Search Results - "SCHORN, T. W"

Angiotensin II receptor subtypes in renal cortex of rats and rhesus monkeys by Gibson, R E, Thorpe, H H, Cartwright, M E, Frank, J D, Schorn, T W, Bunting, P B, Siegl, P K

“…The angiotensin II (ANG II) receptor has recently been shown to exhibit subtypes with respect to antagonist binding. Of particular interest are the potent…”
Get full text

Discovery of L-162,313: a nonpeptide that mimics the biological actions of angiotensin II by Kivlighn, S D, Huckle, W R, Zingaro, G J, Rivero, R A, Lotti, V J, Chang, R S, Schorn, T W, Kevin, N, Johnson, Jr, R G, Greenlee, W J

“…L-162,313 (5,7-dimethyl-2-ethyl-3-[[4-[2(n- butyloxycarbonylsulfonamido)-5-isobutyl-3-thienyl]phenyl]methyl]- imadazo[4,5-b]pyridine) is a nonpeptide that…”
Get full text

Potent, orally active imidazo[4,5-b]pyridine-based angiotensin II receptor antagonists by Mantlo, Nathan B, Chakravarty, Prasun K, Ondeyka, Debra L, Siegl, Peter K. S, Chang, Raymond S, Lotti, Victor J, Faust, Kristie A, Schorn, Terry W, Chen, Tsing Bau

Get full text

Synthesis and use of 3-amino-4-phenyl-2-piperidones and 4-amino-2-benzazepin-3-ones as conformationally restricted phenylalanine isosteres in renin inhibitors by De Laszlo, S. E, Bush, B. L, Doyle, J. J, Greenlee, W. J, Hangauer, D. G, Halgren, T. A, Lynch, R. J, Schorn, T. W, Siegl, P. K. S

“…The design of P2-P3 conformational restrictions in renin inhibitors by the use of a renin computer graphic model led to the synthesis of inhibitors containing…”
Get full text

In vitro and in vivo evaluation of dihydropyrimidinone C-5 amides as potent and selective alpha(1A) receptor antagonists for the treatment of benign prostatic hyperplasia by Barrow, J C, Nantermet, P G, Selnick, H G, Glass, K L, Rittle, K E, Gilbert, K F, Steele, T G, Homnick, C F, Freidinger, R M, Ransom, R W, Kling, P, Reiss, D, Broten, T P, Schorn, T W, Chang, R S, O'Malley, S S, Olah, T V, Ellis, J D, Barrish, A, Kassahun, K, Leppert, P, Nagarathnam, D, Forray, C

“…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…”
Get full text

Renin inhibitors. Syntheses of subnanomolar, competitive, transition-state analog inhibitors containing a novel analog of statine by Boger, Joshua, Payne, Linda S, Perlow, Debra S, Lohr, Nancy S, Poe, Martin, Blaine, Edward H, Ulm, Edgar H, Schorn, Terry W, LaMont, Bruce I

“…Analogues of the renin octapeptide substrate were synthesized in which replacement of the scissile dipeptide with (3S,4S)-4-amino-3-hydroxy-6-methylheptanoic…”
Get full text

Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 1. Structure-activity relationship in dihydropyrimidinones by Nagarathnam, D, Miao, S W, Lagu, B, Chiu, G, Fang, J, Murali Dhar, T G, Zhang, J, Tyagarajan, S, Marzabadi, M R, Zhang, F, Wong, W C, Sun, W, Tian, D, Wetzel, J M, Forray, C, Chang, R S, Broten, T P, Ransom, R W, Schorn, T W, Chen, T B, O'Malley, S, Kling, P, Schneck, K, Bendesky, R, Harrell, C M

“…Dihydropyrimidinones such as compound 12 exhibited high binding affinity and subtype selectivity for the cloned human alpha(1a) receptor. Systematic…”
Get full text

Biotransformation of 5-chloro-3-phenylthioindole-2-carboxamide (L-734,005) in rhesus monkeys and rat liver microsomes to a potent HIV-1 reverse transcriptase inhibitor by Balani, S K, Goldman, M E, Kauffman, L R, Varga, S L, O'Brien, J A, Smith, S J, Olah, T V, Ramjit, H G, Schorn, T W, Pitzenberger, S M

“…Rhesus monkeys were dosed orally with 10 mg/kg 5-chloro-3-phenylthioindole-2-carboxamide (L-734,005), a nonnucleoside human immunodeficiency virus type 1…”
Get more information

Highly potent, orally active diester macrocyclic human renin inhibitors by Weber, Ann E, Steiner, Mark G, Krieter, Philip A, Colletti, Adria E, Tata, James R, Halgren, Thomas A, Ball, Richard G, Doyle, John J, Schorn, Terry W

“…Replacing one amide bond in macrocyclic renin inhibitors of the general structure 1 and 2 with an ester linkage gave glutamate-derived inhibitors 3 and…”
Get full text

Renin inhibitors containing C-termini derived from mercaptoheterocycles by Ashton, Wallace T, Cantone, Christine L, Meurer, Laura C, Tolman, Richard L, Greenlee, William J, Patchett, Arthur A, Lynch, Robert J, Schorn, Terry W, Strouse, John F, Siegl, Peter K. S

“…A series of transition-state analogues having heterocyclythio C-termini has been synthesized and evaluated for inhibition of human renin. Addition of…”
Get full text

Inhibitors of human renin with C-termini derived from amides and esters of .alpha.-mercaptoalkanoic acids by Ashton, Wallace T, Cantone, Christine L, Tolman, Richard L, Greenlee, William J, Lynch, Robert J, Schorn, Terry W, Strouse, John F, Siegl, Peter K. S

“…New transition-state analogues bearing C-termini derived from alpha-mercaptoalkanoic acids, esters, and amides were prepared and evaluated as inhibitors of…”
Get full text

The character of the atrial natriuretic response: pressure and volume effects by Blaine, E H, Heinel, L A, Schorn, T W, Marsh, E A, Whinnery, M A

“…Synthetic atrial natriuretic factor (ANF) was compared to the well-characterized diuretics hydrochlorothiazide and furosemide in rats. While ANF was markedly…”
Get more information

Design and synthesis of novel alpha(1)(a) adrenoceptor-selective antagonists. 2. Approaches to eliminate opioid agonist metabolites via modification of linker and 4-methoxycarbonyl-4-phenylpiperidine moiety by Murali Dhar, T G, Nagarathnam, D, Marzabadi, M R, Lagu, B, Wong, W C, Chiu, G, Tyagarajan, S, Miao, S W, Zhang, F, Sun, W, Tian, D, Shen, Q, Zhang, J, Wetzel, J M, Forray, C, Chang, R S, Broten, T P, Schorn, T W, Chen, T B, O'Malley, S, Ransom, R, Schneck, K, Bendesky, R, Harrell, C M, Vyas, K P

“…We have previously described compound 1a as a high-affinity subtype selective alpha(1a) antagonist. In vitro and in vivo evaluation of compound 1a showed its…”
Get full text

Acute hypotensive responses to peptide inhibitors of renin in conscious monkeys: an effect on blood pressure independent of plasma renin inhibition by Schaffer, L W, Schorn, T W, Winquist, R J, Strouse, J F, Payne, L, Chakravarty, P K, de Laszlo, S E, tenBroeke, J, Veber, D F, Greenlee, W J

“…In order to investigate the hypotensive mechanisms of action of peptide renin inhibitors, blood pressure responses to five renin inhibitors were compared with…”
Get more information

In vivo pharmacology of L-159,913, a new highly potent and selective nonpeptide angiotensin II receptor antagonist by Gabel, R A, Kivlighn, S D, Zingaro, G J, Schorn, T W, Schaffer, L W, Ashton, W T, Chang, L L, Flanagan, K, Greenlee, W J, Siegl, P K

“…The present study was designed to characterize the in vivo pharmacology of L-159,913 (4-[[2'-(N-benzoylsulfamoyl)biphenyl-4-yl]-5butyl-2,4-dihydr o-2-…”
Get more information

An orally active prostaglandin analog with renal vasodilatory activity in the dog by Blaine, E H, Russo, H F, Schorn, T W, Snyder, C

Get more information

Nonpeptide angiotensin II antagonists derived from 4H-1,2,4-triazoles and 3H-imidazo[1,2-b][1,2,4]triazoles by Ashton, Wallace T, Cantone, Christine L, Chang, Linda L, Hutchins, Steven M, Strelitz, Robert A, MacCoss, Malcolm, Chang, Raymond S. L, Lotti, Victor J, Faust, Kristie A

“…By a variety of synthetic routes, we have synthesized a series of 3,4,5-trisubstituted 4H-1,2,4-triazoles and a related series of…”
Get full text

In vivo pharmacology of a novel AT1 selective angiotensin II receptor antagonist, MK-996 by Kivlighn, S D, Zingaro, G J, Gabel, R A, Broten, T P, Schorn, T W, Schaffer, L W, Naylor, E M, Chakravarty, P K, Patchett, A A, Greenlee, W J

“…MK-996, N-(4'-(5,7-dimethyl-2-ethyl-3H-imidazo[4,5-b]pyridin-3-yl- methyl)1,1'-biphenyl-2-yl)-sulfonylbenzamide, is a potent, orally active, highly selective,…”
Get more information

Design and synthesis of N-alkylated saccharins as selective alpha-1a adrenergic receptor antagonists by Nerenberg, J B, Erb, J M, Thompson, W J, Lee, H Y, Guare, J P, Munson, P M, Bergman, J M, Huff, J R, Broten, T P, Chang, R S, Chen, T B, O'Malley, S, Schorn, T W, Scott, A L

“…Benign prostatic hyperplasia can be managed pharmacologically with alpha-1 adrenergic receptor antagonists. Agents that demonstrate selectivity for the…”
Get full text

Novel renin inhibitors containing the amino acid statine by Boger, Joshua, Lohr, Nancy S, Ulm, Edgar H, Poe, Martin, Blaine, Edward H, Fanelli, George M, Lin, Tsau-Yen, Payne, Linda S, Schorn, Terry W, LaMont, Bruce I, Vassil, Ted C, Stabilito, Inez I, Veber, Daniel F, Rich, Daniel H, Bopari, Amrit S

“…The proteolytic enzyme renin (EC3.4.99.19) cleaves the protein substrate angiotensinogen to yield angiotensin I, the decapeptide substrate transformed by…”
Get full text