatory cytokines, interferon-γ and tumor necrosis factor-α were examined...
2012: BMC Pharmacology
https://www.readbyqxmd.com/read/22475049/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
#7
COMPARATIVE STUDY
Aiying Wang, Charles Dorso, Lisa Kopcho, Gregory Locke, Robert Langish, Eric Harstad, Petia Shipkova, Jovita Marcinkeviciene, Lawrence Hamann, Mark S Kirby
BACKGROUND: 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 peptide with a short half life that is secreted for approximately 1 hour following a meal. Since drugs with prolonged binding to their target have been shown to maximize pharmacodynamic effects while minimizing drug levels, we developed a time-dependent inhibitor that has a half-life for dissociation from DPP4 close to the duration of the first phase of GLP-1 release...
2012: BMC Pharmacology
https://www.readbyqxmd.com/read/22463123/computational-models-for-in-vitro-anti-tubercular-activity-of-molecules-based-on-high-throughput-chemical-biology-screening-datasets
#8
Vinita Periwal, Shireesha Kishtapuram, Vinod Scaria
BACKGROUND: 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 novel molecules with anti-tubercular activity. Though high-throughput screens for anti-tubercular activity are available, they are expensive, tedious and time-consuming to be performed on large scales. Thus, there remains an unmet need to prioritize the molecules that are taken up for biological screens to save on cost and time...
2012: BMC Pharmacology
https://www.readbyqxmd.com/read/22168832/the-effect-of-formulation-vehicles-on-the-in-vitro-percutaneous-permeation-of-ibuprofen
#9
Jessica Stahl, Mareike Wohlert, Manfred Kietzmann
BACKGROUND: 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 application and a simple therapeutic regime, the optimization of formulations for transdermal drug delivery has gained interest in the last decades. Ibuprofen is a non-steroidal anti-inflammatory compound which is nowadays often used transdermally. The objective of this work was to conduct a study on the effect of different 5% ibuprofen containing formulations (Ibutop® cream, Ibutop® gel, and ibuprofen solution in phosphate buffered saline) on the in vitro-percutaneous permeation of ibuprofen through skin to emphasise the importance of the formulation on percutaneous permeation and skin reservoir...
2011: BMC Pharmacology
https://www.readbyqxmd.com/read/22039965/polyamidoamine-pamam-dendrimer-conjugate-specifically-activates-the-a3-adenosine-receptor-to-improve-post-ischemic-reperfusion-function-in-isolated-mouse-hearts
#10
Tina C Wan, Dilip K Tosh, Lili Du, Elizabeth T Gizewski, Kenneth A Jacobson, John A Auchampach
BACKGROUND: 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 protective properties of a multivalent dendrimeric conjugate of a nucleoside as a selective multivalent agonist for the mouse A3AR. RESULTS: A PAMAM dendrimer fully substituted by click chemistry on its peripheral groups with 64 moieties of a nucleoside agonist was shown to be potent and selective in binding to the mouse A3AR and effective in cardioprotection in an isolated mouse heart model of ischemia/reperfusion (I/R) injury...
2011: BMC Pharmacology
https://www.readbyqxmd.com/read/22026037/abstracts-of-the-5th-international-conference-on-cgmp-generators-effectors-and-therapeutic-implications-june-24-26-2011-halle-germany
#11
(no author information available yet)
No abstract text is available yet for this article.
2011: BMC Pharmacology
https://www.readbyqxmd.com/read/21999824/17th-scientific-symposium-of-the-austrian-pharmacological-society-aphar-joint-meeting-with-the-hungarian-society-of-experimental-and-clinical-pharmacology-mft-innsbruck-austria-29-30-september-2011-abstracts
#12
https://www.readbyqxmd.com/read/21955547/protection-of-protease-activated-receptor-2-mediated-vasodilatation-against-angiotensin-ii-induced-vascular-dysfunction-in-mice
#13
Elizabeth Chia, Satomi Kagota, Enoka P Wijekoon, John J McGuire
BACKGROUND: 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 and calcium-activated potassium channel (SK3.1) activities. Protease-activated receptor 2 agonist mediated vasodilatation is unknown under conditions of dysfunction caused by angiotensin II. The main purpose of our study was to determine whether PAR2-induced vasodilatation of resistance arteries was attenuated by prolonged angiotensin II treatment in mice...
2011: BMC Pharmacology
https://www.readbyqxmd.com/read/21878090/towards-the-development-of-novel-trypanosoma-brucei-rna-editing-ligase-1-inhibitors
#14
Jacob D Durrant, J Andrew McCammon
BACKGROUND: Trypanosoma brucei (T. brucei) is an infectious agent for which drug development has been largely neglected. We here use a recently developed computer program called AutoGrow to add interacting molecular fragments to S5, a known inhibitor of the validated T. brucei drug target RNA editing ligase 1, in order to improve its predicted binding affinity. RESULTS: The proposed binding modes of the resulting compounds mimic that of ATP, the native substrate, and provide insights into novel protein-ligand interactions that may be exploited in future drug-discovery projects...
2011: BMC Pharmacology
https://www.readbyqxmd.com/read/21791059/dexamethasone-restrains-ongoing-expression-of-interleukin-23p19-in-peripheral-blood-derived-human-macrophages
#15
Linda Palma, Carla Sfara, Antonella Antonelli, Mauro Magnani
BACKGROUND: Since its recent discovery, interleukin-23 has been shown to be involved in the pathogenesis of autoimmune diseases favoring the development of a T cell subset referred to as T helper 17. Glucocorticoids are widely employed in inflammatory and autoimmune diseases as they inhibit pro-inflammatory signaling and prevent production of inflammation mediators. Very limited information is available about the efficacy of synthetic glucocorticoids in containing the expression of interleukin-23 under cell activation...
2011: BMC Pharmacology
https://www.readbyqxmd.com/read/21771338/enhanced-sensitivity-to-cisplatin-and-gemcitabine-in-brca1-deficient-murine-mammary-epithelial-cells
#16
Elizabeth Alli, Vandana B Sharma, Anne-Renee Hartman, Patrick S Lin, Lisa McPherson, James M Ford
BACKGROUND: Breast cancers due to germline mutations or altered expression of the BRCA1 gene associate with an aggressive clinical course and frequently exhibit a "triple-negative" phenotype, i.e. lack of expression of the estrogen and progesterone hormone receptors and lack of overexpression of the HER2/NEU oncogene, thereby rendering them relatively insensitive to hormonal manipulation and targeted HER2 therapy, respectively. BRCA1 plays a role in multiple DNA repair pathways, and thus, when mutated, results in sensitivity to certain DNA damaging drugs...
2011: BMC Pharmacology
https://www.readbyqxmd.com/read/21767384/differential-effects-of-trpv1-receptor-ligands-against-nicotine-induced-depression-like-behaviors
#17
Tamaki Hayase
BACKGROUND: The contributions of brain cannabinoid (CB) receptors, typically CB1 (CB type 1) receptors, to the behavioral effects of nicotine (NC) have been reported to involve brain transient receptor potential vanilloid 1 (TRPV1) receptors, and the activation of candidate endogenous TRPV1 ligands is expected to be therapeutically effective. In the present study, the effects of TRPV1 ligands with or without affinity for CB1 receptors were examined on NC-induced depression-like behavioral alterations in a mouse model in order to elucidate the "antidepressant-like" contributions of TRPV1 receptors against the NC-induced "depression" observed in various types of tobacco abuse...
2011: BMC Pharmacology
https://www.readbyqxmd.com/read/21733180/a-web-server-for-predicting-inhibitors-against-bacterial-target-glmu-protein
#18
Deepak Singla, Meenakshi Anurag, Debasis Dash, Gajendra P S Raghava
BACKGROUND: The emergence of drug resistant tuberculosis poses a serious concern globally and researchers are in rigorous search for new drugs to fight against these dreadful bacteria. Recently, the bacterial GlmU protein, involved in peptidoglycan, lipopolysaccharide and techoic acid synthesis, has been identified as an important drug target. A unique C-terminal disordered tail, essential for survival and the absence of gene in host makes GlmU a suitable target for inhibitor design. RESULTS: This study describes the models developed for predicting inhibitory activity (IC50) of chemical compounds against GlmU protein using QSAR and docking techniques...
2011: BMC Pharmacology
https://www.readbyqxmd.com/read/21619659/synthesis-of-86-species-of-1-5-diaryl-3-oxo-1-4-pentadienes-analogs-of-curcumin-can-yield-a-good-lead-in-vivo
#19
Chieko Kudo, Hiroyuki Yamakoshi, Atsuko Sato, Hiroshi Nanjo, Hisatsugu Ohori, Chikashi Ishioka, Yoshiharu Iwabuchi, Hiroyuki Shibata
BACKGROUND: Curcumin is known to possess many anti-tumor properties such as inhibition of tumor growth and induction of apotosis. However, limited bioavailability of curcumin prevents its clinical application. A synthesized curcumin analog, 1,5-diaryl-3-oxo-1,4-pentadiene such as GO-Y030, has the improved anti-tumor potential in vitro as well as in mouse model of colorectal carcinogenesis. RESULTS: These compounds were divided into two groups; one is the higher anti-proliferative group, in which 79...
2011: BMC Pharmacology
https://www.readbyqxmd.com/read/21473759/altered-5-ht2c-receptor-agonist-induced-responses-and-5-ht2c-receptor-rna-editing-in-the-amygdala-of-serotonin-transporter-knockout-mice
#20
Pablo R Moya, Meredith A Fox, Catherine L Jensen, Justin L Laporte, Helen T French, Jens R Wendland, Dennis L Murphy
BACKGROUND: The serotonin 5-HT2C receptor (5-HT2CR) is expressed in amygdala, a region involved in anxiety and fear responses and implicated in the pathogenesis of several psychiatric disorders such as acute anxiety and post traumatic stress disorder. In humans and in rodent models, there is evidence of both anxiogenic and anxiolytic actions of 5-HT2C ligands. In this study, we determined the responsiveness of 5-HT2CR in serotonin transporter (SERT) knockout (-/-) mice, a model characterized by increased anxiety-like and stress-responsive behaviors...
2011: BMC Pharmacology
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