Search Results - "Pullen, Mark A."

The discovery of GSK221149A: A potent and selective oxytocin antagonist by Liddle, John, Allen, Michael J., Borthwick, Alan D., Brooks, David P., Davies, David E., Edwards, Richard M., Exall, Anne M., Hamlett, Chris, Irving, Wendy R., Mason, Andrew M., McCafferty, Gerald P., Nerozzi, Fabrizio, Peace, Simon, Philp, Joanne, Pollard, Derek, Pullen, Mark A., Shabbir, Shaila S., Sollis, Steve L., Westfall, Timothy D., Woollard, Pat M., Wu, Charlene, Hickey, Deirdre M.B.

“…Optimisation of a series of oxazole diketopiperazines has led to the discovery of a very potent and selective oxytocin antagonist GSK221149A. GSK221149A has…”
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Characterization of the neutralizing activity of digoxin-specific Fab toward ouabain-like steroids by Pullen, Mark A, Brooks, David P, Edwards, Richard M

“…Digoxin-specific Fab (Digibind) is a mixture of antidigoxin Fab fragments prepared from sheep sera and is used as a treatment for digoxin poisoning…”
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The effect of acute angiotensin-converting enzyme and neutral endopeptidase 24.11 inhibition on plasma extravasation in the rat by Sulpizio, Anthony C, Pullen, Mark A, Edwards, Richard M, Brooks, David P

“…The effect of angiotensin-converting enzyme (ACE) and neutral endopeptidase (NEP) inhibition on microvascular plasma leakage (extravasation) was evaluated in a…”
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Mechanism of vasopeptidase inhibitor-induced plasma extravasation: comparison of omapatrilat and the novel neutral endopeptidase 24.11/angiotensin-converting enzyme inhibitor GW796406 by Sulpizio, Anthony C, Pullen, Mark A, Edwards, Richard M, Louttit, James B, West, Rob, Brooks, David P

“…We describe N-[(2S)-2-(mercaptomethyl)-3-methylbutanoyl]-4-(1H-pyrazol-1-yl)-L-phenylalanine (GW796406), a vasopeptidase inhibitor (VPI) that possessed…”
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Pyridyl-2,5-Diketopiperazines as Potent, Selective, and Orally Bioavailable Oxytocin Antagonists: Synthesis, Pharmacokinetics, and In Vivo Potency by Borthwick, Alan D, Liddle, John, Davies, Dave E, Exall, Anne M, Hamlett, Christopher, Hickey, Deirdre M, Mason, Andrew M, Smith, Ian E. D, Nerozzi, Fabrizio, Peace, Simon, Pollard, Derek, Sollis, Steve L, Allen, Michael J, Woollard, Patrick M, Pullen, Mark A, Westfall, Timothy D, Stanislaus, Dinesh J

“…A six-stage stereoselective synthesis of indanyl-7-(3′-pyridyl)-(3R,6R,7R)-2,5-diketopiperazines oxytocin antagonists from indene is described. SAR studies…”
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Endothelin Receptor Subtype Distribution Predisposes Coronary Arteries to Damage by Louden, Calvert S., Nambi, Ponnal, Pullen, Mark A., Thomas, Roberta A., Tierney, Lauren A., Solleveld, Henk A., Schwartz, Lester W.

“…Several vasoactive drugs that lower blood pressure and increase heart rate induce regional cardiotoxicity in the dog, most frequently of right coronary…”
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The angiotensin type 1 receptor antagonist, eprosartan, attenuates the progression of renal disease in spontaneously hypertensive stroke-prone rats with accelerated hypertension by Abrahamsen, Christian T, Barone, Frank C, Campbell, Jr, Wallace G, Nelson, Allen H, Contino, Lisa C, Pullen, Mark A, Grygielko, Eugene T, Edwards, Richard M, Laping, Nicholas J, Brooks, David P

“…The effects of the angiotensin type 1 (AT(1)) receptor antagonist, eprosartan, were studied in a model of severe, chronic hypertension. Treatment of male…”
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Effects of angiotensins II and IV on blood pressure, renal function, and PAI-1 expression in the heart and kidney of the rat by Abrahamsen, Christian T, Pullen, Mark A, Schnackenberg, Christine G, Grygielko, Eugene T, Edwards, Richard M, Laping, Nicholas J, Brooks, David P

“…The role of angiotensin II (AII) and angiotensin IV (AIV) as inducers of PAI-1 expression during hypertension was studied in vivo. A 2-week infusion of AII…”
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Discovery of novel aminothiadiazole amides as selective EP3 receptor antagonists by Hilfiker, Mark A., Wang, Ning, Hou, Xiaoping, Du, Zhimin, Pullen, Mark A., Nord, Melanie, Nagilla, Rakesh, Fries, Harvey E., Wu, Charlene W., Sulpizio, Anthony C., Jaworski, Jon-Paul, Morrow, Dwight, Edwards, Richard M., Jin, Jian

“…A series of 2-aminothiadiazole amides has been identified with potent EP3 antagonist activity, good rat DMPK properties, and excellent prostenoid receptor…”
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Comparison of non-digitalis binding properties of digoxin-specific Fabs using direct binding methods by Pullen, Mark A., Harpel, Mark R., Danoff, Theodore M., Brooks, David P.

“…Digibind and DigiFab are commercial formulations of polyclonal, ovine, digoxin-specific Fabs in clinical use for treatment of digoxin intoxication. Of interest…”
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Use of a novel and highly selective oxytocin receptor antagonist to characterize uterine contractions in the rat by McCafferty, Gerald P, Pullen, Mark A, Wu, Charlene, Edwards, Richard M, Allen, Michael J, Woollard, Patrick M, Borthwick, Alan D, Liddle, John, Hickey, Deirdre M B, Brooks, David P, Westfall, Timothy D

“…Spontaneous and induced uterine contractions in the rat were found to be inhibited by a novel and selective oxytocin receptor antagonist GSK221149A…”
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Determination of conformational changes in the progesterone receptor using ELISA-like assays by Pullen, Mark A., Laping, Nicholas, Edwards, Richard, Bray, Jeffrey

“…The conformation of proteins often influences their functional activity. The effect of progesterone receptor ligands on the C-terminal conformation of the…”
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Neuromedin U elicits cytokine release in murine Th2-type T cell clone D10.G4.1 by Johnson, Eric N, Appelbaum, Edward R, Carpenter, Donald C, Cox, Richard F, Disa, Jyoti, Foley, James J, Ghosh, Sujoy K, Naselsky, Diane P, Pullen, Mark A, Sarau, Henry M, Scheff, Samuel R, Steplewski, Klaudia M, Zaks-Zilberman, Meirav, Aiyar, Nambi

“…Neuromedin U (NmU), originally isolated from porcine spinal cord and later from other species, is a novel peptide that potently contracts smooth muscle. NmU…”
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Neuromedin Elicits Cytokine Release in Murine Th2-Type T Cell Clone D10.G4.1 by Johnson, Eric N, Appelbaum, Edward R, Carptenter, Donald C, Cox, Richard F, Disa, Jyoti, Foley, James J, Ghosh, Sujoy K, Naselsky, Diane P, Pullen, Mark A, Sarau, Henry M, Scheff, Samuel R, Steplewski, Klaudia M, Zaks-Zilberman, Meirav, Aiyar, Nambi

“…Abstract Neuromedin U (NmU), originally isolated from porcine spinal cord and later from other species, is a novel peptide that potently contracts smooth…”
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Functional and binding characterization of endothelin receptors in human bronchus: evidence for a novel endothelin B receptor subtype? by Hay, D W, Luttmann, M A, Pullen, M A, Nambi, P

“…Binding and functional studies were conducted to elucidate the receptor subtypes mediating contractions of human bronchus induced by endothelin (ET) receptor…”
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Stimulation of Hyaluronan synthetase by platelet-derived growth factor bb in human prostate smooth muscle cells by Pullen, M, Thomas, K, Wu, H, Nambi, P

“…Hyaluronic acid (HA) is an important component of the extracellular matrix of prostate cells. Platelet-derived growth factor bb (PDGFbb) has a mitogenic effect…”
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Discovery of novel aminothiadiazole amides as selective EP sub(3) receptor antagonists by Hilfiker, Mark A, Wang, Ning, Hou, Xiaoping, Du, Zhimin, Pullen, Mark A, Nord, Melanie, Nagilla, Rakesh, Fries, Harvey E, Wu, Charlene W, Sulpizio, Anthony C, Jaworski, Jon-Paul, Morrow, Dwight, Edwards, Richard M, Jin, Jian

“…This Letter discloses a series of 2-aminothiadiazole amides as selective EP sub(3) receptor antagonists. SAR optimization resulted in compounds with excellent…”
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Discovery of novel aminothiadiazole amides as selective EP(3) receptor antagonists by Hilfiker, Mark A, Wang, Ning, Hou, Xiaoping, Du, Zhimin, Pullen, Mark A, Nord, Melanie, Nagilla, Rakesh, Fries, Harvey E, Wu, Charlene W, Sulpizio, Anthony C, Jaworski, Jon-Paul, Morrow, Dwight, Edwards, Richard M, Jin, Jian

“…This Letter discloses a series of 2-aminothiadiazole amides as selective EP(3) receptor antagonists. SAR optimization resulted in compounds with excellent…”
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