ApconiX Ion Channels archive
Why is Time Critical to hERG Screening Data? ApconiX has worked hard to optimise our processes and is now returning over 80% of hERG screening data back to clients within one week of compound receipt. This allows critical decisions to be made in medicinal chemistry on a full dataset [...]
ApconiX is delighted to welcome Dr Karen Jones who joins us from AstraZeneca. Karen, a talented electrophysiologist, will work with Dr Michael Morton to ensure the laboratory continues to provide an outstanding service as the demand for ion channel and cardiovascular safety screening increases. Karen graduated from the University of Liverpool with a degree in [...]
Abstract K+/Cl- cotransporter 2 (KCC2) is selectively expressed in the adult nervous system and allows neurons to maintain low intracellular Cl- levels. Thus, KCC2 activity is an essential prerequisite for fast hyperpolarizing synaptic inhibition mediated by type A γ-aminobutyric acid (GABAA) receptors, which are Cl--permeable, ligand-gated ion channels. Consistent with this, deficits in the activity of [...]
Read more here: RA Cardarelli, K Jones, LI Pisella, HJ Wobst, LJ McWilliams, PM Sharpe, MP Burnham, DJ Baker, I Chudotvorova, J Guyot, L Silayeva, DH Morrow, N Dekker, S Zicha, PA Davies, J Holenz, ME Duggan, J Dunlop, RJ Mather, Q Wang, I Medina, NJ Brandon, TZ Deeb and SJ Moss. The small molecule [...]
Cardiovascular toxicity often hinders success – are companies picking the wrong compounds? Prolific novelist and academic CS Lewis once said, “Failures are finger posts on the road to achievement.” (Given pharma’s drug failure rate, the road ahead must truly be paved in gold.) When it comes to drug safety failure, toxicity – especially to the [...]
The European Centre of Excellence for preclinical cardiovascular electrophysiology. The ApconiX team is pleased to announce their alliance with PhysioStim to create a new Centre of Excellence dedicated to cardiac safety studies. Both companies team up to offer a complete range of services in nonclinical cardiovascular electrophysiology. ApconiX, based at Alderley Park in the [...]
Pharmacological and electrophysiological characterization of AZSMO-23, an activator of the hERG K(+) channel Abstract: Background and Purpose: We aimed to characterize the pharmacology and electrophysiology of N-[3-(1H-benzimidazol-2-yl)-4-chloro-phenyl]pyridine-3-carboxamide (AZSMO-23), an activator of the human ether-a-go-go-related gene (hERG)-encoded K+ channel (Kv11.1). Experimental Approach: Automated electrophysiology was used to study the pharmacology of [...]
Predicting changes in cardiac myocyte contractility Abstract: Cardiovascular-related adverse drug effects are a major concern for the pharmaceutical industry. Activity of an investigational drug at the L-type calcium channel could manifest in a number of ways, including changes in cardiac contractility. The aim of this study was to define [...]
Abstract: Cardiomyocytes represent one of the most useful models to conduct cardiac research. A single adult heart yields millions of cardiomyocytes, but these cells do not survive for long after isolation. We aimed to determine whether inhibition of myosin II ATPase that is essential for muscle contraction may preserve fully differentiated adult cardiomyocytes. Using [...]
