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- Publications
- Influence
Design, synthesis, and evaluation of a novel 4-aminomethyl-4-fluoropiperidine as a T-type Ca2+ channel antagonist.
- W. Shipe, J. Barrow, +27 authors J. Renger
- Chemistry, Medicine
- Journal of medicinal chemistry
- 10 June 2008
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 2… Expand
Iloperidone: Preclinical Profile and Early Clinical Evaluation
- R. Corbett, L. Griffiths, +7 authors S. Kongsamut
- Medicine
- 1 June 1997
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 neural… Expand
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.
- H. Vargas, J. Cuevas, L. Ignarro, G. Chaudhuri
- Chemistry, Medicine
- The Journal of pharmacology and experimental…
- 1 June 1991
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 and… Expand
Current challenges in the evaluation of cardiac safety during drug development: translational medicine meets the Critical Path Initiative.
- J. Piccini, D. Whellan, +6 authors M. Krucoff
- Medicine
- American heart journal
- 1 September 2009
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, and… Expand
Vascular alpha 1D-adrenoceptors have a role in the pressor response to phenylephrine in the pithed rat.
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 studies… Expand
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 to… Expand
Safety pharmacology investigations on the nervous system: An industry survey.
- S. Authier, J. Arezzo, +10 authors M. Curtis
- Medicine
- Journal of pharmacological and toxicological…
- 2 June 2016
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 safety… Expand
Evaluation of drug-induced QT interval prolongation in animal and human studies: a literature review of concordance
- H. Vargas, A. Bass, +7 authors Jean-Pierre Valentin
- Medicine
- British journal of pharmacology
- 14 July 2015
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 QT… Expand
The concordance between nonclinical and phase I clinical cardiovascular assessment from a cross-company data sharing initiative.
- Lorna Ewart, Mike Aylott, +16 authors Jean-Pierre Valentin
- Medicine
- Toxicological sciences : an official journal of…
- 1 December 2014
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 a… Expand
Development of 2-aminooxazoline 3-azaxanthenes as orally efficacious β-secretase inhibitors for the potential treatment of Alzheimer's disease.
- J. J. Chen, Qingyian Liu, +34 authors V. Patel
- Chemistry, Medicine
- Bioorganic & medicinal chemistry letters
- 15 February 2015
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 drug… Expand