Zobrazeno 1 - 10
of 28
pro vyhledávání: '"Emir Duzic"'
Autor:
Thomas J. Connors, Jie Qian, Zeck Huang, Joanne R. Mathiasen, Edward R. Bacon, Thelma S. Angeles, Mark J. Huffman, Emir Duzic, Joseph M. Salvino, Beth Ann McKenna, Hervé Schaffhauser, Robert J. McHugh, Lily D. Lu, George C. Morton, Beverly P. Holskin, Karla Kopec, Amy DiCamillo, Gerard C. Rosse, Chrysanthe Spais, Rabindranath Tripathy, Lisa D. Aimone
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:1421-1426
Serotoninergic neurotransmission has been implicated in modulation of learning and memory. It has been demonstrated that 5-hydroxytryptamine(6) (5-HT(6)) receptor antagonists show beneficial effect on cognition in several animal models. Based on a ph
Autor:
Beverly P. Holskin, Karla Kopec, Joanne R. Mathiasen, Amy DiCamillo, Babu G. Sundar, Thomas J. Connors, Emir Duzic, Edward R. Bacon, Gerard C. Rosse, Chrysanthe Spais, Thomas R. Bailey, Beth Ann McKenna, Rebecca A. Brown, Jie Qian, Derek Dunn, Mark J. Huffman, Joseph M. Salvino, Huang Zeqi, Lisa D. Aimone, Hervé Schaffhauser, Deborah Galinis, Thelma S. Angeles, Lily D. Lu, George C. Morton
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 22:120-123
7-Arylsulfonyl substituted benzofuropiperidine was discovered as a novel scaffold for 5HT(6) receptor antagonists. Optimization by substitution at C-1 position led to identification of selective, orally bioavailable, brain penetrant antagonists with
Autor:
Emir Duzic, Edward R. Bacon, Joanne R. Mathiasen, Michael J. Marino, Donna Bozyczko-Coyne, John A. Gruner, John P. Mallamo, Rita Raddatz, Dorothy G. Flood, Lisa D. Aimone, Hervé Schaffhauser, Siyuan Le, Maciej Gasior, Michael Williams, Mark A. Ator, Robert L. Hudkins
Publikováno v:
Journal of Pharmacology and Experimental Therapeutics. 340:124-133
CEP-26401 [irdabisant; 6-{4-[3-((R)-2-methyl-pyrrolidin-1-yl)-propoxy]-phenyl}-2H-pyridazin-3-one HCl] is a novel, potent histamine H₃ receptor (H₃R) antagonist/inverse agonist with drug-like properties. High affinity of CEP-26401 for H₃R was d
Publikováno v:
Burger's Medicinal Chemistry and Drug Discovery. :499-548
Autor:
Beverly P. Holskin, Sheryl L. Meyer, Emmanuel Burgeon, Bruce Jones, Thao Ung, Emir Duzic, Sandra Y. Flores, Mark A. Ator, Vincent J. Dupriez
Publikováno v:
Analytical Biochemistry. 400:184-189
Assay technologies that measure intracellular Ca 2+ release are among the predominant methods for evaluation of GPCR function. These measurements have historically been performed using cell-permeable fluorescent dyes, although the use of the recombin
Publikováno v:
Journal of Biological Chemistry. 277:13827-13830
The Ras-related protein, activator of G-protein signaling 1 (AGS1) or Dexras1, interacts with G(i)/G(o)alpha and activates heterotrimeric G-protein signaling systems independent of a G-protein-coupled receptor (GPCR). As an initial approach to furthe
Publikováno v:
Assay and Drug Development Technologies
Voltage-gated Ca2+ channels play essential roles in control of neurosecretion and muscle contraction. The pharmacological significance of Cav channels stem from their identification as the molecular targets of calcium blockers used in the treatment o
Autor:
Michael Spruyt, Stephen M. Lanier, Jeffrey S. Lizano, Mary J. Cismowski, Xiaobing Xie, Catalina Ribas, Chienling Ma, Emir Duzic
Publikováno v:
Journal of Biological Chemistry. 275:23421-23424
Utilizing a functional screen in the yeastSaccharomyces cerevisiae we identified mammalian proteins that activate heterotrimeric G-protein signaling pathways in a receptor-independent fashion. One of the identified activators, termed AGS1 (for activa
Publikováno v:
Pfl�gers Archiv European Journal of Physiology. 435:280-285
The ability of recombinant rat alpha2D-and alpha2B-adrenoceptors expressed in nerve-growth-factor-differentiated pheochromocytoma PC-12 cells to modulate Ca2+ currents, recorded by the whole-cell patch-clamp technique, has been studied. Ca2+ currents
Autor:
Emir Duzic, Toshiaki Ebina, Naoki Oka, Jun-ichi Kawabe, Yoshihiro Ishikawa, Carsten Schwencke, Yoshiyuki Toya
Publikováno v:
FEBS Letters. 384:273-276
Type V adenylyl cyclase (AC) was stably over-expressed in HEK293 cells (293AC-V). Forskolin-stimulated cAMP accumulation in 293AC-V was 5 times as great as that in control cells. PMA, a protein kinase C (PKC) activator, enhanced cAMP accumulation in