Zobrazeno 1 - 10
of 24
pro vyhledávání: '"Penny G. Threlkeld"'
Autor:
Kjell Svensson, David L. McKinzie, Kenneth W. Perry, David Lee Nelson, Julie F. Falcone, Penny G. Threlkeld, Karen S. Rash, Matthew J. Fell, Gerard J. Marek, Virginia L. Lucaites, Vanessa N. Barth, James A. Monn, Bryan G. Johnson
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 331:1126-1136
Some recently published in vitro studies with two metabotropic glutamate 2/3 receptor (mGluR(2/3)) agonists [(-)-2-oxa-4-aminobicyclo[3.1.0] hexane-4,6-dicarboxylic acid (LY379268) and 1S,2S,5R,6S-2-aminobicyclo[3.1.0]hexane-2,6-bicaroxylate monohydr
Autor:
Kumiko, Takeuchi, Todd J, Kohn, Nicholas A, Honigschmidt, Vincent P, Rocco, Patrick G, Spinazze, Daniel J, Koch, Steven T, Atkinson, Larry W, Hertel, David L, Nelson, D Bradley, Wainscott, Laura J, Ahmad, Janice, Shaw, Penny G, Threlkeld, David T, Wong
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 13:2393-2397
Potent 5-HT1A/SSRIs at low nanomolar and subnanomolar concentrations were identified in a series of 1-(1H-indol-4-yloxy)-3-(4-benzo[b]thiophen-2-ylpiperidinyl)propan-2-ols. Incorporation of an alpha-Me group in the piperidine ring with its specific s
Autor:
Conway Richard Gerard, Kenneth W. Perry, Frank P. Bymaster, David L. Nelson, Penny G. Threlkeld, Susanne Koch
Publikováno v:
Neuropsychopharmacology. 27:949-959
The selective serotonin reuptake inhibitor fluoxetine consists of equal amounts of R and S stereoisomers. In this study, we investigated the pharmacologic properties of the stereoisomers using transporter and receptor binding assays and in vivo micro
Autor:
John H. Heiligenstein, S Michelle Morin, Kenneth W. Perry, David L. Nelson, Frank P. Bymaster, Susan K. Hemrick-Luecke, Penny G. Threlkeld, Jason Katner, Donald R. Gehlert
Publikováno v:
Neuropsychopharmacology. 27:699-711
The selective norepinephrine (NE) transporter inhibitor atomoxetine (formerly called tomoxetine or LY139603) has been shown to alleviate symptoms in Attention Deficit/Hyperactivity Disorder (ADHD). We investigated the mechanism of action of atomoxeti
Autor:
Penny G. Threlkeld, David L. Nelson, Janice Shaw, David T. Wong, Susan K. Hemrick-Luecke, Frank P. Bymaster, L.J. Ahmad, Linda K. Thompson
Publikováno v:
Neuropsychopharmacology. 25:871-880
The blockade of serotonin (5-HT) and norepinephrine (NE) transporters in vitro and in vivo by the dual 5-HT/NE reuptake inhibitors duloxetine and venlafaxine was compared. Duloxetine inhibited binding to the human NE and 5-HT transporters with K(i) v
Autor:
Bruce D. Gitter, Steven S. Y. Cho, Diane C. Waters, Donald R. Gehlert, Thomas Alan Crowell, Brian Stephen Muehl, Penny G. Threlkeld, Kirk W. Johnson, J. H. Krushinski, Karen Lynn Lobb, Robert F. Bruns, Philip Arthur Hipskind, Domenico Regoli, Lee A. Phebus, Nixon James Arthur, Smriti Iyengar, J. Jeffry Howbert, Dominic L. Li, Foreman Mark Mortensen, Norman R. Mason, Rosa Maria A. Simmons
Publikováno v:
ChemInform. 27
Early structure−activity studies on racemic tryptophan ester and amide NK-1 antagonists 5−7 led to the discovery that the potency of the series could be markedly increased by moving the carbonyl function in these molecules to an off-chain positio
Autor:
Penny G. Threlkeld, Carl L. McMillian, Bruce D. Gitter, James E. Fritz, Karen Lynn Lobb, Stephen W. Kaldor, Nixon James Arthur, Philip Arthur Hipskind
Publikováno v:
ChemInform. 32
Solution-phase, parallel-synthesis techniques were used to optimize a series of nonbasic NK-1 antagonists, resulting in the identification of (R)-26, an orally bioavailable compound with subnanomolar potency.
Publikováno v:
Life Sciences. 46:231-235
Saturable [3H]-8OHDPAT binding to 5HT-1A receptors in membranes prepared from hippocampus and frontal cerebral cortex of alcohol-preferring P rats and of alcohol-nonpreferring NP rats has been compared. The Bmax values or densities of recognition sit
Autor:
Kumiko Takeuchi, Todd J. Kohn, Nicholas A. Honigschmidt, Vincent P. Rocco, Patrick G. Spinazze, Susan K. Hemrick-Luecke, Linda K. Thompson, David C. Evans, Kurt Rasmussen, Deanna Koger, David Lodge, Laura J. Martin, Janice Shaw, Penny G. Threlkeld, David T. Wong
Publikováno v:
Bioorganicmedicinal chemistry letters. 16(9)
A series of 1-aryloxy-3-piperidinylpropan-2-ols possessing potent dual 5-HT1A receptor antagonism and serotonin reuptake inhibition was discovered. 1-(1H-Indol-4-yloxy)-3-(4-benzo[b]thiophen-2-ylpiperidinyl)propan-2-ols exhibited selective and high a
Autor:
Penny G. Threlkeld, R.J. Lantz, Tianwei Ma, Ping Yi, David L. Nelson, M. Zmijewski, William J. Wheeler, T.A. Gillespie, Palaniappan Kulanthaivel, Fengjiun Kuo
Publikováno v:
Bioorganicmedicinal chemistry letters. 14(13)
Several putative phase I duloxetine metabolites, 4-hydroxy-, 5-hydroxy-, 6-hydroxy-, 5-hydroxy-6-methoxy-, 6-hydroxy-5-methoxy-, 5,6-dihydroxy-, and 4,6-dihydroxyduloxetine were synthesized, and their phase II metabolite as glucuronide or sulfate con