Results 61 to 70 of about 31,065 (253)

Modelling species selectivity in rat and human cytochrome P450 2D enzymes. [PDF]

open access: yesPLoS ONE, 2013
Updated models of the Rat Cytochrome P450 2D enzymes are produced based on the recent x-ray structures of the Human P450 2D6 enzyme both with and without a ligand bound. The differences in species selectivity between the epimers quinine and quinidine are
Grace H C Edmund   +2 more
doaj   +1 more source

Organocatalytic stereodivergent synthesis of β,β-disubstituted-α-aminoacids [PDF]

open access: yes, 2017
In this work, we present an organocatalytic stereodivergent synthesis of β,β-disubstituted-α-aminoacids using arylidene azlactones as starting materials.
Martinelli, Ada
core  

Block of mouse Slo1 and Slo3 K+ channels by CTX, IbTX, TEA, 4-AP and quinidine [PDF]

open access: yes, 2010
pH-regulated Slo3 channels, perhaps exclusively expressed in mammalian sperm, may play a role in alkalization-mediated K(+) fluxes associated with sperm capacitation.
Lingle, Christopher J   +3 more
core   +2 more sources

Exposure–Response Analysis for Aripiprazole Once‐Monthly in Patients Diagnosed With Bipolar I Disorder

open access: yesClinical Pharmacology in Drug Development, EarlyView.
Abstract Aripiprazole once‐monthly (AOM) is approved for the maintenance monotherapy treatment of bipolar I disorder (BP‐I) in adults. A previously developed population pharmacokinetic model was validated by applying it to data from patients diagnosed with BP‐I.
Xiaofeng Wang   +10 more
wiley   +1 more source

Quantitative Comparison of Effects of Dofetilide, Sotalol, Quinidine, and Verapamil between Human Ex vivo Trabeculae and In silico Ventricular Models Incorporating Inter-Individual Action Potential Variability

open access: yesFrontiers in Physiology, 2017
Background:In silico modeling could soon become a mainstream method of pro-arrhythmic risk assessment in drug development. However, a lack of human-specific data and appropriate modeling techniques has previously prevented quantitative comparison of drug
Oliver J. Britton   +5 more
doaj   +1 more source

J-wave syndromes: Brugada and early repolarization syndromes. [PDF]

open access: yes, 2015
A prominent J wave is encountered in a number of life-threatening cardiac arrhythmia syndromes, including the Brugada syndrome and early repolarization syndromes.
Antzelevitch, Charles, Yan, Gan-Xin
core   +2 more sources

Predicting OCT2/MATEs‐Mediated Drug Interactions in Healthy Volunteers and Patients with Chronic Kidney Disease: Insights from Extended Clearance Concept, Endogenous Biomarkers, and In Vitro Inhibition Studies (Perspectives from the International Transporter Consortium)

open access: yesClinical Pharmacology &Therapeutics, EarlyView.
Organic cation transporter (OCT) 2 and multidrug and toxin extrusion (MATE) transporters play significant roles in the renal secretion of organic cations and drug–drug interactions (DDIs). Recent in vitro studies indicate that the Ki values for OCT2 exhibit substrate dependency and increase in potency with pre‐incubation.
Satoshi Asano   +8 more
wiley   +1 more source

Heme crystallization in a Chagas disease vector acts as a redox-protective mechanism to allow insect reproduction and parasite infection. [PDF]

open access: yesPLoS Neglected Tropical Diseases, 2018
Heme crystallization as hemozoin represents the dominant mechanism of heme disposal in blood feeding triatomine insect vectors of the Chagas disease. The absence of drugs or vaccine for the Chagas disease causative agent, the parasite Trypanosoma cruzi ...
Caroline M Ferreira   +12 more
doaj   +1 more source

Simultaneous knockout of Slo3 and CatSper1 abolishes all alkalization- and voltage-activated current in mouse spermatozoa [PDF]

open access: yes, 2013
During passage through the female reproductive tract, mammalian sperm undergo a maturation process termed capacitation that renders sperm competent to produce fertilization.
Clapham, David E.   +4 more
core   +2 more sources

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