In Vitro and in Vivo Evaluation of Dihydropyrimidinone C-5 Amides as Potent and Selective α1A Receptor Antagonists for the Treatment of Benign Prostatic …
…, P Kling, D Reiss, TP Broten, TW Schorn… - Journal of medicinal …, 2000 - ACS Publications
α 1 Adrenergic receptors mediate both vascular and lower urinary tract tone, and α 1
receptor antagonists such as terazosin (1b) are used to treat both hypertension and benign …
receptor antagonists such as terazosin (1b) are used to treat both hypertension and benign …
Design and Synthesis of Novel α1a Adrenoceptor-Selective Antagonists. 1. Structure−Activity Relationship in Dihydropyrimidinones
…, TP Broten, RW Ransom, TW Schorn… - Journal of medicinal …, 1999 - ACS Publications
Dihydropyrimidinones such as compound 12 exhibited high binding affinity and subtype
selectivity for the cloned human α 1a receptor. Systematic modifications of 12 led to …
selectivity for the cloned human α 1a receptor. Systematic modifications of 12 led to …
Potent, orally active imidazo [4, 5-b] pyridine-based angiotensin II receptor antagonists
…, RS Chang, VJ Lotti, KA Faust, TW Schorn… - Journal of medicinal …, 1991 - ACS Publications
Angiotensin II is the principle pressor agent of the re-nin-angiotensin system (RAS). This
system, a proteolytic cascade that regulates hemodynamics and water and electrolyte balance, …
system, a proteolytic cascade that regulates hemodynamics and water and electrolyte balance, …
Novel renin inhibitors containing the amino acid statine
…, EH Blaine, GM Fanelli, TY Lin, LS Payne, TW Schorn… - Nature, 1983 - nature.com
The proteolytic enzyme renin (EC3.4.99.19) cleaves the protein substrate angiotensinogen
to yield angiotensin I, the decapeptide substrate transformed by converting enzyme into the …
to yield angiotensin I, the decapeptide substrate transformed by converting enzyme into the …
Renin inhibitors. Syntheses of subnanomolar, competitive, transition-state analog inhibitors containing a novel analog of statine
…, M Poe, EH Blaine, EH Ulm, TW Schorn… - Journal of medicinal …, 1985 - ACS Publications
Analogues of the renin octapeptide substrate were synthesized in which replacement of the
scissile dipeptide with (3S, 4S)-4-amino-3-hydroxy-6-methylheptanoic acid (statine, Sta) …
scissile dipeptide with (3S, 4S)-4-amino-3-hydroxy-6-methylheptanoic acid (statine, Sta) …
Discovery of L-162,313: a nonpeptide that mimics the biological actions of angiotensin II
…, VJ Lotti, RS Chang, TW Schorn… - American Journal …, 1995 - journals.physiology.org
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 mimics the biological actions …
imadazo[4,5-b]pyridine) is a nonpeptide that mimics the biological actions …
Angiotensin II receptor subtypes in renal cortex of rats and rhesus monkeys
…, ME Cartwright, JD Frank, TW Schorn… - American Journal …, 1991 - journals.physiology.org
The angiotensin II (ANG II) receptor has recently been shown to exhibit subtypes with respect
to antagonist binding. Of particular interest are the potent nonpeptide antagonists, DUP …
to antagonist binding. Of particular interest are the potent nonpeptide antagonists, DUP …
Highly potent, orally active diester macrocyclic human renin inhibitors
…, RG Ball, JJ Doyle, TW Schorn - Journal of medicinal …, 1992 - ACS Publications
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 serine-derived inhibitors 4. …
with an ester linkage gave glutamate-derived inhibitors 3 and serine-derived inhibitors 4. …
Design and synthesis of novel alpha (1)(a) adrenoceptor-selective antagonists. 2. Approaches to eliminate opioid agonist metabolites via modification of linker and 4 …
…, RS Chang, TP Broten, TW Schorn… - Journal of …, 1999 - pubmed.ncbi.nlm.nih.gov
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 major metabolite to be a …
antagonist. In vitro and in vivo evaluation of compound 1a showed its major metabolite to be a …
Design and Synthesis of Novel α1a Adrenoceptor-Selective Dihydropyridine Antagonists for the Treatment of Benign Prostatic Hyperplasia
…, RSL Chang, T Broten, TW Schorn… - Journal of medicinal …, 1998 - ACS Publications
We report the synthesis and evaluation of novel α 1a adrenoceptor subtype-selective
antagonists. Systematic modification of the lipophilic 4,4-diphenylpiperidinyl moiety of the …
antagonists. Systematic modification of the lipophilic 4,4-diphenylpiperidinyl moiety of the …