Search Results - "TRYBULSKI, E. J"

WAY‐318068: a novel, potent and selective noradrenaline re‐uptake inhibitor with activity in rodent models of pain and depression by Whiteside, GT, Dwyer, JM, Harrison, JE, Beyer, CE, Cummons, T, Manzino, L, Mark, L, Johnston, GH, Strassle, BW, Adedoyin, A, Lu, P, Piesla, MJ, Pulicicchio, CM, Erve, JCL, Platt, BJ, Hughes, ZA, Rogers, KE, Deecher, DC, Trybulski, EJ, Kennedy, JD, Zhang, P, Leventhal, L

“…Background and purpose:  Antidepressants, which raise the CNS concentrations of 5‐HT and noradrenaline, are frequently used in the treatment of chronic pain;…”
Get full text

Quinidine preferentially blocks the slow delayed rectifier potassium channel in the rested state by Yao, J A, Trybulski, E J, Tseng, G N

“…We examined the effects of quinidine on a slow delayed rectifier K current induced by a human IsK cDNA (hlsK) in Xenopus oocytes. The apparent blocking potency…”
Get more information

The design, synthesis and physical chemical properties of novel human vasopressin V2-receptor antagonists optimized for parenteral delivery by ASHWELL, M. A, BAGLI, J. F, WILLIAMS, D. K, CAGGIANO, T. J, CHAN, P. S, MOLINARI, A. J, PALKA, C, PARK, C. H, ROGERS, J. F, SHERMAN, M, TRYBULSKI, E. J

“…Ionizable groups were introduced onto the 10,11-dihydro-5H-pyrrolo[2,1-c][1,4]benzodiazepine scaffold of the vasopressin V2-antagonist WAY-VPA-985 in the…”
Get full text

The synthesis and biochemical pharmacology of enantiomerically pure methylated oxotremorine derivatives by Trybulski, Eugene J, Zhang, Jing, Kramss, Richard H, Mangano, Richard M

“…Previous pharmacological studies of methylated oxotremorine derivatives bearing substituents at the 3-, 4-, and 5-positions of the pyrrolidinone ring have been…”
Get full text

Chemical and biochemical studies of 2-propynylpyrrolidine derivatives. Restricted-rotation analogs of N-methyl-N-(1-methyl-4-pyrrolidino-2-butynyl)acetamide (BM-5) by Trybulski, Eugene J, Kramss, Richard H, Mangano, Richard M, Rusinko, Andrew

“…A series of optically pure 2-[substituted-3-aminopropynyl]pyrrolidine derivatives, which are restricted-rotation analogues of the muscarinic agent…”
Get full text

2-Benzazepines. 9. Synthesis and chemistry of 3H-2-benzazepine and pyrimido[4,5-d][2]benzazepine derivatives by Trybulski, E. J, Fryer, R. I, Reeder, E, Vitone, S, Todaro, L

Get full text

2-Benzazepines. [1,2,3]Triazolo[4,5-d][2]benzazepines and dibenzo[c,f][1,2,3]triazolo[3,4-a]azepines. Synthesis and evaluation as central nervous system agents by Trybulski, E. J, Benjamin, L, Vitone, S, Walser, A, Fryer, R. I

Get full text

2-Benzazepines. 4. [1,2,3]Triazolo[4,5-d][2]benzazepines and dibenzo[c,f][1,2,3]triazolo[3,4-a]azepines: synthesis and evaluation as central nervous system agents by Trybulski, E J, Benjamin, L, Vitone, S, Walser, A, Fryer, R I

“…The facile synthesis of [1,2,3]triazolo((4,5-d][2]benzazepines and dibenzo[c,f][1,2,3]triazolo[3,4-a]azepines by the addition of sodium azide to acetylenic…”
Get full text

Quinazolines and 1,4-benzodiazepines. 90. Structure-activity relationship between substituted 2-amino-N-(2-benzoyl-4-chlorophenyl)acetamides and 1,4-benzodiazepinones by Fryer, R I, Leimgruber, W, Trybulski, E J

“…The syntheses of 2-amino-N-(2-benzoyl)-4-chlorophenyl)acetamides are reported. The pharmacological properties of these compounds were compared with data…”
Get full text

2-Benzazepines. 6. Synthesis and pharmacological properties of the metabolites of 9-chloro-7-(2-chlorophenyl)-5H-pyrimido[5,4-d][2]benzazepine by Trybulski, Eugene J, Fryer, R. Ian, Reeder, Earl, Walser, Armin, Blount, John

“…The 2-benzazepine 9-chloro-7-(2-chlorophenyl)-5H-pyrimido[5,4-d] [2]benzazepine (1) has been selected for development as an anxiolytic agent. In support of…”
Get full text

2-Benzazepines. 5. Synthesis of pyrimido[5,4-d][2]benzazepines and their evaluation as anxiolytic agents by Trybulski, Eugene J, Benjamin, Louis E, Earley, James V, Fryer, R. Ian, Gilman, Norman W, Reeder, Earl, Walser, Armin, Davidson, Arnold B, Horst, W. Dale

“…A series of 5H-pyrimido[5,4-d][2]benzazepines has been synthesized, starting from the corresponding 2-benzazepin-5-ones, and evaluated as potential anxiolytic…”
Get full text

Pyridobenzodiazepines: A novel class of orally active, vasopressin V 2 receptor selective agonists by Failli, Amedeo A., Shumsky, Jay S., Steffan, Robert J., Caggiano, Thomas J., Williams, David K., Trybulski, Eugene J., Ning, Xiaoping, Lock, Yeungwai, Tanikella, Tarak, Hartmann, David, Chan, Peter S., Park, C.H.

“…The synthesis and structure–activity relationships (SAR) of a novel class of potent, orally active, non-peptidic vasopressin V 2 receptor selective agonists…”
Get full text

2-Benzazepines. 2. Thiazolo[5,4-d][2]benzazepines by Benjamin, Louis E, Fryer, R. Ian, Gilman, Norman W, Trybulski, Eugene J

“…As part of a program in the area of annelated 2-benzazepines, several thiazolo[5,4-d))[2]benzazepines were prepared. Treatment of the bromo ketones 7-9 with…”
Get full text

Synthesis and activity of a new class of pathway-selective estrogen receptor ligands: Hydroxybenzoyl-3,4-dihydroquinoxalin-2(1 H)-ones by Mahaney, Paige E., Webb, Michael B., Ye, Fei, Sabatucci, Joseph P., Steffan, Robert J., Chadwick, Christopher C., Harnish, Douglas C., Trybulski, Eugene J.

“…The anti-inflammatory activity of non-selective estrogens has been attributed to their ability to antagonize the activity of nuclear factor κB (NF-κB), a known…”
Get full text

The synthesis of 4H-imidazo[5,1-c][1,4]benzothiazine derivatives by Fryer, R. Ian, Lauer, Rudolph F., Trybulski, Eugene J., Vitone, Stephen, Walser, Armin, Zenchoff, Gladys

“…A facile synthesis of the 4H‐imidazo[5,1‐c][1,4]benzothiazine ring system is described. The synthesis utilized the annulation of an imidazole ring onto a…”
Get full text

Chapter 16. Vasopressin receptor modulators: From non-peptide antagonists to agonists by Trybulski, Eugene J.

“…This chapter elaborates the various aspects of vasopressin receptor modulators. The cyclic peptide hormone arginine vasopressin (AVP) or antidiuretic hormone…”
Get full text

The design, synthesis and physical chemical properties of novel human vasopressin V 2 -receptor antagonists optimized for parenteral delivery by Ashwell, M.A, Bagli, J.F, Caggiano, T.J, Chan, P.S, Molinari, A.J, Palka, C, Park, C.H, Rogers, J.F, Sherman, M, Trybulski, E.J, Williams, D.K

Get full text

2-Benzazepines. IX: Synthesis and chemistry of 3H-2-benzazepine and pyrimido[4,5-d][2]benzazepine derivatives by TRYBULSKI, E. J, FRYER, R. I, REEDER, E, VITONE, S, TODARO, L

Get full text

2-Benzazepines. VI: Synthesis and pharmacological properties of the metabolites of 9-chloro-7-(2-chlorophenyl)-5H-pyrimido [5,4-d] [2] benzazepine by TRYBULSKI, E. J, FRYER, R. I, REEDER, E, WALSER, A, BLOUNT, J

Get full text

Synthetic approach to the skeleton of histrionicotoxin by Tufariello, Joseph J, Trybulski, Eugene J

Get full text