… , and structure− activity relationships of novel 2-substituted pyrazinoylguanidine epithelial sodium channel blockers: drugs for cystic fibrosis and chronic bronchitis
AJ Hirsh, BF Molino, J Zhang… - Journal of medicinal …, 2006 - ACS Publications
… blockers and thereby reduce renal side effects. This report describes the design and synthesis
of novel ENaC blockers that … We found that all of the compounds synthesized in this study …
of novel ENaC blockers that … We found that all of the compounds synthesized in this study …
ENaC inhibitors for the treatment of cystic fibrosis
R Butler, T Hunt, NJ Smith - Pharmaceutical patent analyst, 2015 - Future Science
… , chronic obstructive pulmonary disease (COPD) and chronic … further conclusions regarding
structure–activity relationships; … -02), a novel epithelial sodium channel blocker with potential …
structure–activity relationships; … -02), a novel epithelial sodium channel blocker with potential …
Novel small molecule epithelial sodium channel inhibitors as potential therapeutics in cystic fibrosis–a patent evaluation
M Schoenberger, M Althaus - Expert Opinion on Therapeutic …, 2013 - Taylor & Francis
… successful in blocking ENaC activity, and in many cases, novel ENaC blockers are amiloride
… Years of optimizing amiloride structure–activity relationships have taught us that first, a …
… Years of optimizing amiloride structure–activity relationships have taught us that first, a …
… -(2, 3-dihydroxypropoxy) phenyl] butyl-guanidine methanesulfonate (552-02), a novel epithelial sodium channel blocker with potential clinical efficacy for cystic fibrosis …
AJ Hirsh, J Zhang, A Zamurs, J Fleegle… - … of Pharmacology and …, 2008 - ASPET
… In summary, compound 552-02 is a novel potent, more selective, less epithelial-permeant,
more durable epithelial sodium channel blocker than amiloride. When administered as an …
more durable epithelial sodium channel blocker than amiloride. When administered as an …
Controlling epithelial sodium channels with light using photoswitchable amilorides
… Thus, our novel optical tool can be operated by turning on and … ENaC blocker PA1 has
been designed, synthesized and … new insights into the structure–activity relationships of the …
been designed, synthesized and … new insights into the structure–activity relationships of the …
Sodium channels and cystic fibrosis
SH Donaldson, RC Boucher - Chest, 2007 - Elsevier
… epithelial sodium channel … chronic bronchitis exacerbations and other syndromes associated
with reductions in mucociliary clearance, thereby creating the possibility for novel treatment …
with reductions in mucociliary clearance, thereby creating the possibility for novel treatment …
Defining an inhibitory domain in the α-subunit of the epithelial sodium channel
MD Carattino, CJ Passero, CA Steren… - American Journal …, 2008 - journals.physiology.org
… produces a phenotype similar to cystic fibrosis (CF) with airway … Structure-activity analyses
of the inhibitory peptide revealed … and chronic bronchitis (10). Amiloride is a prototypic ENaC …
of the inhibitory peptide revealed … and chronic bronchitis (10). Amiloride is a prototypic ENaC …
Cystic fibrosis: pathogenesis and future treatment strategies
FA Ratjen - Respiratory care, 2009 - rc.rcjournal.com
… In clinical trials, amiloride (an epithelial sodium channel blocker with … Design, synthesis,
and structure-activity relationships of novel 2-substituted pyrazinoylguanidine epithelial sodium …
and structure-activity relationships of novel 2-substituted pyrazinoylguanidine epithelial sodium …
ENaC inhibitors and airway re-hydration in cystic fibrosis: state of the art
M Althaus - Current molecular pharmacology, 2013 - ingentaconnect.com
… The discovery and development of novel ENaC inhibitors are thus still an important area of
… Mutations in the amiloride-sensitive epithelial sodium channel in patients with cystic fibrosis-…
… Mutations in the amiloride-sensitive epithelial sodium channel in patients with cystic fibrosis-…
[HTML][HTML] High-content siRNA screen reveals global ENaC regulators and potential cystic fibrosis therapy targets
… epithelial sodium channel that regulates salt and water reabsorption in epithelia, causes
several human diseases, including cystic … As most of these hit genes are novel proteins for …
several human diseases, including cystic … As most of these hit genes are novel proteins for …