Search Results - "Waldron, T L"

BMS-201620: a selective beta 3 agonist by Washburn, W.N., Sun, C.-Q., Bisacchi, G., Wu, G., Cheng, P.T., Sher, P.M., Ryono, D., Gavai, A.V., Poss, K., Girotra, R.N., McCann, P.J., Mikkilineni, A.B., Dejneka, T.C., Wang, T.C., Merchant, Z., Morella, M., Arbeeny, C.M., Harper, T.W., Slusarchyk, D.A., Skwish, S., Russell, A.D., Allen, G.T., Tesfamariam, B., Frohlich, B.H., Abboa-Offei, B.E., Cap, M., Waldron, T.L., George, R.J., Young, D., Dickinson, K.E., Seymour, A.A.

“…Graphic A series of N-(4-hydroxy-3-methylsulfonanilidoethanol)arylglycinamides were prepared and evaluated for their human β 3 adrenergic receptor agonist…”
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Beta 3 agonists. Part 1: evolution from inception to BMS-194449 by Washburn, W.N., Sher, P.M., Poss, K.M., Girotra, R.N., McCann, P.J., Gavai, A.V., Mikkilineni, A.B., Mathur, A., Cheng, P., Dejneka, T.C., Sun, C.Q., Wang, T.C., Harper, T.W., Russell, A.D., Slusarchyk, D.A., Skwish, S., Allen, G.T., Hillyer, D.E., Frohlich, B.H., Abboa-Offei, B.E., Cap, M., Waldron, T.L., George, R.J., Tesfamariam, B., Ciosek, C.P., Ryono, D., Young, D.A., Dickinson, K.E., Seymour, A.A., Arbeeny, C.M., Gregg, R.E.

“…Screening of the BMS collection identified 4-hydroxy-3-methylsulfonanilidoethanolamines as full beta 3 agonists. Substitution of the ethanolamine nitrogen with…”
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Antihypertensive Effects of a Novel Endothelin - A Receptor Antagonist in Rats by Bird, Eileen J, Moreland, Suzanne, Waldron, Thomas L, Powell, James R

“…Endothelin is a potent pressor agent mediated primarily through activation of endothelin-A receptors on vascular smooth muscle. Surprisingly, there is no…”
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Quinoxaline N-oxide containing potent angiotensin II receptor antagonists: synthesis, biological properties, and structure-activity relationships by Kim, Kyoung Soon, Qian, Ligang, Bird, J. Eileen, Dickinson, Kenneth E. J, Moreland, Suzanne, Schaeffer, Thomas R, Waldron, Thomas L, Delaney, Carol L, Weller, Harold N, Miller, Arthur V

“…A series of novel quinoxaline heterocycle containing angiotensin II receptor antagonist analogs were prepared. This heterocycle was coupled to the biphenyl…”
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Endogenous synthesis of endothelin-1 may mediate a delayed pressor response after injection of endothelin-1 in rats by Bird, J E, Waldron, T L

“…We previously described delayed pressor response (DPR) 3 h after endothelin (ET)-1 injection in normotensive rats. In the current study, we examined effects of…”
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Fosinopril, a phosphinic acid inhibitor of angiotensin I converting enzyme: in vitro and preclinical in vivo pharmacology by DeForrest, J M, Waldron, T L, Harvey, C, Scalese, B, Rubin, B, Powell, J R, Petrillo, E W, Cushman, D W

“…Fosinopril is the first member of a new chemical class of angiotensin I (AI) converting enzyme (ACE) inhibitors, the phosphinic acids. In vitro, SQ 27,519, the…”
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Arylpropanolamines : Selective β3 agonists arising from strategies to mitigate phase I metabolic transformations by WASHBURN, W. N, HARPER, T. W, DEJNEKA, T, AHMED, S, CARINGAL, Y, HANGELAND, J, ZHANG, M, CHENG, P. T. W, RUSSELL, A. D, SKWISH, S, SLUSARCHYK, D. A, ALLEN, G. T, WU, G, FROHLICH, B. H, ABBOA-OFFEI, B. E, CAP, M, WALDRON, T. L, GEORGE, R. J, TESFAMARIAM, B, DICKINSON, K. E, SEYMOUR, A. A, SHER, P. M, GODFREY, J. D, MCCANN, P, GIROTRA, R, SHAO, C, ZHANG, H, GAVAI, A, MIKKILINENI, A

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Preclinical pharmacology of zofenopril, an inhibitor of angiotensin I converting enzyme by DeForrest, J M, Waldron, T L, Krapcho, J, Turk, C, Rubin, B, Powell, J R, Cushman, D W, Petrillo, E W

“…Zofenopril calcium (one-half calcium salt) is a prodrug ester analog of captopril whose biological effects are manifested by its active component, SQ 26,333…”
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The effects of novel cathepsin E inhibitors on the big endothelin pressor response in conscious rats by Bird, J E, Waldron, T L, Little, D K, Asaad, M M, Dorso, C R, DiDonato, G, Norman, J A

“…The aspartic protease, cathepsin E, has been shown to specifically cleave big endothelin (big ET-1) at the Trp21-Val22 bond to produce endothelin (ET-1) and…”
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Ceranapril (SQ 29,852), an orally active inhibitor of angiotensin converting enzyme (ACE) by DeForrest, J M, Waldron, T L, Harvey, C, Scalese, R, Hammerstone, S, Powell, J R, Karanewsky, D

“…Ceranapril (SQ 29,852) is a new inhibitor of angiotensin I (AI) converting enzyme (ACE) belonging to the hydroxylphosphonate class. The purpose of the present…”
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Blood pressure lowering and renal hemodynamic effects of fosinopril in conscious animal models by DeForrest, J M, Waldron, T L, Harvey, C, Scalese, B, Mitch, S, Powell, J R, Petrillo, W, Cushman, D W

“…The blood pressure lowering and renal hemodynamic effects of fosinopril, the chemically novel inhibitor of angiotensin I converting enzyme (ACE), was assessed…”
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Effects of the endothelin (ET) receptor antagonist BQ 123 on initial and delayed vascular responses induced by ET-1 in conscious, normotensive rats by Bird, J E, Waldron, T L, Dorso, C R, Asaad, M M

“…The ETA receptor antagonist, BQ 123 was used to characterize depressor and initial and delayed pressor responses to ET-1 in conscious rats. BQ 123 (0.001-0.01…”
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Incomplete inhibition of endothelin-1 pressor effects by an endothelin ETA receptor antagonist by Bird, J E, Waldron, T L

“…Incomplete inhibition of endothelin-1-induced pressor effects by FR-139317, a novel, potent, ETA receptor antagonist, was observed in conscious, normotensive…”
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SQ 27,786 and SQ 28,853: two angiotensin converting enzyme inhibitors with potent diuretic activity by DeForrest, J M, Waldron, T L, Powell, J R, Floyd, D M, Sundeen, J E

“…SQ 27,786 and SQ 28,853 were designed to possess both angiotensin converting enzyme (ACE) inhibitory and diuretic properties. Both compounds were given to…”
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Perinephritis hypertension in Macaca fascicularis (cynomolgus monkey): studies of the renin-angiotensin-aldosterone axis and renal hemodynamic function by DeForrest, J M, Scalese, R J, Oehl, R S, Waldron, T L, Mitch, S, Brittain, R J, Free, C A, Asaad, M, Burkett, D

“…The purpose of the present study was to characterize the etiology of bilateral perinephritis hypertension in the non-human primate. Hypertension was induced in…”
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Renal response to captopril in conscious dogs pretreated with indomethacin by DeForrest, J M, Waldron, T L, Antonaccio, M J

“…This study was designed to determine whether the prostaglandins mediate the renal effects of captopril in the conscious sodium-replete dog. In a group of…”
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BMS-196085: a potent and selective full agonist of the human beta(3) adrenergic receptor by Gavai, A V, Sher, P M, Mikkilineni, A B, Poss, K M, McCann, P J, Girotra, R N, Fisher, L G, Wu, G, Bednarz, M S, Mathur, A, Wang, T C, Sun, C Q, Slusarchyk, D A, Skwish, S, Allen, G T, Hillyer, D E, Frohlich, B H, Abboa-Offei, B E, Cap, M, Waldron, T L, George, R J, Tesfamariam, B, Harper, T W, Ciosek, Jr, C P, Young, D A, Dickinson, K E, Seymour, A A, Arbeeny, C M, Washburn, W N

“…A series of 4-hydroxy-3-methylsulfonanilido-1,2-diarylethylamines were prepared and evaluated for their human beta(3) adrenergic receptor agonist activity. SAR…”
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Dihydropyrimidine angiotensin II receptor antagonists by Atwal, Karnail S, Ahmed, Syed Z, Bird, J. Eileen, Delaney, Carol L, Dickinson, Kenneth E. J, Ferrara, Francis N, Hedberg, Anders, Miller, Arthur V, Moreland, Suzanne

“…The discovery of the nonpeptide angiotensin II (AII) receptor antagonist losartan, previously called DuP 753, has stimulated considerable interest in the…”
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Arylpropanolamines: selective beta3 agonists arising from strategies to mitigate phase I metabolic transformations by Washburn, W N, Harper, T W, Wu, G, Godfrey, J D, McCann, P, Girotra, R, Shao, C, Zhang, H, Gavai, A, Mikkilineni, A, Dejneka, T, Ahmed, S, Caringal, Y, Hangeland, J, Zhang, M, Cheng, P T W, Russell, A D, Skwish, S, Slusarchyk, D A, Allen, G T, Frohlich, B H, Abboa-Offei, B E, Cap, M, Waldron, T L, George, R J, Tesfamariam, B, Dickinson, K E, Seymour, A A, Sher, P M

“…Utilization of N-substituted-4-hydroxy-3-methylsulfonanilidoethanolamines 1 as selective beta(3) agonists is complicated by their propensity to undergo…”
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Arylpropanolamines: Selective beta sub(3) agonists arising from strategies to mitigate phase I metabolic transformations by Washburn, W N, Harper, T W, Wu, G, Godfrey, J D, McCann, P, Girotra, R, Shao, C, Zhang, H, Gavai, A, Mikkilineni, A, Dejneka, T, Ahmed, S, Caringal, Y, Hangeland, J, Zhang, M, Cheng, PTW, Russell, AD, Skwish, S, Slusarchyk, DA, Allen, G T, Frohlich, B H, Abboa-Offei, B E, Cap, M, Waldron, T L, George, R J, Tesfamariam, B, Dickinson, KE, Seymour, A A, Sher, P M

“…Utilization of N-substituted-4-hydroxy-3-methylsulfonanilidoethanolamines 1 as selective beta sub(3) agonists is complicated by their propensity to undergo…”
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