Search Results - "Regan, Christopher P"
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Development and characterization of canine‐specific computational models to predict pulsatile arterial hemodynamics and ventricular‐arterial coupling
Published in Physiological reports (01-06-2023)“…Pulsatile hemodynamics analyses provide important information about the ventricular‐arterial system which cannot be inferred by standard blood pressure…”
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2
Association of respiratory failure with inhibition of NaV1.6 in the phrenic nerve
Published in Channels (Austin, Tex.) (31-12-2022)“…As part of a drug discovery effort to identify potent inhibitors of NaV1.7 for the treatment of pain, we observed that inhibitors produced unexpected…”
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Erk5 Null Mice Display Multiple Extraembryonic Vascular and Embryonic Cardiovascular Defects
Published in Proceedings of the National Academy of Sciences - PNAS (09-07-2002)“…Erk5 is a mitogen-activated protein kinase, the biological role of which is largely undefined. Therefore, we deleted the erk5 gene in mice to assess its…”
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4
Design and Synthesis of Novel Isoquinoline-3-nitriles as Orally Bioavailable Kv1.5 Antagonists for the Treatment of Atrial Fibrillation
Published in Journal of medicinal chemistry (30-11-2006)“…Novel 3-cyanoisoquinoline Kv1.5 antagonists have been prepared and evaluated in in vitro and in vivo assays for inhibition of the Kv1.5 potassium channel and…”
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Smooth Muscle–Targeted Knockout of Connexin43 Enhances Neointimal Formation in Response to Vascular Injury
Published in Arteriosclerosis, thrombosis, and vascular biology (01-05-2007)“…OBJECTIVE—Vascular disease alters and reduces connexin expression and a reduction in connexin 43 (Cx43) expression diminishes the extent of atherosclerosis…”
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Calcitonin gene-related peptide receptor antagonism does not affect the severity of myocardial ischemia during atrial pacing in dogs with coronary artery stenosis
Published in The Journal of pharmacology and experimental therapeutics (01-02-2009)“…Calcitonin gene-related peptide (CGRP) is a sensory neuropeptide that also has potent vasodilator activity. There are conflicting preclinical reports regarding…”
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In vivo antiarrhythmic and cardiac electrophysiologic effects of a novel diphenylphosphine oxide IKur blocker (2-isopropyl-5-methylcyclohexyl) diphenylphosphine oxide
Published in The Journal of pharmacology and experimental therapeutics (01-12-2005)“…The antiarrhythmic efficacy of the novel ultrarapid delayed rectifier potassium current (IKur) blocker (2-isopropyl-5-methylcyclohexyl) diphenylphosphine oxide…”
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Autonomic Dysfunction Linked to Inhibition of the Nav1.7 Sodium Channel
Published in Circulation (New York, N.Y.) (23-04-2024)Get full text
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Atrial antifibrillatory effects of structurally distinct IKur blockers 3-[(dimethylamino)methyl]-6-methoxy-2-methyl-4-phenylisoquinolin-1(2H)-one and 2-phenyl-1,1-dipyridin-3-yl-2-pyrrolidin-1-yl-ethanol in dogs with underlying heart failure
Published in The Journal of pharmacology and experimental therapeutics (01-01-2008)“…Drug discovery efforts have focused recently on atrial-selective targets, including the Kv1.5 channel, which underlies the ultrarapid delayed rectifier…”
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Autonomic Dysfunction Linked to Inhibition of the Na v 1.7 Sodium Channel
Published in Circulation (New York, N.Y.) (23-04-2024)Get full text
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11
Characterization of Ubrogepant: A Potent and Selective Antagonist of the Human Calcitonin Gene‒Related Peptide Receptor
Published in The Journal of pharmacology and experimental therapeutics (28-01-2020)“…A growing body of evidence has implicated the calcitonin gene-related peptide (CGRP) receptors in migraine pathophysiology. With the recent approval of…”
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12
A generalized canine transfer function accurately reconstructs central aortic pressure waveforms to enable enhanced pulse wave analysis
Published in Journal of pharmacological and toxicological methods (01-11-2023)“…Routine preclinical blood pressure evaluation is an important risk assessment tool. Although proximal aortic pressure is most relevant for key target organs,…”
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13
In vivo cardiac electrophysiologic effects of a novel diphenylphosphine oxide IKur blocker, (2-Isopropyl-5-methylcyclohexyl) diphenylphosphine oxide, in rat and nonhuman primate
Published in The Journal of pharmacology and experimental therapeutics (01-02-2006)“…The voltage-gated potassium channel, Kv1.5, which underlies the ultrarapid delayed rectifier current, I(Kur), is reported to be enriched in human atrium versus…”
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Attenuation of edema and infarct volume following focal cerebral ischemia by early but not delayed administration of a novel small molecule KDR kinase inhibitor
Published in Neuroscience research (2009)“…Vascular endothelial growth factor (VEGF) may mediate increases in vascular permeability and hence plasma extravasation and edema following cerebral ischemia…”
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Pharmacologic characterization of atogepant: A potent and selective calcitonin gene-related peptide receptor antagonist
Published in Cephalalgia (01-01-2024)“…The trigeminal sensory neuropeptide calcitonin gene-related peptide (CGRP) is identified as an essential element in migraine pathogenesis. and studies…”
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Discovery of triarylethanolamine inhibitors of the Kv1.5 potassium channel
Published in Bioorganic & medicinal chemistry letters (15-04-2010)“…A series of triarylethanolamine inhibitors of the Kv1.5 potassium channel have been prepared and evaluated for their effects in vitro and in vivo. The…”
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Development of a Smooth Muscle–Targeted Cre Recombinase Mouse Reveals Novel Insights Regarding Smooth Muscle Myosin Heavy Chain Promoter Regulation
Published in Circulation research (01-09-2000)“…The use of genetically modified mice has been an important model system to study gene function in cardiovascular development and under pathophysiological…”
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Discovery of sulfone containing metallo-β-lactamase inhibitors with reduced bacterial cell efflux and histamine release issues
Published in Bioorganic & medicinal chemistry letters (01-12-2024)“…[Display omitted] •Gram-Negative Bacterial Coverage.•Anti-bacterial Resistance.•Sulfone Containing Drug.•Histamine Release.•Enzyme-Inhibitor X- Ray…”
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Characterization of ascending dose canine telemetry model supports its use in E14/S7B QT integrated risk assessments
Published in Journal of pharmacological and toxicological methods (01-07-2024)“…Nonclinical evaluation of the cardiovascular effects of novel chemical or biological entities (NCE, NBEs) is crucial for supporting first-in-human clinical…”
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Structure Guided Discovery of Novel Pan Metallo-β-Lactamase Inhibitors with Improved Gram-Negative Bacterial Cell Penetration
Published in Journal of medicinal chemistry (14-03-2024)“…The use of β-lactam (BL) and β-lactamase inhibitor combination to overcome BL antibiotic resistance has been validated through clinically approved drug…”
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