• Publications
  • Influence
Design, synthesis, and evaluation of a novel 4-aminomethyl-4-fluoropiperidine as a T-type Ca2+ channel antagonist.
The novel T-type antagonist ( S)- 5 has been prepared and evaluated in in vitro and in vivo assays for T-type calcium ion channel activity. Structural modification of the piperidine leads 1 and 2Expand
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Iloperidone: Preclinical Profile and Early Clinical Evaluation
Schizophrenia is a severe mental illness affecting an estimated 1% of the world's population (73). The disease has an uncertain pathophysiology possibly leading to disruption of dopaminergic neuralExpand
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Comparison of the inhibitory potencies of N(G)-methyl-, N(G)-nitro- and N(G)-amino-L-arginine on EDRF function in the rat: evidence for continuous basal EDRF release.
The relative potencies of the argininolytic agents NG-methyl-L-arginine (L-NMA), NG-nitro-L-arginine (L-NNA) and NG-amino-L-arginine (L-NAA) were assayed by their inhibitory effect on both basal andExpand
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Current challenges in the evaluation of cardiac safety during drug development: translational medicine meets the Critical Path Initiative.
In October 2008, in a public forum organized by the Cardiac Safety Research Consortium and the Health and Environmental Sciences Institute, leaders from government, the pharmaceutical industry, andExpand
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Vascular alpha 1D-adrenoceptors have a role in the pressor response to phenylephrine in the pithed rat.
  • L. Zhou, H. Vargas
  • Chemistry, Medicine
  • European journal of pharmacology
  • 3 June 1996
In rats, the pressor response to intravenous (i.v.) phenylephrine is mediated by vascular alpha 1A- and alpha 1B-adrenoceptors, but the role of alpha 1D-adrenoceptors is uncertain. These studiesExpand
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Proarrhythmia Risk Assessment in Human Induced Pluripotent Stem Cell-Derived Cardiomyocytes Using the Maestro MEA Platform.
  • Yusheng Qu, H. Vargas
  • Medicine, Chemistry
  • Toxicological sciences : an official journal of…
  • 1 September 2015
Evaluation of stem cell-derived cardiomyocytes (SC-CM) using multi-electrode array (MEA) has attracted attention as a novel model to detect drug-induced arrhythmia. An experiment was conducted toExpand
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Safety pharmacology investigations on the nervous system: An industry survey.
The Safety Pharmacology Society (SPS) conducted an industry survey in 2015 to identify industry practices as they relate to central, peripheral and autonomic nervous system ('CNS') drug safetyExpand
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Evaluation of drug-induced QT interval prolongation in animal and human studies: a literature review of concordance
Evaluating whether a new medication prolongs QT intervals is a critical safety activity that is conducted in a sensitive animal model during non‐clinical drug development. The importance of QTExpand
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The concordance between nonclinical and phase I clinical cardiovascular assessment from a cross-company data sharing initiative.
It is widely accepted that more needs to be done to bring new, safe, and efficacious drugs to the market. Cardiovascular toxicity detected both in early drug discovery as well as in the clinic, is aExpand
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Development of 2-aminooxazoline 3-azaxanthenes as orally efficacious β-secretase inhibitors for the potential treatment of Alzheimer's disease.
The β-site amyloid precursor protein (APP) cleaving enzyme 1 (BACE1) is one of the most hotly pursued targets for the treatment of Alzheimer's disease. We used a structure- and property-based drugExpand
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