Results 51 to 60 of about 31,065 (253)

Identification of New KCNT1‐Epilepsy Drugs by In Silico, Cell, and Drosophila Modeling

Annals of Neurology, EarlyView.
Objective Hyperactive KCNT1 potassium channels, caused by gain‐of‐function mutations, are associated with a range of epilepsy disorders. Patients typically experience drug‐resistant seizures and, in cases with infantile onset, developmental regression can follow.
Michael G. Ricos, Bethan A. Cole, Rashid Hussain, Grigori Y. Rychkov, Zeeshan Shaukat, Nadia Pilati, Stephen P. Muench, Katie J. Simmons, Leanne M. Dibbens, Jonathan D. Lippiat   +9 more
wiley   +1 more source

Computational Analysis of the Mode of Action of Disopyramide and Quinidine on hERG-Linked Short QT Syndrome in Human Ventricles

Frontiers in Physiology, 2017
The short QT syndrome (SQTS) is a rare cardiac disorder associated with arrhythmias and sudden death. Gain-of-function mutations to potassium channels mediating the rapid delayed rectifier current, IKr, underlie SQTS variant 1 (SQT1), in which treatment ...
Dominic G. Whittaker, Haibo Ni, Alan P. Benson, Alan P. Benson, Jules C. Hancox, Jules C. Hancox, Henggui Zhang, Henggui Zhang, Henggui Zhang   +8 more
doaj   +1 more source

The effects of repetitive electric cardiac stimulation in dogs with normal hearts, complete heart block and experimental cardiac arrest [PDF]

, 1955
Direct cardiac stimulation was conducted in the open chest. In normal animals, auricular stimulation at frequencies faster than the spontaneous rate caused little change in vascular pressures or cardiac output.
GAERTNER, RA, STARZL, TE, WEBB, RC
core   +1 more source

Chemical Composition, Antioxidant, and Antibacterial Activities of Mezilaurus duckei (Lauraceae)

Chemistry &Biodiversity, EarlyView.
ABSTRACT Mezilaurus duckei, a Brazilian endemic tree species found exclusively in the Amazon Rainforest, is primarily exploited for timber in construction. Due to its endangered status, this study aimed to investigate the chemical profile and biological properties of the ethanolic extract and its phases derived from M. duckei leaves. Chemical profiling
Bruna S. Moroto, Valéria S. Gonçalves, David J. Machate, Talita V. Freire, Érica L. Santos, Flávio M. Alves, Ana C. Micheletti, Nídia C. Yoshida   +7 more
wiley   +1 more source

Inhibition of ATP-Sensitive K+ Channels and L-Type Ca2+ Channels by Amiodarone Elicits Contradictory Effect on Insulin Secretion in MIN6 Cells

Journal of Pharmacological Sciences, 2011
.: Some class I antiarrhythmic drugs induce a sporadic hypoglycemia by producing insulin secretion via inhibition of ATP-sensitive K+ (KATP) channels of pancreatic β-cells.
Atsushi Nishida, Taichi Takizawa, Akio Matsumoto, Takashi Miki, Susumu Seino, Haruaki Nakaya   +5 more
doaj   +1 more source

A Common Genetic Variant Risk Score is Associated with Drug-Induced QT Prolongation and Torsade de Pointes Risk: A Pilot Study. [PDF]

, 2017
Background -Drug-induced QT interval prolongation, a risk factor for life-threatening ventricular arrhythmias, is a potential side effect of many marketed and withdrawn medications.
Behr, ER, Blinova, K, Johannesen, L, Kosova, G, Mason, JW, Newton-Cheh, C, Roden, DM, Rosenberg, MA, Strauss, DG, Vicente, J, Weeke, P, Woosley, R   +11 more
core   +2 more sources

Enantioselective Desymmetrization by Chiral Bifunctional H‐Bonding Organocatalysts

Chemistry – A European Journal, EarlyView.
Enantioselective desymmetrization has emerged as a highly efficient and conceptually elegant strategy for the construction of chiral molecules from readily available prochiral substrates. This review focuses on recent developments in organocatalytic desymmetrization reactions, with particular emphasis on approaches involving bifunctional activation ...
Michal Urban, Jan Veselý
wiley   +1 more source

Characterization of porcine hepatic and intestinal drug metabolizing CYP450 : comparison with human orthologues from a quantitative, activity and selectivity perspective [PDF]

, 2019
Over the past two decades, the pig has gained attention as a potential model for human drug metabolism. Cytochrome P450 enzymes (CYP450), a superfamily of biotransformation enzymes, are pivotal in drug metabolism.
Croubels, Siska, De Clerck, Laura, Deforce, Dieter, Devreese, Mathias, Govaert, Elisabeth, Millecam, Joske, Schelstraete, Wim, Van Bocxlaer, Jan   +7 more
core   +1 more source

Potent Antisickling Furaldehyde Analogs for Acute Sickle Cell Therapy: Enhanced Efficacy and Intravenous Formulation Potential

ChemMedChem, EarlyView.
This study reports novel 5‐HMF analogs with potent antisickling activities. Lead compound MMA509 enhances hemoglobin oxygen affinity and prevents erythrocyte sickling. Crystal structure of hemoglobin‐MMA509 complex explains MMA509 mechanism of action. An IV formulation is successfully developed, positioning MMA509 as a promising fast‐acting treatment ...
Abdelsattar M. Omar, Moustafa E. El‐Araby, Tarek A. Ahmed, Akua K. Donkor, Albert Opare, Mohini S. Ghatge, Anfal S. Aljahdali, Rana T. Alhashimi, Trevohn N. Robinson, Benita Balogun, Mariana Macias, Salma Roland, Yan Zhang, Faik N. Musayev, Osheiza Abdulmalik, Martin K. Safo   +15 more
wiley   +1 more source

Brugada syndrome update

Frontiers in Physiology
Brugada syndrome (BrS), a genetic disorder affecting cardiac ion channels, predominantly manifests due to mutations that impair the function of the Nav1.5 sodium channel’s α-subunit.
Tingting Xu, Shaokun Wang, Jiawen Wang, Jihong Xing   +3 more
doaj   +1 more source