Zobrazeno 1 - 10
of 18
pro vyhledávání: '"Paul J. Kling"'
Autor:
Robert J. Bendesky, Wai C. Wong, Theodore P. Broten, Fengqi Zhang, Dake Tian, Carlos Forray, James Fang, Sriram Tyagarajan, Dhanapalan Nagarathnam, and Kamlesh P. Vyas, Shou Wu Miao, George Chiu, Mohammad R. Marzabadi, T. G. Murali Dhar, Charles Gluchowski, Kathryn Schneck, Paul J. Kling, Raymond S.L. Chang, Bharat Lagu, Jack Zhang, Wanying Sun, Stacey O'Malley, Tsing B. Chen, Richard W. Ransom, Terry W. Schorn, Charles M. Harrell, John M. Wetzel
Publikováno v:
Journal of Medicinal Chemistry. 42:4764-4777
Dihydropyrimidinones such as compound 12 exhibited high binding affinity and subtype selectivity for the cloned human alpha(1a) receptor. Systematic modifications of 12 led to identification of highly potent and subtype-selective compounds such as (+
Autor:
Miao Shou Wu, Stacey O'Malley, Kamlesh P. Vyas, Paul J. Kling, Raymond S.L. Chang, Wanying Sun, Wai C. Wong, Richard W. Ransom, Kanyin Zhang, John M. Wetzel, Jian Peng, Charles Gluchowski, Theodore P. Broten, Dhanapalan Nagarathnam, Carlos Forray, Fengqi Zhang, Dake Tian, Bharat Lagu, Tsing B. Chen, Mohammad R. Marzabadi
Publikováno v:
Journal of Medicinal Chemistry. 42:4804-4813
We have previously disclosed dihydropyridines such as 1a,b as selective alpha(1a) antagonists as a potential treatment for benign prostatic hyperplasia (BPH). The propensity of dihydropyridines toward an oxidation led us to find suitable replacements
Autor:
Tsing-B. Chen, Kristie A. Faust, Elizabeth M. Naylor, Bradley V. Clineschmidt, Prasun K. Chakravarty, Victor J. Lotti, Robert J. Bendesky, Stacey A. O'Malley, Paul J. Kling, Raymond S.L. Chang, Arthur A. Patchett, William J. Greenlee
Publikováno v:
Drug Development Research. 32:161-171
MK-996 (N-((4′-((5,7-Dimethyl-2-ethyl-3H-imidazo[4,5-b]pyridin-3-yl)methyl) (1,1′-biphenyl)-2-yl) sulfonylbenzamide) interacted in a competitive manner with rabbit aortic angiotensin II (All) receptors as determined by Scatchard analysis of speci
Autor:
L.W. Schaffer, Victor J. Lotti, Prasun K. Chakravarty, Wallace T. Ashton, Arthur A. Patchett, Tsing-Bau Chen, K. L. Flanagan, Salah D. Kivlighn, Elizabeth M. Naylor, W.J. Greenlee, Robert J. Bendesky, Linda L. Chang, Peter K. S. Siegl, R. S. L. Chang, Terry W. Schorn, Kristie A. Faust, Gloria J. Zingaro, Paul J. Kling
Publikováno v:
Bioorganic & Medicinal Chemistry Letters. 4:115-120
A series of trisubstituted triazolinones with a [2′-(N-acylsulfamoy)biphenyl-4-yl]methyl side chain at N4 has been prepared. The inhibition of AII pressor responses by these potent AT1-selective AII antagonists indicated some of them to be superior
Autor:
Kelem Kassahun, Philippe G. Nantermet, Roger M. Freidinger, Timothy V. Olah, Carlos Forray, Harold G. Selnick, Thomas G. Steele, Theodore P. Broten, James C. Barrow, Kenneth E. Rittle, Raymond S.L. Chang, Duane R. Reiss, Carl F. Homnick, Rick W. Ransom, Paul J. Kling, Kristen L. Glass, A. Barrish, Kevin F. Gilbert, Paula Leppert, Stacey O'Malley, Dhanapalan Nagarathnam, Terry W. Schorn, Joan D. Ellis
Publikováno v:
Journal of medicinal chemistry. 43(14)
alpha(1) Adrenergic receptors mediate both vascular and lower urinary tract tone, and alpha(1) receptor antagonists such as terazosin (1b) are used to treat both hypertension and benign prostatic hyperplasia (BPH). Recently, three different subtypes
Autor:
William J. Greenlee, Salah D. Kivlighn, Deborah Ondeyka, Peter K. S. Siegl, Victor J. Lotti, Raymond S.L. Chang, Stacey O'Malley, Paul J. Kling, Tsing-Bau Chen, Robert J. Bendesky, Nathan B. Mantlo
Publikováno v:
European journal of pharmacology. 294(2-3)
L-163,017 (6-[benzoylamino]-7-methyl-2-propyl-3-[[2'-(N-(3-methyl-1-butoxy) carbonylaminosulfonyl) [1,1']-biphenyl-4-yl]methyl]-3H-imidazo[4,5-b]pyridine) inhibited specific 125I-[Sar1, Ile8]angiotensin II binding to angiotensin AT1 receptor (Ki = 0.
Publikováno v:
Life Sciences. 29:633-639
Desipramine (DMI), protriptyline, chlorpromazine, amitriptyline and cocaine, alone or in the presence of prazosin, produced a dose-related inhibition of contractions induced by field stimulation of the rat vas deferens. The inhibition of contractions
Autor:
James P. Springer, Tsing-Bau Chen, Robert M. DiPardo, Roger M. Freidinger, Paul J. Kling, Paul S. Anderson, D. J. Cerino, K. A. Kunkel, Daniel F. Veber, J. Hirshfield, W. L. Whitter, Kenneth E. Rittle, Ben E. Evans, Victor J. Lotti, George F. Lundell, Mark G. Bock, Raymond S.L. Chang
Publikováno v:
Journal of Medicinal Chemistry. 31:2235-2246
3-(Acylamino)-5-phenyl-2H-1,4-benzodiazepines, antagonists of the peptide hormone cholecystokinin (CCK), are described. Developed by reasoned modification of the known anxiolytic benzodiazepines, these compounds provide highly potent, orally effectiv
Publikováno v:
European Journal of Pharmacology. 84:161-167
Schild plots for (-)-propranolol, timolol and IPS 339, but not penbutolol or carazolol, as antagonists of isoproterenol in the isolated, field-stimulated rat vas deferens exhibited biphasic curves indicating the presence of both high and low affinity
Publikováno v:
Life Sciences. 37:2111-2122
The binding of biologically active 125I-Bolton-Hunter (BH)-NPY to rat brain membranes was saturable and reversible and regulated by inorganic cations and guanyl nucleotides consistent with other neurotransmitter receptor systems. The concentration of