National Library of Medicine (NCBI)
Peter Brown Editor of Special Reports, Andrew Robson, Widget Finn, Stewart Tendler and David Lister, Ian M. Ellis, David Charter Health Correspondent, Helen Studd, Robert Cole, Andrew Pierce, Patricia Davies, Sarah Potter, Philip Webster Melissa Kite and David Lister, Frances Gibb Legal Editor, Magnus Linklater, Julian Neely, Mark Souster, Richard Hobson, Martin Richards, David Rhys Jones, John Hall, Chief Education Officer, Michael Evans Defence Editor, Andrew Norfolk and Paul Wilkinson, Matt Wolf, Philip Howard, Miranda Stober, Joanna Bale, Richard Irving, Gabrielle Starkey, Lord Archer and Ted Francis, Richard Eaton, Barbara Ellen, Jeremy Whittle, Kevin Eason, Tony and Linton Dawe, Geoff Brown, Irwin Stelzer, Sam Lister, Joe Joseph, Giles Coren, John Thicknesse, Martin Fletcher, Ben Webster Transport Correspondent, L. Kelly (Merchant Navy), Pat Gibson, Thrasy Petropoulos, Dominic Walsh, Victoria Segal, Alix Ramsay Tennis Correspondent, Norman Harris, Tim Reid, Audrey Magee Ireland Correspondent, Martin Barrow, Dalya Alberge Arts Correspondent, Oliver Wright, Ian Clarke (Marketing Director), Robert Avery, J. A. T. Duncan, Robert Bruce, Grant Wilson, John O'Leary, Nick Wyke, Anatole Kaletsky, John O'Leary and Glen Owen, David A. Spencer, Charles Bremner, Catherine Lockwood, John Hutton, Greg Hurst, Peter Barnard, Mark Court, Clive Mathieson Telecoms Correspondent, Arthur Leathley City Correspondent, Caroline Merrell Banking Correspondent, Stuart Crainer, Angela Jameson, Emily Jane Baker's, Robert Hough (Chairman), Andrew Stables, Russell Kempson, Paula Hawkins, Oliver Kay, Ted Awty, David Lister, Gordon Cumming, Matt Dickinson Football Correspondent, Robin Owen, Philip Webster, Peter Riddell and Greg Hurst, Simon de Bruxelles, Rob Wright, Richard Davy, Glynn Gardner, Raymond Keene, D. A. P. Saunders-Davies, Sean MacAulay, Irene Zoech, Philip Whiteley, K. H. Wollaston, Alix Ramsay, Beryl Dixon, Damian Whitworth, Christopher Martin-Jenkins Chief Cricket Correspondent, Roger Boyes, John Stern, Barry Shooter, Nick Hasell, Rob Wrlght, John Speller, David Hands Rugby Correspondent, Ben Hammersley, Dearbáil Jordan, Mary Ann Sieghart, James Doran, Melissa Kite Political Correspondent, Philip Webster Political Editor, Giles Whittell, Colin Gillert, Jane Shilling, Tim Hames, Mel Webb, Stephen Sklaroff Deputy Director-General, Ian Johns, James Landale and Helen Rumbelow, Matthew Parris, Anjana Ahuja, Chris McGrath, Alan Lee, Stephen Hoare, Peter Riddell, Ben MacIntyre, Roy Hattersley, Tony Dawe, Michael Pilch (Chairman), Ben Webster, Alison Gibson, Chris Quick, Gary Duncan Economics Correspondent, Martin Waller, Chris Ayres, Patrick O'Brien, Mark Baldwin, Laura Peek, Ahmer Khokhar, Christopher Warman, Benedict Nightingale, Dr Thomas Stuttaford, Stephen Dalton, Matthew Paris Q&a, James Christopher, Alice Miles, Arthur Leathley, Adam Sherwin, Susan MacDonald, Tom Baldwin Deputy Political Editor, Hugh Sebag-Montefiore, Sally Patten, Emma Burns, Sally Patten Retail Correspondent, Roger Ordish, Damian Barr,
... at private schools, good reading for children and the quality of IT teaching Are musicians born or made? Parents who want their children to take up an instrument often agonist over how hard to push them. Catherine Lockwood ...
2001 - Gale Group | TDA
Daniel Cussac, Stéphane Schaak, Colette Denis, Hervé Paris,
... of the cardiovascular and sedative effects of α2-agonists, the precise functions of each subtype are far from ... those observed with α2-agonists. Like for α2-agonists, the action of AA was prevented by batimastat, 1, ... of the cardiovascular and sedative effects of α2-agonists, the precise functions of each subtype are far from ... those observed with α2-agonists. Like for α2-agonists, the action of AA was prevented by batimastat, 1, ... those observed with α2-agonists. Like for α2-agonists, the action of AA was prevented by batimastat, 1, ...
Tópico(s): Pharmacogenetics and Drug Metabolism
2002 - Elsevier BV | Journal of Biological Chemistry
National Library of Medicine (NCBI)
... qualitatively different from classical competitive antagonism in that the agonist and antagonist are not in mass-action equilibrium ... point other than the site of action of the agonist in question. Nonequilibrium blockade cannot be adequately distinguished ... noncompetitive blockade on the basis of effects on the agonist dose-response curves, or on the basis of ... the antagonist is in mass-action equlibrium with the agonist and may be remobed relatively casily by washing ... and is no longer in competitive equilibrium with the agonist. Because of the competitive phase early in the ...
Tópico(s): Pharmacological Effects and Assays
1957 - American Society for Pharmacology and Experimental Therapeutics | Pharmacological Reviews
J. Glen Newell, Susan M. J. Dunn,
... desensitized state even in the continued presence of agonist. The characteristics of desensitization in the wild-type and ... desensitized state even in the continued presence of agonist. The characteristics of desensitization in the wild-type and ... neurobiological adaptation to prolonged or repeated exposure to agonist. The molecular mechanisms by which this occurs have been ... even in the continued presence of the perfused agonist. The representative traces in Fig. 5 illustrate this phenomenon. ...
Tópico(s): Neuroendocrine regulation and behavior
2002 - Elsevier BV | Journal of Biological Chemistry
National Library of Medicine (NCBI)
Stephan A. Pless, Joseph W. Lynch,
... reaction is similar for low and high efficacy agonists. The present study sought to identify a conformational change ... reaction is similar for low and high efficacy agonists. The present study sought to identify a conformational change ... A–C). Furthermore, for each of the three agonists, the nH values for the ΔF dose response were ... and supplemental Fig. S1). Additionally, for all three agonists the nH for ΔF was significantly lower that that ...
Tópico(s): Synthesis and Biological Evaluation
2009 - Elsevier BV | Journal of Biological Chemistry
... impaired in apoE knockout adipocytes treated with PPARγ agonists. The current studies investigate the molecular mechanism for PPARγ ... is required for the apoE response to PPARγ agonists. The response of the apoE gene to treatment with ... impaired in apoE knockout adipocytes treated with PPARγ agonists. The current studies investigate the molecular mechanism for PPARγ ... is required for the apoE response to PPARγ agonists. The response of the apoE gene to treatment with ... apoE gene does not respond directly to PPARγ agonists and that the response requires involvement of an intermediary pathway. Based ...
Tópico(s): Lipid metabolism and biosynthesis
2009 - Elsevier BV | Journal of Biological Chemistry
Xiang‐Qun Hu, Li Zhang, Randall R. Stewart, Forrest F. Weight,
... current deactivation kinetics after rapid removal of the agonist. The records in Fig. 7, A and B, illustrate ... 7C). Desensitization Kinetics—In the continued presence of agonist, the activated current exhibited a marked decrease in amplitude ... receptors decayed with similar kinetics upon removal of agonist. The observation that the mutation did not alter the ...
Tópico(s): Receptor Mechanisms and Signaling
2003 - Elsevier BV | Journal of Biological Chemistry
... is 1 way of looking at these elective agonists? The answer is yes, provided they can offer results ... is 1 way of looking at these elective agonists? The answer is yes, provided they can offer results ... is 1 way of looking at these elective agonists? The answer is yes, provided they can offer results ...
Tópico(s): Cardiac electrophysiology and arrhythmias
2007 - Elsevier BV | The American Journal of Cardiology
Peter C. Simons, Sean M. Biggs, Anna Waller, Terry D. Foutz, Daniel F. Cimino, Qing Guo, Richard R. Neubig, Wei‐Jen Tang, Eric R. Prossnitz, Larry A. Sklar,
... the lowest intrinsic activity to 95% for full agonists; the percent correlated roughly with the intrinsic adenylyl cyclase activity of the agonist. The functional consequences of cellular ternary complex formation include ... in a ternary complex. For full and partial agonists, the maximal amount of ternary complex correlated with agonist ... with the concentration of β2AR-GFP for both agonists, with the full agonist, isoproterenol, showing the greatest slope. These data are consistent with a ... to the 0.3–1 μm Kd of the agonist-bound formyl peptide receptor and Gαi3β1γ2 (10Simons P. ...
Tópico(s): Advanced Biosensing Techniques and Applications
2004 - Elsevier BV | Journal of Biological Chemistry
C. S. Breivogel, Dana E. Selley, Steven R. Childers,
... GDP modulation of G-protein activation by cannabinoid agonists. The cannabinoid system is ideal for the study of ... by 30 μm GDP in the absence of agonist, the effect of GDP in the presence of WIN ... low affinity sites were not significantly affected by agonist. The apparent K Dof the agonist-induced high affinity ( ...
Tópico(s): Neurotransmitter Receptor Influence on Behavior
1998 - Elsevier BV | Journal of Biological Chemistry
Aldebaran M. Hofer, Barbara Landolfi, Lucantonio Debellis, Tullio Pozzan, Silvana Curci,
... sequester Ca2+ effectively in the continued presence of agonists. The rate at which this reuptake occurred was highly ... stores, either in the presence or absence of agonist. The luminal [Ca2+] of the cell shown in Figure ... normal Ringer's solution, and then restimulated with agonist. The two applications of BK yielded responses which were ...
Tópico(s): Pancreatic function and diabetes
1998 - Springer Nature | The EMBO Journal
Gaspar A. Fernández Nievas, Francisco J. Barrantes, Silvia S. Antollini,
... CrV (Fig. 1a). Remarkably, in the absence of agonist, the curves furnished in the presence of steroid were ... in the D state. In the presence of agonist, the curves obtained with or without steroid (control) were ... when CrV was added in the presence of agonist, the KD values obtained from samples treated with both ...
Tópico(s): Neuroscience and Neuropharmacology Research
2008 - Elsevier BV | Journal of Biological Chemistry
F.A. Lefebvre, A. Bélanger, G. Pelletier, Fernand Labrie,
... animals having received either dose of the LHRH agonist. The testicular steroidogenic responsiveness was measured 2 hours following ... five months of daily treatment with the LHRH agonist, the main findings are a decreased response of pregnenolone, ... recovery in all groups treated with the LHRH agonist. The present data show that long‐term treatment with an LHRH agonist in the rat induced compensatory changes in the testicular steroidogenic ...
Tópico(s): Birth, Development, and Health
1984 - Wiley | Andrology
Gianfranco Tortorici, B.X. Zhang, Xiaowu Xu, Shmuel Muallem,
... b) when cells were stimulated with a single agonist, the antagonists prevented only the effect of their specific agonist. The differential behavior of the antagonists in intact and ... signaling was obtained by showing that the partial agonist (the CCK octapeptide analogue JMV-180) can access and ... the affinity for IP3 resulted in a quantal agonist-evoked Ca2+ release. The overall findings are discussed in the context of ...
Tópico(s): Calcium signaling and nucleotide metabolism
1994 - Elsevier BV | Journal of Biological Chemistry
Ralf Hausmann, Mandy Bodnár, Ronja Woltersdorf, Haihong Wang, Martin Fuchs, Nanette Messemer, Ying Qin, Janka Günther, Thomas Riedel, Marcus Grohmann, K Nieber, Günther Schmalzing, Patrizia Rubini, Péter Illés,
... only the latter combination failed to respond to agonists. The effects of α,β-methylene–ATP and 2- ... to allow these receptors to react with their agonists. The aim of the present experiments was to clarify ... only the latter combination failed to respond to agonists. The effects of α,β-methylene–ATP and 2- ...
Tópico(s): Neuroendocrine regulation and behavior
2012 - Elsevier BV | Journal of Biological Chemistry
Nuriya Mukhtasimova, Corrie J.B. daCosta, Steven M. Sine,
... with successive agonist occupancy, and for a full agonist, the forward rate constant increases more than the equilibrium constant; for a partial agonist, the forward rate and equilibrium constants increase equally. The ... As observed for a full and a partial agonist, the gain-of-function mutation affects the relationship between ... distinguishes priming from gating steps and reveals how the corresponding rate and equilibrium constants depend on agonist occupancy.
Tópico(s): Nicotinic Acetylcholine Receptors Study
2016 - Rockefeller University Press | The Journal of General Physiology
G. Babnigg, Tatiana K. Zagranichnaya, Xiaoyan Wu, Mitchel L. Villereal,
... additional Ca2+ could be released by the second agonist. The data in Fig. 3 indicate that there is ... the other agonist. When CCh is the first agonist, the area under the BK curve is 15.4 ± ... the first peak. When BK is the first agonist, the area under the CCh peak is 60.1 ± ...
Tópico(s): Ion Transport and Channel Regulation
2003 - Elsevier BV | Journal of Biological Chemistry
Bridgette January, Anita Seibold, Brenda S. Whaley, R. William Hipkin, Doris Lin, Agnes Schönbrunn, Roger Barber, Richard B. Clark,
... for 0.5–30 min. Following incubation with agonist, the medium was removed and cells were washed six ... Scopus (143) Google Scholar);i.e. for poorer agonists the EC50 approaches theK d, and the EC50/K ...
Tópico(s): Hormonal Regulation and Hypertension
1997 - Elsevier BV | Journal of Biological Chemistry
Kenneth D. Fitch, Malcolm Sue‐Chu, Sandra D. Anderson, Louis‐Philippe Boulet, Robert J. Hancox, Donald C. McKenzie, Vibeke Backer, Kenneth W. Rundell, Juan Manuel Alonso, Pascale Kippelen, Joseph Cummiskey, Alain Garnier, Arne Ljungqvist,
... without asthma may have been using inhaled β2-agonists, the symposium recommended that to be granted permission to ... the IOC and WADA with respect to β2-agonists. The conference examined a number of issues including the ... asthma/AHR, the performance of athletes inhaling β2-agonists, and the future of β2-agonists at Olympic Games. This ... will need a fast-acting bronchodilator. Inhaled β2-agonists are the most effective bronchodilators for the relief of asthma ... Unfortunately, studies show that regular treatment with β2-agonists increases the sensitivity of the airways to bronchoconstrictive stimuli including ...
Tópico(s): Pharmacological Effects and Assays
2008 - Elsevier BV | Journal of Allergy and Clinical Immunology
Dana B. Fathy, Tosso Leeb, Sandra A. Mathis, L.M. Fredrik Leeb-Lundberg,
... that in the absence of a more efficacious agonist, the efficacy and behavior of a partial agonist should ... than the result of antagonism of endogenously released agonist. The action of NPC17731 and HOE140 either as agonists ... Scholar) reported that the efficacies of several inverse agonists at the β2-adrenergic receptor were perturbed following agonist pretreatment ...
Tópico(s): Receptor Mechanisms and Signaling
1999 - Elsevier BV | Journal of Biological Chemistry
... facilitate the design of novel cAMP antagonists and agonists. The cAMP-binding domain (CBD) is an ancient and ... facilitate the design of novel cAMP antagonists and agonists. The cAMP-binding domain (CBD) 2The abbreviations used are: ... Rp)-cAMPS, (Sp)-cAMPS behaves as a cAMP agonist, revealing the stringent stereo-specific requirements of antagonism. However, it ... cAMPS analogs function as a cAMP antagonist and agonist, respectively. The crystal structures of the regulatory subunit of PKA ( ...
Tópico(s): Protein Kinase Regulation and GTPase Signaling
2006 - Elsevier BV | Journal of Biological Chemistry
Jean Labrecque, Julie Deschênes, Normand McNicoll, André De Léan,
... a treatment with rat ANP or with other agonists. The NPR-AD435C mutant has not been subjected to ... a treatment with rat ANP or with other agonists. The NPR-AD435C mutant has not been subjected to ... dimer formation after the removal of the inducer agonist. On the other hand, a construction where the intracellular domain ... these, NPR-A and NPR-B, respond to agonists by the activation of their guanylyl cyclase catalytic domain. The ... BSA, and the protease inhibitors) containing 1 μm agonist. For the specificity study, rANP, pBNP, atriopeptin I (API), CNP, ...
Tópico(s): Pharmaceutical studies and practices
2001 - Elsevier BV | Journal of Biological Chemistry
Nanping Wang, Lynne Verna, Neng-Guin Chen, Jasmine Chen, Hongling Li, Barry M. Forman, Michael B. Stemerman,
... results also suggest that, in addition to pharmacological agonists, the genetic modification of the PPAR-γ activity in ... results also suggest that, in addition to pharmacological agonists, the genetic modification of the PPAR-γ activity in ... account for pleiotropic effects of individual pharmacological PPAR agonists. For the time being, the exact pathways leading to a ...
Tópico(s): Adipose Tissue and Metabolism
2002 - Elsevier BV | Journal of Biological Chemistry
Remigijus Lapė, David Colquhoun, Lucia G. Sivilotti,
... agonists, though in the case of a partial agonist, the maximum response is only a fraction of that evoked by a full agonist. The mechanism underlying this pharmacological observation is investigated and ... opening as those that are bound to full agonists. Instead, the diminished response results from a reduced ability to ...
Tópico(s): Ion channel regulation and function
2008 - Nature Portfolio | Nature