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Pharmacology of Novel Heteroaromatic Polycycle Antibacterials

Gross, M.; Bürli, R.; Jones, P.; Garcia, M.; Batiste, B.; Kaizerman, J.; Moser, H.; Jiang, V.; Hoch, U.; Duan, J.-X.; Tanaka, R.; Johnson, K. W.
Fonte: American Society for Microbiology Publicador: American Society for Microbiology
Tipo: Artigo de Revista Científica
Publicado em /11/2003 EN
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36.53%
Heteroaromatic polycycle (HARP) compounds are a novel class of small (Mw, 600 to 650) DNA-binding antibacterials. HARP compounds exhibit a novel mechanism of action by preferentially binding to AT-rich sites commonly found in bacterial promoters and replication origins. Noncovalent binding in the minor groove of DNA results in inhibition of DNA replication and DNA-dependent RNA transcription and subsequent bacterial growth. HARP compounds have previously been shown to have potent in vitro activities against a broad spectrum of gram-positive organisms. The present report describes the extensive profiling of the in vitro and in vivo pharmacology of HARP antibacterials. The efficacies of representative compounds (GSQ-2287, GSQ-10547, and GSQ-11203), which exhibited good MIC activity, were tested in murine lethal peritonitis and neutropenic thigh infection models following intravenous (i.v.) administration. All compounds were efficacious in vivo, with potencies generally correlating with MICs. GSQ-10547 was the most potent compound in vitro and in vivo, with a 50% effective dose in the murine lethal peritonitis model of 7 mg/kg of body weight against methicillin-sensitive Staphylococcus aureus (MSSA) and 13 mg/kg against methicillin-resistant S. aureus (MRSA). In the neutropenic mouse thigh infection model...

Behavioural pharmacology: 40+ years of progress, with a focus on glutamate receptors and cognition

Robbins, Trevor W.; Murphy, Emily R.
Fonte: Published By Elsevier In Association With The International Union Of Pharmacology Publicador: Published By Elsevier In Association With The International Union Of Pharmacology
Tipo: Artigo de Revista Científica
Publicado em /03/2006 EN
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Behavioural pharmacology is an interdisciplinary field at the intersection of several research areas that ultimately lead to the development of drugs for clinical use and build understanding of how brain functions enable cognition and behaviour. In this article, the development of behavioural pharmacology in the UK is briefly surveyed, and the current status and success of the field is highlighted by the progress in our understanding of learning and memory that has resulted from discoveries in glutamate receptor pharmacology allied to theoretical and methodological advances in behavioural neuroscience. We describe the original breakthrough in terms of the role of NMDA receptors in hippocampal-mediated spatial learning and long-term potentiation, and review recent advances that demonstrate the involvement of glutamate receptor in working memory, recognition memory, stimulus–response learning and memory, and higher cognitive functions. We also discuss the unique functions of NMDA receptors and the fundamental role of AMPA receptors in processes that are common to some of these forms of memory, including encoding, consolidation and retrieval.

Pharmacology under the microscope: the use of fluorescence correlation spectroscopy to determine the properties of ligand–receptor complexes

Briddon, Stephen J.; Hill, Stephen J.
Fonte: Published By Elsevier In Association With The International Union Of Pharmacology Publicador: Published By Elsevier In Association With The International Union Of Pharmacology
Tipo: Artigo de Revista Científica
Publicado em /12/2007 EN
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Recent years have revealed a high degree of structural organisation in the way in which cell-surface receptors and their associated signalling complexes interact at a molecular level. Fluorescence-based techniques have been at the forefront of methodologies used to investigate this organisation and dissect the pharmacology of drug–receptor interactions at the single-cell level. One such technique, fluorescence correlation spectroscopy (FCS), in conjunction with a fluorescent ligand or receptor, is capable of providing quantitative information about the number of receptors and their mobilities within small areas of the cell membrane that approach the size of some signalling domains. This article describes the use of FCS to perform subcellular quantitative pharmacology, with particular reference to G-protein-coupled receptors (GPCRs). In conjunction with other forms of fluctuation analysis, such as two-colour cross-correlation FCS and molecular brightness analysis, FCS provides the first opportunity to investigate the domain-specific nature of GPCR pharmacology.

Effect of HIV-1 Infection and Sex on the Cellular Pharmacology of the Antiretroviral Drugs Zidovudine and Lamivudine

Rower, Joseph E.; Meditz, Amie; Gardner, Edward M.; Lichtenstein, Kenneth; Predhomme, Julie; Bushman, Lane R.; Klein, Brandon; Zheng, Jia-Hua; MaWhinney, Samantha; Anderson, Peter L.
Fonte: American Society for Microbiology Publicador: American Society for Microbiology
Tipo: Artigo de Revista Científica
Publicado em /06/2012 EN
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The cellular pharmacology of zidovudine (ZDV) and lamivudine (3TC) in vivo is not completely understood. This prospective longitudinal study investigated the relationship between HIV-1 serostatus, sex, race, and time on therapy with intracellular and plasma ZDV and 3TC concentrations. Of 20 HIV-seronegative and 23 HIV-seropositive volunteers enrolled, 16 (8 women) and 21 (5 women) completed all 12 study days, respectively. Volunteers began ZDV-3TC therapy (plus a third active drug in HIV-seropositive volunteers), and steady-state concentrations (Css) were determined after days 1, 3, 7, and 12. A repeated-measures mixed model was utilized. HIV-seronegative status was associated with 22% (95% confidence interval [CI], 0%, 50%) and 37% (15%, 67%) higher Css estimates compared to those of HIV-seropositive individuals for intracellular ZDV-TP and 3TC-TP levels, respectively. African-Americans had 36% (8%, 72%) higher ZDV-TP estimates than non-African-Americans. Sex was not associated with ZDV-TP or 3TC-TP (P > 0.19). Women had 36% (4%, 78%) higher plasma ZDV, but the effect was lessened when normalized by lean body weight (5% [−19%, 38%]; P = 0.68). Plasma 3TC was 19% (0%, 41%) higher in HIV-seropositive volunteers and 22% (0%, 48%) higher in African American volunteers...

Integrating pharmacology and clinical pharmacology in universities

Buckingham, Julia C
Fonte: Blackwell Science Inc Publicador: Blackwell Science Inc
Tipo: Artigo de Revista Científica
EN
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36.66%
Continuing development of safe and effective new medicines is critically important for global health, social prosperity and the economy. The drug discovery–development pipeline depends critically on close partnerships between scientists and clinicians and on educational programmes that ensure that the pharmacological workforce, in its broadest sense, is fit for purpose. Here I consider factors that have influenced the development of basic and clinical pharmacology in UK universities over the past 40 years and discuss ways in which basic pharmacologists, clinical pharmacologists and scientists from different disciplines can work together effectively, while retaining their professional identities and fostering developments in their disciplines. Specifically, I propose the establishment of Institutes of Drug Discovery and Development, whose activities could include development and implementation of a translational pharmacology research strategy, drawing on the collective expertise of the membership and the university as whole; provision of a forum for regular seminars and symposia to promote the discipline, encourage collaboration and develop a cohesive community; provision of a research advisory service, covering, for example, data management...

How should teaching of undergraduates in clinical pharmacology and therapeutics be delivered and assessed?

Maxwell, Simon R J
Fonte: Blackwell Science Inc Publicador: Blackwell Science Inc
Tipo: Artigo de Revista Científica
EN
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Clinical pharmacology and therapeutics is the academic discipline that informs rational prescribing of medicines. There is accumulating evidence that a significant minority of prescriptions in the UK National Health Service contain errors. This comes at a time when the approach to and success of undergraduate education in this area has been called into question. Various stakeholders are now in agreement that this challenging area of undergraduate education needs to be strengthened. The principles that should form the basis of future educational strategy include greater visibility of clinical pharmacology and therapeutics in the curriculum, clear learning outcomes that are consistent with national guidance, strong and enthusiastic leadership, a student formulary, opportunities to practice prescribing, a robust assessment of prescribing competencies and external quality control. Important new developments in the UK are Prescribe, a repository of e-learning materials to support education in clinical pharmacology and prescribing, and the Prescribing Skills Assessment, a national online assessment designed to allow medical students to demonstrate that they have achieved the core competencies required to begin postgraduate training.

Lung Function Measurements in Rodents in Safety Pharmacology Studies

Hoymann, Heinz Gerd
Fonte: Frontiers Research Foundation Publicador: Frontiers Research Foundation
Tipo: Artigo de Revista Científica
Publicado em 28/08/2012 EN
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36.66%
The ICH guideline S7A requires safety pharmacology tests including measurements of pulmonary function. In the first step – as part of the “core battery” – lung function tests in conscious animals are requested. If potential adverse effects raise concern for human safety, these should be explored in a second step as a “follow-up study”. For these two stages of safety pharmacology testing, both non-invasive and invasive techniques are needed which should be as precise and reliable as possible. A short overview of typical in vivo measurement techniques is given, their advantages and disadvantages are discussed and out of these the non-invasive head-out body plethysmography and the invasive but repeatable body plethysmography in orotracheally intubated rodents are presented in detail. For validation purposes the changes in the respective parameters such as tidal midexpiratory flow (EF50) or lung resistance have been recorded in the same animals in typical bronchoconstriction models and compared. In addition, the technique of head-out body plethysmography has been shown to be useful to measure lung function in juvenile rats starting from day two of age. This allows safety pharmacology testing and toxicological studies in juvenile animals as a model for the young developing organism as requested by the regulatory authorities (e.g....

Pharmacology and Structure of Isolated Conformations of the Adenosine A2A Receptor Define Ligand Efficacy

Bennett, Kirstie A.; Tehan, Benjamin; Lebon, Guillaume; Tate, Christopher G.; Weir, Malcolm; Marshall, Fiona H.; Langmead, Christopher J.
Fonte: The American Society for Pharmacology and Experimental Therapeutics Publicador: The American Society for Pharmacology and Experimental Therapeutics
Tipo: Artigo de Revista Científica
EN
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Using isolated receptor conformations crystal structures of the adenosine A2A receptor have been solved in active and inactive states. Studying the change in affinity of ligands at these conformations allowed qualitative prediction of compound efficacy in vitro in a system-independent manner. Agonist 5′-N-ethylcarboxamidoadenosine displayed a clear preference to bind to the active state receptor; inverse agonists (xanthine amine congener, ZM241385, SCH58261, and preladenant) bound preferentially to the inactive state, whereas neutral antagonists (theophylline, caffeine, and istradefylline) demonstrated equal affinity for active and inactive states. Ligand docking into the known crystal structures of the A2A receptor rationalized the pharmacology observed; inverse agonists, unlike neutral antagonists, cannot be accommodated within the agonist-binding site of the receptor. The availability of isolated receptor conformations opens the door to the concept of “reverse pharmacology” whereby the functional pharmacology of ligands can be characterized in a system-independent manner by their affinity for a pair (or set) of G protein–coupled receptor conformations.

The Pharmacology of Regenerative Medicine

Christ, George J.; Saul, Justin M.; Furth, Mark E.; Andersson, Karl-Erik
Fonte: The American Society for Pharmacology and Experimental Therapeutics Publicador: The American Society for Pharmacology and Experimental Therapeutics
Tipo: Artigo de Revista Científica
EN
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36.66%
Regenerative medicine is a rapidly evolving multidisciplinary, translational research enterprise whose explicit purpose is to advance technologies for the repair and replacement of damaged cells, tissues, and organs. Scientific progress in the field has been steady and expectations for its robust clinical application continue to rise. The major thesis of this review is that the pharmacological sciences will contribute critically to the accelerated translational progress and clinical utility of regenerative medicine technologies. In 2007, we coined the phrase “regenerative pharmacology” to describe the enormous possibilities that could occur at the interface between pharmacology, regenerative medicine, and tissue engineering. The operational definition of regenerative pharmacology is “the application of pharmacological sciences to accelerate, optimize, and characterize (either in vitro or in vivo) the development, maturation, and function of bioengineered and regenerating tissues.” As such, regenerative pharmacology seeks to cure disease through restoration of tissue/organ function. This strategy is distinct from standard pharmacotherapy, which is often limited to the amelioration of symptoms. Our goal here is to get pharmacologists more involved in this field of research by exposing them to the tools...

International Union of Pharmacology. LXXXIX. Update on the Extended Family of Chemokine Receptors and Introducing a New Nomenclature for Atypical Chemokine Receptors

Bachelerie, Francoise; Ben-Baruch, Adit; Burkhardt, Amanda M.; Combadiere, Christophe; Farber, Joshua M.; Graham, Gerard J.; Horuk, Richard; Sparre-Ulrich, Alexander Hovard; Locati, Massimo; Luster, Andrew D.; Mantovani, Alberto; Matsushima, Kouji; Murphy
Fonte: The American Society for Pharmacology and Experimental Therapeutics Publicador: The American Society for Pharmacology and Experimental Therapeutics
Tipo: Artigo de Revista Científica
EN
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36.6%
Sixteen years ago, the Nomenclature Committee of the International Union of Pharmacology approved a system for naming human seven-transmembrane (7TM) G protein-coupled chemokine receptors, the large family of leukocyte chemoattractant receptors that regulates immune system development and function, in large part by mediating leukocyte trafficking. This was announced in Pharmacological Reviews in a major overview of the first decade of research in this field [Murphy PM, Baggiolini M, Charo IF, Hébert CA, Horuk R, Matsushima K, Miller LH, Oppenheim JJ, and Power CA (2000) Pharmacol Rev 52:145–176]. Since then, several new receptors have been discovered, and major advances have been made for the others in many areas, including structural biology, signal transduction mechanisms, biology, and pharmacology. New and diverse roles have been identified in infection, immunity, inflammation, development, cancer, and other areas. The first two drugs acting at chemokine receptors have been approved by the U.S. Food and Drug Administration (FDA), maraviroc targeting CCR5 in human immunodeficiency virus (HIV)/AIDS, and plerixafor targeting CXCR4 for stem cell mobilization for transplantation in cancer, and other candidates are now undergoing pivotal clinical trials for diverse disease indications. In addition...

The pharmacology of TRP channels

Holzer, Peter; Izzo, Angelo A
Fonte: Blackwell Publishing Ltd Publicador: Blackwell Publishing Ltd
Tipo: Artigo de Revista Científica
EN
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36.6%
This themed issue of the British Journal of Pharmacology contains review and research articles on recent advances in transient receptor potential (TRP) channel pharmacology. The review articles, written by a panel of distinguished experts, address the rapid progress in TRP channel research in fields as diverse as oncology, urology, dermatology, migraine, inflammation and pain. These reviews are complemented by original research reports focusing, among others, on the emerging roles of TRPV1 in osteoporosis and cystitis and on evodiamine as a lead structure for the development of potent TRPV1 agonists/desensitizers. Other papers highlight the differences in TRPV3 pharmacology between recombinant and native systems, the mechanisms of TRPM3 activation/inhibition and TRPP2 as a target of naringenin, a dietary flavonoid with anticancer actions. New therapeutic opportunities in pain may arise from the strategy to combine TRP channel and cell membrane impermeant sodium channel blockers to inhibit sensory nerve activity.

Benefits of a Pharmacology Antimalarial Reference Standard and Proficiency Testing Program Provided by the Worldwide Antimalarial Resistance Network (WWARN)

Lourens, Chris; Lindegardh, Niklas; Barnes, Karen I.; Guerin, Philippe J.; Sibley, Carol H.; White, Nicholas J.; Tarning, Joel
Fonte: American Society for Microbiology Publicador: American Society for Microbiology
Tipo: Artigo de Revista Científica
Publicado em /07/2014 EN
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Comprehensive assessment of antimalarial drug resistance should include measurements of antimalarial blood or plasma concentrations in clinical trials and in individual assessments of treatment failure so that true resistance can be differentiated from inadequate drug exposure. Pharmacometric modeling is necessary to assess pharmacokinetic-pharmacodynamic relationships in different populations to optimize dosing. To accomplish both effectively and to allow comparison of data from different laboratories, it is essential that drug concentration measurement is accurate. Proficiency testing (PT) of laboratory procedures is necessary for verification of assay results. Within the Worldwide Antimalarial Resistance Network (WWARN), the goal of the quality assurance/quality control (QA/QC) program is to facilitate and sustain high-quality antimalarial assays. The QA/QC program consists of an international PT program for pharmacology laboratories and a reference material (RM) program for the provision of antimalarial drug standards, metabolites, and internal standards for laboratory use. The RM program currently distributes accurately weighed quantities of antimalarial drug standards, metabolites, and internal standards to 44 pharmacology, in vitro...

Antibacterial mechanisms identified through structural systems pharmacology

Chang, Roger L; Xie, Lei; Bourne, Philip E; Palsson, Bernhard O
Fonte: BioMed Central Publicador: BioMed Central
Tipo: Artigo de Revista Científica
EN_US
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36.6%
Background: The growing discipline of structural systems pharmacology is applied prospectively in this study to predict pharmacological outcomes of antibacterial compounds in Escherichia coli K12. This work builds upon previously established methods for structural prediction of ligand binding pockets on protein molecules and utilizes and expands upon the previously developed genome scale model of metabolism integrated with protein structures (GEM-PRO) for E. coli, structurally accounting for protein complexes. Carefully selected case studies are demonstrated to display the potential for this structural systems pharmacology framework in discovery and development of antibacterial compounds. Results: The prediction framework for antibacterial activity of compounds was validated for a control set of well-studied compounds, recapitulating experimentally-determined protein binding interactions and deleterious growth phenotypes resulting from these interactions. The antibacterial activity of fosfomycin, sulfathiazole, and trimethoprim were accurately predicted, and as a negative control glucose was found to have no predicted antibacterial activity. Previously uncharacterized mechanisms of action were predicted for compounds with known antibacterial properties...

HST.151 Principles of Pharmacology, Spring 2003; Principles of Pharmacology

Rosow, Carl E. (Carl Elliott), 1947-; Standaert, David; Strichartz, G. R. (Gary R.), 1943-; Dershwitz, Mark; Di Salvo, Thomas; Ko, Dickens; Kufe, Donald; Langer, Robert S.; Lees, Robert S.; Rubin, Robert H., 1941-; Ruskin, Jeremy N.; Tepper, Robert; Walsh
Fonte: MIT - Massachusetts Institute of Technology Publicador: MIT - Massachusetts Institute of Technology
EN-US
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36.6%
An introduction to pharmacology. Topics include mechanisms of drug action, dose-response relations, pharmacokinetics, drug delivery systems, drug metabolism, toxicity of pharmacological agents, drug interactions, and substance abuse. Selected agents and classes of agents examined in detail. (Only HST students may register under HST.150, graded P/D/F.) From the course home page: Course Description The objective of this course is to teach and approach to the study of pharmacologic agents. It is not intended to be a review of the pharmacopoeia nor is it intended to be a replace dicussions of relevant drugs in the organ systems HST pathophysiology courses.

An evaluation of pharmacology curricula in Australian science and health-related degree programs

Lloyd, H.; Hinton, T.; Bullock, S.; Babey, A.M.; Davis, E.; Fernandes, L.; Hart, J.; Musgrave, I.; Ziogas, J.
Fonte: BioMed Central Ltd. Publicador: BioMed Central Ltd.
Tipo: Artigo de Revista Científica
Publicado em //2013 EN
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36.78%
Background: Pharmacology is a biomedical discipline taught in basic science and professional degree programs. In order to provide information that would facilitate pharmacology curricula to be refined and developed, and approaches to teaching to be updated, a national survey was undertaken in Australia that investigated pharmacology course content, teaching and summative assessment methods. Methods: Twenty-two institutions participated in a purpose-built online questionnaire, which enabled an evaluation of 147 courses taught in 10 different degrees. To enable comparison, degrees were grouped into four major degree programs, namely science, pharmacy, medicine and nursing. The pharmacology content was then classified into 16 lecture themes, with 2-21 lecture topics identified per theme. The resultant data were analysed for similarities and differences in pharmacology curricula across the degree programs. Results: While all lecture themes were taught across degree programs, curriculum content differed with respect to the breadth and hours of coverage. Overall, lecture themes were taught most broadly in medicine and with greatest coverage in pharmacy. Reflecting a more traditional approach, lectures were a dominant teaching method (at least 90% of courses). Sixty-three percent of science courses provided practical classes but such sessions occurred much less frequently in other degree programs...

Social pharmacology: expanding horizons

Maiti, Rituparna; Alloza, José‑Luis
Fonte: Wolters Kluwer Publicador: Wolters Kluwer
Tipo: Artigo de Revista Científica Formato: application/pdf
ENG
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In the current modern and global society, social changes are in constant evolution due to scientific progress (technology, culture, customs, and hygiene) and produce the freedom in individuals to take decisions by themselves or with their doctors toward drug consumption. In the arena of marketed drug products which includes society, individual, administration, and pharmaceutical industry, the young discipline emerged is social pharmacology or sociopharmacology. This science arises from clinical pharmacology, and deals with different parameters, which are important in creating knowledge on marketed drugs. However, the scope of “social pharmacology” is not covered by the so‑called “Phase IV” alone, but it is the science that handles the postmarketing knowledge of drugs. The social pharmacology studies the “life cycle” of any marketed pharmaceutical product in the social terrain, and evaluates the effects of the real environment under circumstances totally different in the drug development process. Therefore, there are far‑reaching horizons, plural, and shared predictions among health professionals and other, for beneficial use of a drug, toward maximizing the benefits of therapy, while minimizing negative social consequences.

A Multi-Level Analysis of World Scientific Output in Pharmacology

Olmeda-Gómez, Carlos; Ovalle-Perandones, María Antonia; Perianes-Rodríguez, Antonio
Fonte: Intech Publicador: Intech
Tipo: info:eu-repo/semantics/publishedVersion; info:eu-repo/semantics/bookPart Formato: application/pdf
Publicado em //2012 ENG
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The purpose of this chapter is to analyse international research in "pharmacology, toxicology and pharmaceutics" (hereafter pharmacology) on the basis of the scientific papers listed in the Scopus multidisciplinary database. This primary objective is reached by answering the following questions (in the section on results). What weight does the subject area "pharmacology, toxicology and pharmaceutics" carry in world-wide science? What is the percentage contribution made by the various regions of the world to the subject area "pharmacology, toxicology and pharmaceutics?" Can certain regions be identified as leaders on that basis, as in other scientific contexts? Are emerging countries present in the field? Do the most productive countries also publish the largest number of journals? What features characterise the scientific output of companies that publish pharmacological papers?

Untersuchung zur Zellulären Pharmakologie von peptidischen und nichtpeptidischen Wirkstoffmolekülen; Investigation of the Cellular Pharmacology of Peptidic and Non-Peptidic Compounds

Ruttekolk, Ivo Robert
Fonte: Universität Tübingen Publicador: Universität Tübingen
Tipo: Dissertation; info:eu-repo/semantics/doctoralThesis
DE_DE
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Untersuchung zur Zellulären Pharmakologie von peptidischen und nichtpeptidischen Wirkstoffmolekülen mittels Fluoreszenzkorrelationsspektroskopie, konfokaler Mikroscopie usw.; For more than 100 years, trials in “systemic” or “clinical” pharmacology have been revealing the behavior of drug-like molecules in organisms. In this context pharmacology is divided in pharmacodynamics and pharmacokinetics. Whereas pharmacodynamics deal with the impact of a drug or a combination of those on organisms, pharmacokinetics in turn describe the impact of an organism and its metabolic systems on the fate of the drug compound. Moreover, in the last decades many biophysical and bioanalytical techniques were developed and established to display the exact binding properties of defined binding partners, an area of activity that is often named “molecular pharmacology”. Especially highthroughput screening approaches play a key role in today's drug discovery. In cell culturebased approaches mostly the impact of a molecule on a single response that can be easily read out is displayed. Between systemic and molecular pharmacology there is still a large gap and the behavior of a molecule in its cellular and subcellular context is misleadingly assumed to be rather simple: the compound penetrates the plasma membrane...

Ginseng pharmacology: a new paradigm based on gintonin-lysophosphatidic acid receptor interactions

Choi, Sun-Hye; Jung, Seok-Won; Lee, Byung-Hwan; Kim, Hyeon-Joong; Hwang, Sung-Hee; Kim, Ho-Kyoung; Nah, Seung-Yeol
Fonte: Frontiers Media S.A. Publicador: Frontiers Media S.A.
Tipo: Artigo de Revista Científica
Publicado em 27/10/2015 EN
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Ginseng, the root of Panax ginseng, is used as a traditional medicine. Despite the long history of the use of ginseng, there is no specific scientific or clinical rationale for ginseng pharmacology besides its application as a general tonic. The ambiguous description of ginseng pharmacology might be due to the absence of a predominant active ingredient that represents ginseng pharmacology. Recent studies show that ginseng abundantly contains lysophosphatidic acids (LPAs), which are phospholipid-derived growth factor with diverse biological functions including those claimed to be exhibited by ginseng. LPAs in ginseng form a complex with ginseng proteins, which can bind and deliver LPA to its cognate receptors with a high affinity. As a first messenger, gintonin produces second messenger Ca2+ via G protein-coupled LPA receptors. Ca2+ is an intracellular mediator of gintonin and initiates a cascade of amplifications for further intercellular communications by activation of Ca2+-dependent kinases, receptors, gliotransmitter, and neurotransmitter release. Ginsenosides, which have been regarded as primary ingredients of ginseng, cannot elicit intracellular [Ca2+]i transients, since they lack specific cell surface receptor. However, ginsenosides exhibit non-specific ion channel and receptor regulations. This is the key characteristic that distinguishes gintonin from ginsenosides. Although the current discourse on ginseng pharmacology is focused on ginsenosides...

Uma introdução à farmacologia comportamental; An introduction to behavioral pharmacology

Leonardi, Jan Luiz; Pontifícia Universidade Católica de São Paulo; Núcleo Paradigma; Bravin, André Amaral; Universidade Federal de Goiás; Universidade de Brasília
Fonte: UFPR Publicador: UFPR
Tipo: info:eu-repo/semantics/article; info:eu-repo/semantics/publishedVersion; avaliado por pares; Formato: application/pdf
Publicado em 05/06/2012 POR
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 The aim of this paper is to introduce behavioral pharmacology, emphasizing it as an area that shows the relevance of the complementarity between behavior analysis and physiology. Initially, the text presents a brief history of the subject and explores its fundamental precept – the assertion that the effects of a drug are environmental variables that exert different stimulus functions in respondent and operant contingencies. Afterwards, some experiments which investigated the behavioral mechanisms of drug action are briefly described. Finally, the paper points out that the investigation on drug-behavior relations carried out by behavioral pharmacology is consistent with the philosophical assumptions of radical behaviorism and with the conceptual and empirical basis of behavior analysis. Keywords: behavioral pharmacology; behavior analysis; drugs.;  O presente artigo tem como objetivo introduzir a farmacologia comportamental, enfatizando-a como uma área que demonstra a relevância da complementaridade entre análise do comportamento e fisiologia. Inicialmente, o texto apresenta um breve histórico da disciplina e explora seu preceito fundamental – o de que os efeitos de uma droga constituem-se em variáveis ambientais que exercem diferentes funções de estímulo em contingências respondentes e operantes. Em seguida...