ApconiX Welcomes George Buchanan

George joins ApconiX as a placement student for the month of August.  George graduated from the University of Newcastle last year after studying Biology.  He decided to take a year out before beginning a master’s degree in stem cell technology and regenerative medicine at the University of Nottingham in September. George was keen to gain [...]

By |2018-07-31T13:02:03+00:00July 31st, 2018|Ion Channels, Careers|Comments Off on ApconiX Welcomes George Buchanan

ApconiX Welcomes Katie Cox

Katie joins ApconiX as a placement student for the month of July.  Katie, a third-year student from Sheffield University studying Biomedical Sciences hopes to carry on with her studies and complete a master’s degree at Sheffield after graduation. Eager to gain experience of a real-world laboratory, Katie took her tutor’s advice and applied.  Dr Stephen [...]

By |2018-07-31T10:46:01+00:00July 5th, 2018|Ion Channels, Careers|Comments Off on ApconiX Welcomes Katie Cox

ApconiX Return Over 80% of hERG Screening Data to Clients Within One Week

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 of compound properties, avoiding mistakes and [...]

By |2018-07-19T16:25:00+00:00March 5th, 2018|Ion Channels|Comments Off on ApconiX Return Over 80% of hERG Screening Data to Clients Within One Week

ApconiX Welcomes Dr Karen Jones to The Team.

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 [...]

By |2018-07-11T14:36:29+00:00December 2nd, 2017|Ion Channels, Careers|Comments Off on ApconiX Welcomes Dr Karen Jones to The Team.

N-Ethylmaleimide increases KCC2 cotransporter activity by modulating transporter phosphorylation.

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 KCC2 [...]

By |2018-07-05T13:46:47+00:00December 1st, 2017|Ion Channels, Publications|Comments Off on N-Ethylmaleimide increases KCC2 cotransporter activity by modulating transporter phosphorylation.

The small molecule CLP257 does not modify activity of the K+/Cl- co-transporter KCC2 but does potentiate GABA A receptor activity.

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 CLP257 [...]

By |2018-07-11T14:46:53+00:00December 1st, 2017|Ion Channels, Publications|Comments Off on The small molecule CLP257 does not modify activity of the K+/Cl- co-transporter KCC2 but does potentiate GABA A receptor activity.

Learning from Failure

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 [...]

By |2018-07-11T15:26:46+00:00November 2nd, 2017|Ion Channels, Press|Comments Off on Learning from Failure

ApconiX Announce Their Alliance with PhysioStim.

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 U.K. [...]

By |2018-06-20T16:06:07+00:00September 21st, 2017|Ion Channels, Press|Comments Off on ApconiX Announce Their Alliance with PhysioStim.

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 AZSMO-23 on wild-type (WT), Y652A, F656T or G628C/S631C hERG, and on other cardiac ion channels. Its mechanism of action [...]

By |2018-06-20T16:06:22+00:00June 20th, 2015|Ion Channels, Publications|Comments Off on Pharmacological and electrophysiological characterization of AZSMO-23, an activator of the hERG K(+) channel

Predicting changes in cardiac myocyte contractility during early drug discovery with in vitro assays

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 which of the two assay technologies - radioligand-binding or automated electrophysiology - [...]

By |2018-06-20T16:43:00+00:00September 20th, 2014|Ion Channels, Publications|Comments Off on Predicting changes in cardiac myocyte contractility during early drug discovery with in vitro assays