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Discovery of Dihydrobenzoxazepinone (GS-6615) Late Sodium Current Inhibitor (Late I Nai), a Phase II Agent with Demonstrated Preclinical Anti-Ischemic and Antiarrhythmic Properties

Journal of medicinal chemistry, 2016-10, Vol.59 (19), p.9005-9017

2016

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Discovery of triazolopyridinone GS-462808, a late sodium current inhibitor (Late INai) of the cardiac Nav1.5 channel with improved efficacy and potency relative to ranolazine

Bioorganic & medicinal chemistry letters, 2016-07, Vol.26 (13), p.3207-3211

2016

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Discovery of triazolopyridine GS-458967, a late sodium current inhibitor (Late INai) of the cardiac NaV 1.5 channel with improved efficacy and potency relative to ranolazine

Bioorganic & medicinal chemistry letters, 2016-07, Vol.26 (13), p.3202-3206

2016

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Novel short-acting A2A adenosine receptor agonists for coronary vasodilation: inverse relationship between affinity and duration of action of A2A agonists

The Journal of pharmacology and experimental therapeutics, 2001-07, Vol.298 (1), p.209

2001

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Structure-affinity relationships of the affinity of 2-pyrazolyl adenosine analogues for the adenosine A2A receptor

Bioorganic & medicinal chemistry letters, 2002-10, Vol.12 (20), p.2935-2939

2002

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Structure-affinity relationships of 5'-aromatic ethers and 5'-aromatic sulfides as partial A1 adenosine agonists, potential supraventricular anti-arrhythmic agents

Bioorganic & medicinal chemistry letters, 2004-07, Vol.14 (14), p.3793-3797

2004

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Affinity and intrinsic efficacy (IE) of 5'-carbamoyl adenosine analogues for the A1 adenosine receptor: efforts towards the discovery of a chronic ventricular rate control agent for the treatment of atrial fibrillation (AF)

Bioorganic & medicinal chemistry letters, 2004-01, Vol.14 (2), p.535-539

2004

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Discovery of triazolopyridine GS-458967, a late sodium current inhibitor (Late I Na i) of the cardiac Na V 1.5 channel with improved efficacy and potency relative to ranolazine

Bioorganic & medicinal chemistry letters, 2016-07, Vol.26 (13), p.3202-3206

2016

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Discovery of triazolopyridinone GS-462808, a late sodium current inhibitor (Late I Na i) of the cardiac Na v 1.5 channel with improved efficacy and potency relative to ranolazine

Bioorganic & medicinal chemistry letters, 2016-07, Vol.26 (13), p.3207-3211

2016

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Partial A1 Adenosine Receptor Agonists from a Molecular Perspective and Their Potential Use as Chronic Ventricular Rate Control Agents During Atrial Fibrillation (AF)

Current topics in medicinal chemistry, 2004-04, Vol.4 (8), p.839-854

2004

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Using Patchxpress to Screen Blockers of the Cardiac Sodium Channel (Nav1.5) for Effects on Late INA, Peak INA, and Channel Kinetics

Biophysical journal, 2010-01, Vol.98 (3), p.113a-113a

2010

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Affinity and intrinsic efficacy (IE) of 5′-carbamoyl adenosine analogues for the A 1 adenosine receptor—efforts towards the discovery of a chronic ventricular rate control agent for the treatment of atrial fibrillation (AF)

Bioorganic & medicinal chemistry letters, 2004, Vol.14 (2), p.535-539

2004

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Structure–affinity relationships of 5 ′ -aromatic ethers and 5 ′ -aromatic sulfides as partial A 1 adenosine agonists, potential supraventricular anti-arrhythmic agents

Bioorganic & medicinal chemistry letters, 2004-07, Vol.14 (14), p.3793-3797

2004

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CVT-4325: A Potent Fatty Acid Oxidation Inhibitor with Favorable Oral Bioavailability

ChemInform, 2005-04, Vol.36 (15), p.no-no

2005

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Structure‐Affinity Relationships of the Affinity of 2‐Pyrazolyl Adenosine Analogues for the Adenosine A 2A Receptor

ChemInform, 2003-02, Vol.34 (8)

2003

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Structure-Affinity Relationships of the Affinity of 2-Pyrazolyl Adenosine Analogues for the Adenosine A2A Receptor

ChemInform, 2003-02, Vol.34 (8), p.no-no

2003

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A1 adenosine receptor agonists and their potential therapeutic applications

Expert opinion on investigational drugs, 2008-12, Vol.17 (12), p.1901-1910

2008

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Molecule Evoluator CIDRUX BV, Park Oosterspaarn 6, 2036 MB Haarlem, The Netherlands. www. cidrux.com. See Web site for pricing information

Journal of the American Chemical Society, 2007-10, Vol.129 (41), p.12586-12586

Zablocki, Jeff

2007

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Marked difference in saxitoxin and tetrodoxin affinity for the human nociceptive voltage-gated sodium channel (Naᵥ1.7)

Proceedings of the National Academy of Sciences - PNAS, 2012-10, Vol.109 (44), p.18102-18107

2012

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A1 adenosine receptor antagonists, agonists, and allosteric enhancers

Handbook of experimental pharmacology, 2009 (193), p.25

2009

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The novel late Na super(+) current inhibitor, GS-6615 (eleclazine) and its anti-arrhythmic effects in rabbit isolated heart preparations

British journal of pharmacology, 2016-11, Vol.173 (21), p.3088-3098

2016

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A 1 adenosine receptor agonists and their potential therapeutic applications

Expert opinion on investigational drugs, 2008-12, Vol.17 (12), p.1901-1910

2008

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Progress in the discovery of selective, high affinity A2B adenosine receptor antagonists as clinical candidates

Purinergic signalling, 2009, Vol.5 (1), p.21-29

2009

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Discovery of a Novel A2B Adenosine Receptor Antagonist as a Clinical Candidate for Chronic Inflammatory Airway Diseases

Journal of medicinal chemistry, 2008-04, Vol.51 (7), p.2267-2278

2008

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Marked difference in saxitoxin and tetrodotoxin affinity for the human nociceptive voltage-gated sodium channel (Nav1.7)

Proceedings of the National Academy of Sciences - PNAS, 2012-10, Vol.109 (44), p.18102-18107

2012

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Discovery of Dihydrobenzoxazepinone (GS-6615) Late Sodium Current Inhibitor (Late I Nai), a Phase II Agent with Demonstrated Preclinical Anti-Ischemic and Antiarrhythmic Properties

Discovery of triazolopyridinone GS-462808, a late sodium current inhibitor (Late INai) of the cardiac Nav1.5 channel with improved efficacy and potency relative to ranolazine

Discovery of triazolopyridine GS-458967, a late sodium current inhibitor (Late INai) of the cardiac NaV 1.5 channel with improved efficacy and potency relative to ranolazine

Novel short-acting A2A adenosine receptor agonists for coronary vasodilation: inverse relationship between affinity and duration of action of A2A agonists

Structure-affinity relationships of the affinity of 2-pyrazolyl adenosine analogues for the adenosine A2A receptor

Structure-affinity relationships of 5'-aromatic ethers and 5'-aromatic sulfides as partial A1 adenosine agonists, potential supraventricular anti-arrhythmic agents

Affinity and intrinsic efficacy (IE) of 5'-carbamoyl adenosine analogues for the A1 adenosine receptor: efforts towards the discovery of a chronic ventricular rate control agent for the treatment of atrial fibrillation (AF)

Discovery of triazolopyridine GS-458967, a late sodium current inhibitor (Late I Na i) of the cardiac Na V 1.5 channel with improved efficacy and potency relative to ranolazine

Discovery of triazolopyridinone GS-462808, a late sodium current inhibitor (Late I Na i) of the cardiac Na v 1.5 channel with improved efficacy and potency relative to ranolazine

Partial A1 Adenosine Receptor Agonists from a Molecular Perspective and Their Potential Use as Chronic Ventricular Rate Control Agents During Atrial Fibrillation (AF)

Using Patchxpress to Screen Blockers of the Cardiac Sodium Channel (Nav1.5) for Effects on Late INA, Peak INA, and Channel Kinetics

Affinity and intrinsic efficacy (IE) of 5′-carbamoyl adenosine analogues for the A 1 adenosine receptor—efforts towards the discovery of a chronic ventricular rate control agent for the treatment of atrial fibrillation (AF)

Structure–affinity relationships of 5 ′ -aromatic ethers and 5 ′ -aromatic sulfides as partial A 1 adenosine agonists, potential supraventricular anti-arrhythmic agents

CVT-4325: A Potent Fatty Acid Oxidation Inhibitor with Favorable Oral Bioavailability

Structure‐Affinity Relationships of the Affinity of 2‐Pyrazolyl Adenosine Analogues for the Adenosine A 2A Receptor

Structure-Affinity Relationships of the Affinity of 2-Pyrazolyl Adenosine Analogues for the Adenosine A2A Receptor

A1 adenosine receptor agonists and their potential therapeutic applications

Molecule Evoluator CIDRUX BV, Park Oosterspaarn 6, 2036 MB Haarlem, The Netherlands. www. cidrux.com. See Web site for pricing information

Marked difference in saxitoxin and tetrodoxin affinity for the human nociceptive voltage-gated sodium channel (Naᵥ1.7)

A1 adenosine receptor antagonists, agonists, and allosteric enhancers

The novel late Na super(+) current inhibitor, GS-6615 (eleclazine) and its anti-arrhythmic effects in rabbit isolated heart preparations

A 1 adenosine receptor agonists and their potential therapeutic applications

Progress in the discovery of selective, high affinity A2B adenosine receptor antagonists as clinical candidates

Discovery of a Novel A2B Adenosine Receptor Antagonist as a Clinical Candidate for Chronic Inflammatory Airway Diseases

Marked difference in saxitoxin and tetrodotoxin affinity for the human nociceptive voltage-gated sodium channel (Nav1.7)

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