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| http://dx.doi.org/10.1053/j.ajkd.2013.08.015 | DOI Listing |
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Updates on Intrinsic Medicinal Chemistry of 1,4-dihydropyridines, Perspectives on Synthesis and Pharmacokinetics of Novel 1,4-dihydropyrimidines as Calcium Channel Blockers: Clinical Pharmacology.
Curr Top Med Chem
January 2025
Department of Pharmaceutical Chemistry, JSS College of Pharmacy, JSS Academy of Higher Education & Research (JSS AHER), Mysuru, Karnataka, India.
Background: Several chemical studies described the physiological efficacy of 1,4- dihydropyridines (DHPs). DHPs bind to specific sites on the α1 subunit of L-type calcium channels, where they demonstrate a more pronounced inhibition of Ca2+ influx in vascular smooth muscle compared to myocardial tissue. This selective inhibition is the basis for their preferential vasodilatory action on peripheral and coronary arteries, a characteristic that underlies their therapeutic utility in managing hypertension and angina.
View Article and Find Full Text PDFHaloperidol dopamine receptor occupancy and antagonism correspond to delirium agitation scores and EPS risk: A PBPK-PD modeling analysis.
J Psychopharmacol
January 2025
Department of Psychiatry, University of Pennsylvania Perelman School of Medicine, Philadelphia, PA, USA.
Background: Delirium is a severe neuropsychiatric disorder associated with increased morbidity and mortality. Numerous precipitating factors and etiologies merge into the pathophysiology of this condition which can be marked by agitation and psychosis. Judicious use of antipsychotic medications such as intravenous haloperidol reduces these symptoms and distress in critically ill individuals.
View Article and Find Full Text PDFJanus LAAM-loaded electrospun fibrous buccal films for treating opioid use disorder.
Biomaterials
December 2024
Department of Pharmaceutics, Virginia Commonwealth University, Richmond, VA, 23298, USA; Department of Ophthalmology, Virginia Commonwealth University, Richmond, VA, 23298, USA; Department of Biomedical Engineering, Virginia Commonwealth University, Richmond, VA, 23298, USA; Center for Pharmaceutical Engineering, Center for Drug Discovery, Department of Pediatrics, and Massey Cancer Center, Virginia Commonwealth University, Richmond, VA, 23298, USA. Electronic address:
The opioid crisis has claimed approximately one million lives in the United States since 1999, underscoring a significant public health concern. This surge in opioid use disorder (OUD) fatalities necessitates improved therapeutic options. Current OUD therapies often require daily clinical visits, leading to poor patient compliance and high costs to the health systems.
View Article and Find Full Text PDFBasic Science and Pathogenesis.
Alzheimers Dement
December 2024
Indiana University, Indianapolis, IN, USA.
Background: Preclinical testing in animal models is a critical component of the drug discovery process. Over the past three decades hundreds of interventions have demonstrated preclinical efficacy for ameliorating cognitive impairments in animal models; however, none have translated to efficacy in Alzheimer's disease (AD) clinical trials. This lack of translation suggests that there are issues with the animal models employed, the preclinical assays, and poor scientific rigor and reproducibility during execution.
View Article and Find Full Text PDFBasic Science and Pathogenesis.
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Indiana University School of Medicine, Indianapolis, IN, USA.
Background: Although pharmacokinetics and pharmacodynamics of biotherapeutics are commonly studied through ELISAs; however, the extremely strong binding of modern antibody-based therapeutics result in background, inability of secondary antibody binding, and nonlinear response curves. The selectivity and specificity imparted through the use of liquid chromatography-targeted mass spectrometry (LC-MS/MS) allows for absolute quantitation of chosen peptides. For MODEL-AD, here we present a high-throughput workflow for absolute quantification of chimeric aducanumab from cortex and plasma of 5XFAD mice.
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