Zobrazeno 1 - 8
of 8
pro vyhledávání: '"Diane, Naselsky"'
Autor:
Steven D. Knight, Richard M. Keenan, James J. Foley, Diane Naselsky, Ralph A. Rivero, Kevin L. Salyers, Stephen A. Douglas, Anthony Sapienza, Nambi Aiyar, Ming An, Jian Jin, Dashyant Dhanak, Henry M. Sarau
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 18:3950-3954
SAR exploration of the central diamine, benzyl, and terminal aminoalkoxy regions of the N-cyclic azaalkyl benzamide series led to the identification of very potent human urotensin-II receptor antagonists such as 1a with a Ki of 4 nM. The synthesis an
Autor:
Richard M. Keenan, Henry M. Sarau, Nambi Aiyar, David J. Behm, Schmidt Stanley J, Lisa T. Christmann, Steven D. Knight, William E. Wixted, Lance Ridgers, Peter T. Buckley, Timothy Francis Gallagher, James J. Foley, Graham J. Riley, John G Gleason, Jyoti Disa, Diane Naselsky, Dashyant Dhanak, Stephen A. Douglas, Jian Jin, Widdowson Katherine L, Dulcie B. Schmidt, David P. Brooks, Eliot H. Ohlstein
Publikováno v:
British Journal of Pharmacology. 145:620-635
1. SB-706375 potently inhibited [(125)I]hU-II binding to both mammalian recombinant and 'native' UT receptors (K(i) 4.7+/-1.5 to 20.7+/-3.6 nM at rodent, feline and primate recombinant UT receptors and K(i) 5.4+/-0.4 nM at the endogenous UT receptor
Autor:
Jian Jin, Widdowson Katherine L, Dashyant Dhanak, Dulcie B. Schmidt, Henry M. Sarau, Nambi Aiyar, Richard M. Keenan, Stephen A. Douglas, Carl D. Bennett, Steven D. Knight, James J. Foley, Ralph A. Rivero, Diane Naselsky, Gregory L. Warren, Bing Wang, Michael L. Moore
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 15:3229-3232
High throughput screening of the corporate compound collection led to the discovery of a novel series of substituted aminoalkoxybenzyl pyrrolidines as human urotensin-II receptor antagonists. The synthesis, initial structure-activity relationships, a
Autor:
Nambi Aiyar, Diane Naselsky, Zhaohui Ao, Christopher L Herold, Frank Lynch, Stephen A. Douglas, Jyoti Disa
Publikováno v:
British Journal of Pharmacology. 142:921-932
1 In an effort to identify endogenous, native mammalian urotensin-II (U-II) receptors (UT), a diverse range of human, primate and rodent cell lines (49 in total) were screened for the presence of detectable [125I]hU-II binding sites. 2 UT mRNA (North
Autor:
Nambi Aiyar, Beverly E. Maleeff, Usman Shabon, Diane Naselsky, Zhaohui Ao, Stephen M. Harrison, Jyoti Disa, Stephen A. Douglas, Graham Duddy, Nabil Elshourbagy, Jan L. Sechler
Publikováno v:
British Journal of Pharmacology. 136:9-22
Urotensin-II (U-II) and its receptor (UT) represent novel therapeutic targets for management of a variety of cardiovascular diseases. To test such hypothesis, it will be necessary to develop experimental animal models for the manipulation of U-II/UT
Autor:
Stephen A, Douglas, Diane, Naselsky, Zhaohui, Ao, Jyoti, Disa, Christopher L, Herold, Frank, Lynch, Nambi V, Aiyar
Publikováno v:
British journal of pharmacology. 142(6)
1 In an effort to identify endogenous, native mammalian urotensin-II (U-II) receptors (UT), a diverse range of human, primate and rodent cell lines (49 in total) were screened for the presence of detectable [125I]hU-II binding sites. 2 UT mRNA (North
Autor:
Diane Naselsky, Brian F. Guida, Stephen A. Douglas, Frederick C. Kull, Jyoti Disa, Nambi Aiyar, David J. Behm, Zhaohui Ao, Jui-Lan Su
Publikováno v:
Peptides. 25(8)
Plasma and urinary levels of “urotensin(U)-II-like” substances determined in healthy human volunteers were 12.4 ± 0.6 ng/ml and 2.2 ± 0.3 ng/ml by RIA, an order of magnitude lower than that seen by RRA, 167.5 ± 9.5 ng/ml and 65.2 ± 4.3 ng/ml.
Autor:
Nabil A, Elshourbagy, Stephen A, Douglas, Usman, Shabon, Stephen, Harrison, Graham, Duddy, Jan L, Sechler, Zhaohui, Ao, Beverly E, Maleeff, Diane, Naselsky, Jyoti, Disa, Nambi V, Aiyar
Publikováno v:
British journal of pharmacology. 136(1)
Urotensin-II (U-II) and its receptor (UT) represent novel therapeutic targets for management of a variety of cardiovascular diseases. To test such hypothesis, it will be necessary to develop experimental animal models for the manipulation of U-II/UT