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An efficient drug delivery vehicle for botulism countermeasureEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusions: An effective BoNT-based drug delivery vehicle can be used to directly deliver toxin inhibitors into intoxicated nerve terminal cytosol. This approach can potentially be utilized for targeted drug delivery to treat other neuronal and neuromuscular disorders. This report also provides new knowledge of endocytosis and exocytosis as well as of BoNT trafficking. (Source: BMC Pharmacology)
Source: BMC Pharmacology - October 27, 2009 Category: Drugs & Pharmacology Authors: Peng ZhangRadharaman RayBal Ram SinghDan LiMichael AdlerPrabhati Ray Source Type: journals

Evaluation of molecular descriptors for antitumor drugs with respect to noncovalent binding to DNA and antiproliferative activityEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusions: For drugs binding reversibly to DNA, both their strength of binding and their cytoxicity are fairly predicted from molecular descriptors by using multiple regression methods. The equations derived may be useful for rational drug design. The results obtained agree with that compounds more active across the National Cancer Institute's 60-cell line data set tend to have common structural features. (Source: BMC Pharmacology)
Source: BMC Pharmacology - September 15, 2009 Category: Drugs & Pharmacology Authors: Jose Portugal Source Type: journals

Psychotropic drugs up-regulate the expression of cholesterol transport proteins including ApoE in cultured human CNS- and liver cellsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusion: Our data show that stimulation of cellular lipid biosynthesis by amphiphilic psychotropic drugs is followed by a transcriptional activation of cholesterol transport and efflux pathways. Such effects may be relevant for both therapeutic effects and metabolic adverse effects of psychotropic drugs. (Source: BMC Pharmacology)
Source: BMC Pharmacology - August 28, 2009 Category: Drugs & Pharmacology Authors: Audun Vik-MoJohan FernoSilje SkredeVidar Steen Source Type: journals

A covalent peptide inhibitor of RGS4 identified in a focused one-bead, one compound library screenEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusions: Though it has some RGS selectivity, 5nd appears to be a partially random cysteine modifier. These data suggest that it inhibits RGS4 by forming disulfide bridges with the protein. (Source: BMC Pharmacology)
Source: BMC Pharmacology - May 22, 2009 Category: Drugs & Pharmacology Authors: Rebecca RoofDavid RomanSamuel ClementsKatarzyna Sobczyk-KojiroLevi BlazerShodai OtaHenry MosbergRichard Neubig Source Type: journals

N-acetylcysteine amide decreases oxidative stress but not cell death induced by doxorubicin in H9c2 cardiomyocytesEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusions: NACA did little to protect NACA H9c2 cells from DOX-induced cell death, even though NACA mitigated the DOX induced decrease of the activities of all of the antioxidant enzymes. These unexpected results suggest that mechanisms not dependent on the production of ROS are involved in DOX induced apoptosis in cardiomyocytes. (Source: BMC Pharmacology)
Source: BMC Pharmacology - April 15, 2009 Category: Drugs & Pharmacology Authors: Rong Shi, Chuan-Chin Huang, Robert S Aronstam, Nuran Ercal, Adam Martin and Yue-wern Huang Source Type: journals

Rapamycin weekly maintenance dosing and the potential efficacy of combination sorafenib plus rapamycin but not atorvastatin or doxycycline in tuberous sclerosis preclinical modelsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Background: Tuberous sclerosis complex (TSC) is an autosomal dominant tumor suppressor syndrome, characterized by hamartomatous growths in the brain, skin, kidneys, lungs, and heart, which lead to significant morbidity. TSC is caused by mutations in the TSC1 or TSC2 genes, whose products, hamartin and tuberin, form a tumor suppressor complex that regulates the PI3K/Akt/mTOR pathway. Early clinical trials show that TSC-related kidney tumors (angiomyolipomas) regress when treated with the mammalian target of rapamycin (mTOR) inhibitor, rapamycin (also known as sirolimus). Although side effects are tolerable, responses are in...
Source: BMC Pharmacology - April 15, 2009 Category: Drugs & Pharmacology Authors: Nancy Lee, Chelsey L Woodrum, Alison M Nobil, Aubrey E Rauktys, Michael P Messina and Sandra L Dabora Source Type: journals

Haloperidol changes mRNA expression of a QKI splice variant in human astrocytoma cellsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusions: The results in U343 cells suggest that QKI-7 mRNA expression in human astrocytes is induced by Haloperidol, at concentrations similar to plasma levels relevant to clinical treatment of schizophrenia. The molecular mechanism of action of antipsychotic drugs after binding to receptors is not well known. We hypothesize that QKI regulation is involved in this mechanism. (Source: BMC Pharmacology)
Source: BMC Pharmacology - March 31, 2009 Category: Drugs & Pharmacology Authors: Lin Jiang, Peter Saetre, Elena Jazin and Eva Lindholm Carlstrom Source Type: journals

Preferential uptake of the non steroid anti-inflammatory drug diclofenac into inflamed tissues after a single oral dose in ratsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusion: This animal study demonstrated that diclofenac and/or its metabolites were rapidly and preferentially taken up and retained in inflamed tissues. Although there were theoretical considerations that mildly acidic NSAID may show some preferential distribution in inflamed tissues there was no clear experimental proof for diclofenac until the present study. (Source: BMC Pharmacology)
Source: BMC Pharmacology - March 16, 2009 Category: Drugs & Pharmacology Authors: A. Schweitzer, N. Hasler-Nguyen and J. Zijlstra Source Type: journals

Bioinformatic characterizations and prediction of K+ and Na+ ion channels effector toxinsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Background: K+ and Na+ channel toxins constitute a large set of polypeptides, which interact with their ion channel targets. These polypeptides are classified in two different structural groups. Recently a new structural group called birtoxin-like appeared to contain both types of toxins has been described. We hypothesized that peptides of this group may contain two conserved structural motifs in K+ and/or Na+ channels scorpion toxins, allowing these birtoxin-like peptides to be active on K+ and/or Na+ channels. Results: Four multilevel motifs, overrepresented and specific to each group of K+ and/or Na+ ion channel toxins ...
Source: BMC Pharmacology - March 10, 2009 Category: Drugs & Pharmacology Authors: Rima Soli, Belhassen Kaabi, Mourad Barhoumi, Mohamed El-Ayeb and Najet Srairi-Abid Source Type: journals

The mode of action of dimeticone 4% lotion against head lice, Pediculus capitisEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusion: This work raises doubts that lice treated using dimeticone preparations die from anoxia despite blockage of the outer respiratory tract because movements can be observed for hours after exposure. However, the blockage inhibits water excretion, which causes physiological stress that leads to death either through prolonged immobilisation or, in some cases, disruption of internal organs such as the gut. (Source: BMC Pharmacology)
Source: BMC Pharmacology - February 20, 2009 Category: Drugs & Pharmacology Authors: Ian F Burgess Source Type: journals

The mode of action of dimeticone 4% lotion against head lice, Pediculus capitis.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusions: This work raises doubts that lice treated using dimeticone preparations die from anoxia despite blockage of the outer respiratory tract because movements can be observed for hours after exposure. However, the blockage inhibits water excretion, which causes physiological stress that leads to death either through prolonged immobilisation or, in some cases, disruption of internal organs such as the gut. (Source: BMC Pharmacology)
Source: BMC Pharmacology - February 20, 2009 Category: Drugs & Pharmacology Authors: Ian F Burgess Source Type: journals

AICAR activates the Pluripotency Transcriptional Network in Embryonic Stem Cells and induces KLF4 and KLF2 Expression in FibroblastsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusions: AICAR is able to activate the molecular circuitry of pluripotency in mESC and to induce the expression of several key regulators of pluripotency in somatic cells. AICAR is therefore a useful pharmacological entity for studying small molecule mediated induction of pluripotency. (Source: BMC Pharmacology)
Source: BMC Pharmacology - February 12, 2009 Category: Drugs & Pharmacology Authors: Luigi Adamo, Yuzhi Zhang and Guillermo Garcia-Cardena Source Type: journals

Conformational changes in α7 acetylcholine receptors underlying allosteric modulation by divalent cationsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Allosteric modulation of membrane receptors is a widespread mechanism by which endogenous and exogenous agents regulate receptor function. For example, several members of the nicotinic receptor family are modulated by physiological concentrations of extracellular calcium ions. In this paper, we examined conformational changes underlying this modulation and compare these with changes evoked by ACh. Two sets of residues in the α7 acetylcholine receptor extracellular domain were mutated to cysteine and analyzed by measuring the rates of modification by the thiol-specific reagent 2-aminoethylmethane thiosulfonate. Using Ba2+ ...
Source: BMC Pharmacology - January 13, 2009 Category: Drugs & Pharmacology Authors: James T McLaughlin, Sean C Barron, Jennifer A See and Robert L Rosenberg Source Type: journals

Conformational changes in alpha 7 acetylcholine receptors underlying allosteric modulation by divalent cationsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusions: : Our data demonstrate that modulation by divalent cations involves substantial conformational changes in the receptor extracellular domain. Our evidence also suggests the modulation occurs via a binding site distinct from one which includes either (or both) of the conserved glutamates at E44 or E172. (Source: BMC Pharmacology)
Source: BMC Pharmacology - January 13, 2009 Category: Drugs & Pharmacology Authors: James T McLaughlin, Sean C Barron, Jennifer A See and Robert L Rosenberg Source Type: journals

Flexible modulation of agonist efficacy at the human A3 adenosine receptor by the imidazoquinoline allosteric enhancer LUF6000Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusions: LUF6000 was found to be an allosteric enhancer of Emax of structurally diverse agonists at the A3 AR, being more effective for low-Emax agonists than for high-Emax agonists. LUF6000 was demonstrated to convert an antagonist into an agonist, which represents the first example in G protein-coupled receptors. The observations from the present study are consistent with that predicted by mathematical modeling. (Source: BMC Pharmacology)
Source: BMC Pharmacology - December 12, 2008 Category: Drugs & Pharmacology Authors: Zhan-Guo Gao, Kai Ye, Aniko Goblyos, Ad P IJzerman and Kenneth A Jacobson Source Type: journals

Substituted trans-stilbenes can inhibit or enhance the TPA-induced up-regulation of activator protein-1Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusions: The ability of trans-stilbenes to inhibit or enhance the effects of TPA does not depend upon their anti-oxidant properties. (Source: BMC Pharmacology)
Source: BMC Pharmacology - November 10, 2008 Category: Drugs & Pharmacology Authors: Lorraine M Deck, Lucy A Hunsaker, Amanda M Gonzales, Robert A Orlando and David L Vander Jagt Source Type: journals

Bioequivalence study of three ibuprofen formulations after single dose administration in healthy volunteersEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Background: This phase I study was designed to determine the bioavailability and bioequivalence of 400 mg Eudorlin(R) extra (Ibuprofen) in comparison to two reference formulations (400 mg Nurofen(R) forte and 400 mg Migranin(R)) after single dose administration under fasting conditions in healthy subjects. Therefore the design of a randomized, open label, multiple sequence cross-over study with a wash-out period of 7-10 days was used. Results: AUC0-t(last) and AUC0-infinity (90%CI) were within the 80 to 125 % interval required for bioequivalence as stipulated in the current regulations of the EMEA. Cmax (90%CI) was within ...
Source: BMC Pharmacology - October 29, 2008 Category: Drugs & Pharmacology Authors: Peter Bramlage and Adrian Goldis Source Type: journals

Alpha-2 adrenergic-induced changes in rectal temperature in adult and 13-day old rats following acute and repeated desipramine administrationEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusions: The results suggest that juvenile rats response differently than adult rats to agonist stimulation of alpha-2 adrenoceptors with and without pretreatment with the antidepressant desipramine. In the absence of desipramine pretreatment, the alpha-2 adrenoceptor-induced hypothermic effect in juvenile rats is greater than in adult rats. Acute injections of desipramine, in the absence of agonist produced a hypothermic effect in adult but not juvenile rats. In addition, the increased alpha-2 agonist-induced hypothermic effect following repeated injections of desipramine that is seen in adult rats is not seen in juve...
Source: BMC Pharmacology - October 2, 2008 Category: Drugs & Pharmacology Authors: Jean D Deupree, William J Burke and David B Bylund Source Type: journals

Methoxylation enhances stilbene bioactivity in Caenorhabditis elegansEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusions: These findings demonstrate that, for the group of stilbenes investigated, methoxylation generally increased bioactivity in vivo in a whole organism, with the exception of pinostilbene. Differences in bioactivity in C. elegans adults did not appear to correlate with differential uptake. Rather, we speculate that methoxylated stilbenes may have increased interactions with biological targets in vivo or may interact with specific targets unaffected by hydroxylated stilbenes. The potent activities of methoxylated stilbenes provide a basis for further investigations to identify in vivo targets for these compounds. (...
Source: BMC Pharmacology - August 13, 2008 Category: Drugs & Pharmacology Authors: Mark A Wilson, Agnes M Rimando and Catherine A Wolkow Source Type: journals

Ameliorative Role of Atorvastatin and Pitavastatin in L-Methionine Induced Vascular Dementia in RatsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusion: The beneficial effects of statins may be attributed to their multiple effects and the study highlights the potential of these drugs in vascular dementia. (Source: BMC Pharmacology)
Source: BMC Pharmacology - August 9, 2008 Category: Drugs & Pharmacology Authors: Rajeshkumar U. Koladiya, Amteshwar S. Jaggi, Nirmal Singh and Bhupesh K Sharma Source Type: journals

A classification model to predict synergism/antagonism of cytotoxic mixtures using protein-drug docking scoresEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusions: Useful classification models can be constructed to predict drug synergism, even in those situations where a limited subset of component drugs can be tested. Compared to the pseudomolecule approach, the virtual docking approach has the advantage of greater potential for biologic interpretation. This distinction may become important as virtual docking software becomes more accurate and docking results more closely resemble actual binding affinities. This is the first published report of a model designed to predict the degree of in-vitro synergism based on the pseudomolecule or docking data approach. (Source: BMC Pharmacology)
Source: BMC Pharmacology - July 29, 2008 Category: Drugs & Pharmacology Authors: John C Boik and Robert A Newman Source Type: journals

Pharmacological Properties of DOV 315,090, an ocinaplon metabolite.Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
We report that DOV 315,090 possesses modulatory activity at GABAA-Rs, but that its selectivity profile is similar to that of ocinaplon. This implies that DOV 315,090 could contribute to the action of ocinaplon in vivo, but that the anxioselective properties of ocinaplon cannot be readily explained by a subtype selective effect/action of DOV 315,090. Further inquiry is required to identify the extent to which different subtypes are involved in the anxiolytic and other pharmacological effects of GABAA-R modulators. (Source: BMC Pharmacology)
Source: BMC Pharmacology - June 13, 2008 Category: Drugs & Pharmacology Authors: Dmytro Berezhnoy, Maria C Gravielle, Scott Downing, Emmanuel Kostakis, Anthony S Basile, Phil Skolnick, Terrell T Gibbs and David H Farb Source Type: journals

Structure-activity models of oral clearance, cytotoxicity, and LD50: a screen for promising anticancer compoundsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusions: Multitask learning can be useful in some QSAR models. A suite of QSAR models was constructed and used to screen a large drug library for compounds likely to be cytotoxic to multiple cancer cell lines in vitro, have low systemic toxicity in rats, and have favorable pharmacokinetic properties in humans. (Source: BMC Pharmacology)
Source: BMC Pharmacology - June 13, 2008 Category: Drugs & Pharmacology Authors: John C. Boik and Robert A. Newman Source Type: journals

Benfotiamine, a synthetic S-acyl thiamine derivative, has different mechanisms of action and a different pharmacological profile than lipid-soluble thiamine disulfide derivativesEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusions: Our results show that, though benfotiamine strongly increases thiamine levels in blood and liver, it has no significant effect in the brain. This would explain why beneficial effects of benfotiamine have only been observed in peripheral tissues, while sulbutiamine, a lipid-soluble thiamine disulfide derivative, that increases thiamine derivatives in the brain as well as in cultured cells, acts as a central nervous system drug. We propose that benfotiamine only penetrates the cells after dephosphorylation by intestinal alkaline phosphatases. It then enters the bloodstream as S-benzoylthiamine that is converted ...
Source: BMC Pharmacology - June 12, 2008 Category: Drugs & Pharmacology Authors: Marie-Laure Volvert, Sandrine Seyen, Marie Piette, Brigitte Evrard, Marjorie Gangolf, Jean-Christophe Plumier and Lucien Bettendorff Source Type: journals

Antagonist affinity measurements at the Gi-coupled human histamine H3 receptor expressed in CHO cellsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusions: In contrast to all three subtypes of the beta-adrenoceptors, but in keeping with the traditional pharmacological dogma, antagonist affinity measurements remained constant at the human H3 receptor, including the medium-efficacy proxyfan-induced state of the receptor and the VUF5681-induced state of the receptor. (Source: BMC Pharmacology)
Source: BMC Pharmacology - June 6, 2008 Category: Drugs & Pharmacology Authors: Jillian G Baker Source Type: journals

Comparison of four different colorimetric and fluorometric cytotoxicity assays in a zebrafish liver cell lineEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusions: We recommend the alamarBlue and CFDA-AM assays for cytotoxicity assessment in ZFL cells, which can be applied either singly or combined. (Source: BMC Pharmacology)
Source: BMC Pharmacology - May 30, 2008 Category: Drugs & Pharmacology Authors: Stephanie K Bopp and Teresa Lettieri Source Type: journals

RU486 did not exacerbate cytokine release in mice challenged with LPS nor in db/db miceEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusions: RU486 at doses that were efficacious in lowering blood glucose did not exacerbate cytokine release in these three mouse models. RU486 actually suppressed the lower dose LPS-mediated TNFalpha release, possibly due to the increased release of glucocorticoids. (Source: BMC Pharmacology)
Source: BMC Pharmacology - May 12, 2008 Category: Drugs & Pharmacology Authors: Baichun Yang, Ryan P Trump, Ying Shen, Judi A McNulty, Lisa G Clifton, Peiyuan Lin, Stephen A Stimpson and Greg L Pahel Source Type: journals

A global view of drug-therapy interactionsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusions: These findings provide for the first time a global map of the large-scale organization of all known drugs and associated therapies, bringing new insights on possible strategies for future drug development. Special attention should be given to drugs which combine the two properties of (a) having a high centrality value in the drug-therapy network and (b) acting on multiple molecular targets in the human system. (Source: BMC Pharmacology)
Source: BMC Pharmacology - March 4, 2008 Category: Drugs & Pharmacology Authors: Jose C Nacher and Jean-Marc Schwartz Source Type: journals

Anti-depressive drugs modulate growth factors in cultured cellsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusion: The antidepressant effects antidepressant drugs might be explained by selective modulation of growth factors, which subsequently affects neuronal plasticity. (Source: BMC Pharmacology)
Source: BMC Pharmacology - March 4, 2008 Category: Drugs & Pharmacology Authors: Andreas W Henkel, Wolfgang Sperling, Andrea Rotter, Udo Reulbach, Cornelia Reichardt, Dominikus Bonsch, Juan M Maler, Johannes Kornhuber and Jens Wiltfang Source Type: journals

Role of sulphated polysaccharides from Sargassum wightii in Cyclosporine A-induced oxidative liver injury in ratsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusions: Thus, the present study highlights that sulphated polysaccharides can act therapeutically against CsA-induced hepatotoxicity. (Source: BMC Pharmacology)
Source: BMC Pharmacology - February 20, 2008 Category: Drugs & Pharmacology Authors: Anthony Josephine, Kalaiselvam Nithya, Ganapathy Amudha, Coothan KANDASWAMY Veena, Sreenivasan P Preetha and Palaninathan Varalakshmi Source Type: journals

Inhibition of 11beta HSD1 with the S-phenylethylaminothiazolone BVT116429 increases adiponectin concentrations and improves glucose homeostasis in diabetic KKAy miceEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusion: Inhibition of 11beta HSD1 can be expected to be beneficial for treating the pathology of type 2 diabetes mellitus. The differences seen in adiponectin between BVT116429 and BVT2733 could be explained by different pharmacodynamics exerted by the compounds in different tissues in the body. Increases in adiponectin concentrations may be an integral component in the mechanism of action of this new 11beta HSD1 inhibitor and may be a useful marker of efficacy during the clinical development of 11beta HSD1 inhibitor compounds. (Source: BMC Pharmacology)
Source: BMC Pharmacology - February 12, 2008 Category: Drugs & Pharmacology Authors: Maj Sundbom, Christina Kaiser, Eva Bjorkstrand, Victor M Castro, Catarina Larsson, Goran Selen, Charlotta Soderberg Nyhem and Stephen R James Source Type: journals

Comparative study of the antimutagenic properties of vitamin C and E on mutations induced by norfloxacinEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Background: Norfloxacin NOR , as other flour-quinolones, is known to be mutagenic on Salmonella typhimurium TA102 strain. This mutagenic effect is due to free oxygen radicals (ROS), as it is inhibited by antioxidants such as -carotene and natural occurring antioxidants of Roheo discolor and other plants. The aim of this work is to evaluate the combined therapy of norfloxacin and vitamins C and E as an alternative to reduce possible genotoxic risk due to fluoroquinolones treatment. Results: The antimutagenicity of -tocoferol (E) and ascorbic acid (C) was evaluated on the S. typhimurium TA102 employing the aroclor-1254 in...
Source: BMC Pharmacology - February 11, 2008 Category: Drugs & Pharmacology Authors: Myriam Arriaga-Alba, Roberto Rivera-Sanchez, Nancy Ruiz-Perez, Jaime Sanchez-Navarrete, Rocio Flores-Paz, Araceli Montoya Estrada and Juan Jose Hicks Gomez Source Type: journals

Dicholine salt of succinic acid, a neuronal insulin sensitizer, ameliorates cognitive deficits in rodent models of normal aging, chronic cerebral hypoperfusion, and beta-amyloid peptide-(25-35)-induced amnesiaEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusions: The results of the present study suggest that dicholine salt of succinic acid, a novel neuronal insulin sensitizer, ameliorates cognitive deficits and neuronal dysfunctions in animal models relevant to age-related cognitive impairments, vascular dementia, and Alzheimers disease. (Source: BMC Pharmacology)
Source: BMC Pharmacology - January 23, 2008 Category: Drugs & Pharmacology Authors: Zinaida I Storozheva, Andrey T Proshin, Vladimir V Sherstnev, Tatiana P Storozhevykh, Yana E Senilova, Nadezhda A Persiyantseva, Vsevolod G Pinelis, Natalia A Semenova, Elena I Zakharova and Igor A Pomytkin Source Type: journals

The presence of beta2-adrenoceptors sensitizes alpha2A-adrenoceptors to desensitization after chronic epinephrine treatmentEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusions: This study further supports the hypothesis that the presence of the beta-AR renders the alpha2A-AR more susceptible to desensitization with physiological levels of EPI. (Source: BMC Pharmacology)
Source: BMC Pharmacology - December 20, 2007 Category: Drugs & Pharmacology Authors: Tasneem Bawa-Khalfe, Ghazi F Altememi, Chitra D Mandyam, Lindsay A Schwarz, Douglas C Eikenburg and Kelly M Standifer Source Type: journals

Chlorin e6 - polyvinylpyrrolidone mediated photosensitization is effective against human non-small cell lung carcinoma compared to small cell lung carcinoma xenograftsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusion: The formulation of Ce6-PVP is distinctly advantageous as a diagnostic and therapeutic agent for fluorescence diagnosis and PDT of NSCLC. (Source: BMC Pharmacology)
Source: BMC Pharmacology - December 1, 2007 Category: Drugs & Pharmacology Authors: William WL Chin, Paul WS Heng and Malini Olivo Source Type: journals

Tuberous sclerosis preclinical studies: timing of treatment, combination of a rapamycin analog (CCI-779) and interferon-gamma, and comparison of rapamycin to CCI-779Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusions: Preventing the genesis of TSC-related kidney lesions in Tsc2+/- mice is not an effective treatment strategy; rather, the presence of growing tumors appears to be the most important factor when determining an appropriate treatment schedule. Treatment with rapamycin was more effective in reducing tumor growth and improving survival in nude mice bearing Tsc2-/- tumors and also resulted in higher rapamycin levels in blood, brain, and kidney tissue than treatment with an equal milligram dose of CCI-779. We anticipate these results will influence future preclinical and clinical trials for TSC. (Source: BMC Pharmacology)
Source: BMC Pharmacology - November 6, 2007 Category: Drugs & Pharmacology Authors: Michael P Messina, Aubrey Rauktys, Laifong Lee and Sandra L Dabora Source Type: journals

Impact of imatinib on the pharmacokinetics and in vivo efficacy of etoposide and/or ifosfamideEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusions: Altogether, these results therefore justify further prospective phase I and II clinical trials with combinations of etoposide-based chemotherapy and imatinib in patients with certain cancers, such as malignant lymphoma, with careful toxicologic monitoring. (Source: BMC Pharmacology)
Source: BMC Pharmacology - October 27, 2007 Category: Drugs & Pharmacology Authors: Keyvan Rezai, Francois Lokiec, Isabelle Grandjean, Sophie Weill, Patricia de Cremoux, Vincent Bordier, Richard Ekue, Mickael Garcia, Marie-France Poupon and Didier Decaudin Source Type: journals

Ciclesonide uptake and metabolism in human alveolar type II epithelial cells (A549)Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusions: Uptake of ciclesonide into A549 cells was more efficient than that of the less lipophilic fluticasone propionate. Intracellular concentrations of the pharmacologically active metabolite des-CIC were maintained for up to 24 h. The local anti-inflammatory activity of ciclesonide in the lung may be prolonged by the slow release of active drug from the depot of fatty acid esters. (Source: BMC Pharmacology)
Source: BMC Pharmacology - September 27, 2007 Category: Drugs & Pharmacology Authors: Takashi Nonaka, Ruediger Nave, Nigel McCracken, Atsuko Kawashimo and Yasuhiro Katsuura Source Type: journals

Gene expression profiling reveals effects of Cimicifuga racemosa (L.) NUTT. (black cohosh) on the estrogen receptor positive human breast cancer cell line MCF-7Email this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusion: No estrogenic but antiproliferative and proapoptotic gene expression was shown for black cohosh in MCF-7 cells at the transcriptional level. The effects may be results of the activation of different pathways. The cycloartane glycosides and - for the first time - their aglycons could be identified as an active principle in black cohosh. (Source: BMC Pharmacology)
Source: BMC Pharmacology - September 20, 2007 Category: Drugs & Pharmacology Authors: Friedemann Gaube, Stefan Wolfl, Larissa Pusch, Torsten C Kroll and Matthias Hamburger Source Type: journals

An integrative in silico approach for discovering candidates for drug-targetable protein-protein interactions in interactome dataEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusions: An integrative in silico approach for discovering candidates for drug-targetable PPIs was applied to original human PPIs data. The system excludes false positive interactions and selects reliable PPIs as drug targets. Its effectiveness was demonstrated by the discovery of the six promising candidate target PPIs. Inhibition or stabilization of the two interactions may have potential therapeutic effects against human diseases. (Source: BMC Pharmacology)
Source: BMC Pharmacology - August 20, 2007 Category: Drugs & Pharmacology Authors: Nobuyoshi Sugaya, Kazuyoshi Ikeda, Toshiyuki Tashiro, Shizu Takeda, Jun Otomo, Yoshiko Ishida, Akiko Shiratori, Atsushi Toyoda, Hideki Noguchi, Tadayuki Takeda, Satoru Kuhara, Yoshiyuki Sakaki and Takao Iwayanagi Source Type: journals

Structural and functional definition of the specificity of a novel caspase-3 inhibitor, Ac-DNLD-CHOEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusions: On the basis of our results, we conclude that Ac-DNLD-CHO is a reliable, potent and selective inhibitor of caspase-3. The specific inhibitory effect on caspase-3 suggests that this inhibitor could become an important tool for investigations of the biological function of caspase-3. Furthermore, Ac-DNLD-CHO may be an attractive lead compound to generate novel effective non-peptidic pharmaceuticals for caspase-mediated apoptosis diseases, such as neurodegenerative disorders and viral infection diseases. (Source: BMC Pharmacology)
Source: BMC Pharmacology - June 27, 2007 Category: Drugs & Pharmacology Authors: Atsushi Yoshimori, Junichi Sakai, Satoshi Sunaga, Takanobu Kobayashi, Satoshi Takahashi, Naoyuki Okita, Ryoko Takasawa and Sei-ichi Tanuma Source Type: journals

Uptake and metabolism of ciclesonide and retention of desisobutyryl-ciclesonide for up to 24 hours in rabbit nasal mucosaEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusion: These data suggest that a hypotonic ciclesonide suspension provides higher intracellular concentrations of des-CIC up to 24 h, thereby providing a rationale for investigation of ciclesonide as a convenient once-daily nasal spray for treatment of allergic rhinitis. (Source: BMC Pharmacology)
Source: BMC Pharmacology - June 6, 2007 Category: Drugs & Pharmacology Authors: Hideyuki Sato, Ruediger Nave, Takashi Nonaka, Nishibe Yoshihisa, Nagano Atsuhiro, Tsutomu Mochizuki, Shigehiro Takahama, Shiro Kondo and Mark Wingertzahn Source Type: journals

The enantiomers of tramadol and its major metabolite inhibit peristalsis in the guinea pig small intestine via differential mechanismsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusions: The results show that the metabolite O-desmethyltramadol is more potent in inhibiting peristalsis than its parent compound. The action of all tramadol forms depends on opioid receptors, and that of (+)- and (-)-tramadol also involves adrenoceptors. (Source: BMC Pharmacology)
Source: BMC Pharmacology - March 16, 2007 Category: Drugs & Pharmacology Authors: Michael K Herbert, Rebecca Weis and Peter Holzer Source Type: journals

In rats, oral oleoyl-DHEA is rapidly hydrolyzed and converted to DHEA-sulphateEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusion: The esterase activities found may condition the pharmacological availability (and depot effect) of orally administered steroid hormone fatty acid esters such as oleoyl-DHEA. The oral administration of oleoyl-DHEA in order to extend DHEA plasma availability has not been proved effective, since the ester is rapidly hydrolysed, probably in the intestine itself, and mainly converted to DHEA-sulfate at least in females. (Source: BMC Pharmacology)
Source: BMC Pharmacology - March 9, 2007 Category: Drugs & Pharmacology Authors: Marta Serrano, Maria del Mar Grasa, Jose Antonio Fernandez-Lopez and Maria Alemany Source Type: journals

Mapping the contribution of beta3-containing GABAAreceptors to volatile and intravenous general anesthetic actionsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusion: Our results provide evidence for a defined role of beta3-containing GABA(A) receptors in mediating some, but not all, of the actions of general anesthetics, and confirming the multisite model of general anesthetic action. This pharmacological separation of anesthetic endpoints also suggests that subtype-selective substances with an improved side-effect profile may be developed. (Source: BMC Pharmacology)
Source: BMC Pharmacology - February 24, 2007 Category: Drugs & Pharmacology Authors: Anja Zeller, Margarete Arras, Rachel Jurd and Uwe Rudolph Source Type: journals

A comparative study of the actions of alkylpyridinium salts from a marine sponge and related synthetic compounds in rat cultured hippocampal neuronsEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusions: Poly-APS induced pore formation in hippocampal neurones and such pores were transient, with neurones recovering from exposure to these polymers. Synthetic structurally related oligomers were not potent pore formers when compared to poly-APS and affected a smaller percentage of the hippocampal neurone population. Poly-APS may have potential as agents for macromolecular delivery into CNS neurones however; the smaller synthetic oligomers tested in this study show little potential for such use. This comparative analysis indicated that the level of polymerisation giving rise to the supermolecular structure in the n...
Source: BMC Pharmacology - February 2, 2007 Category: Drugs & Pharmacology Authors: David J Koss, Kathleen P Hindley, Kanola C David, Ines Mancini, Graziano Guella, Kristina Sepcic, Tom Turk, Katja Rebolj, Gernot Riedel, Bettina Platt and Roderick H Scott Source Type: journals

A comparative study of the actions of alkylpyridinium salts from a marine sponge and related synthetic compounds in rat cultured hippocampal neuronesEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
Conclusion: Poly-APS induced pore formation in hippocampal neurones and such pores were transient, with neurones recovering from exposure to these polymers. Synthetic structurally related oligomers were not potent pore formers when compared to poly-APS and affected a smaller percentage of the hippocampal neurone population. Poly-APS may have potential as agents for macromolecular delivery into CNS neurones however; the smaller synthetic oligomers tested in this study show little potential for such use. This comparative analysis indicated that the level of polymerisation giving rise to the supermolecular structure in the na...
Source: BMC Pharmacology - February 2, 2007 Category: Drugs & Pharmacology Authors: David J Koss, Kathleen P Hindley, Kanola C David, Ines Mancini, Graziano Guella, Kristina Sepčić, Tom Turk, Katja Rebolj, Gernot Riedel, Bettina Platt and Roderick H Scott Source Type: journals

Correction: Identification of specific calcitonin-like receptor residues important for calcitonin gene-related peptide high affinity bindingEmail this article to a colleague. Save this article to My Clippings. Discuss or comment on this article.
This is a correction article.After publication of this work 1, we became aware of the fact that Robert C. Speth was not included as an author. Dr. Speth put a considerable amount of time and effort into developing and preparing the radiopeptide used to carry out the radioligand binding studies reported in this manuscript and therefore should have originally been included as an author. We apologize to Dr. Speth for any inconvenience that this oversight might have caused and thank him for his invaluable contribution to this project. (Source: BMC Pharmacology)
Source: BMC Pharmacology - December 6, 2006 Category: Drugs & Pharmacology Authors: Sugato Banerjee, Janel Evanson, Erik Harris, Stephen L Lowe, Robert C Speth, Kathryn A Thomasson and James E Porter Source Type: journals