Sensory & Pain System
Nebivolol as a Potent TRPM8 Channel Blocker: A Drug-Screening Approach through Automated Patch Clamping and Ligand-Based Virtual Screening
In this featured article, Jahanfar et al. aimed to discover novel transient receptor potential melastatin 8 (TRPM8) blocking agents. The TRPM8 ion channel has been implicated in various conditions, including neuropathic pain and cancer. The investigators leveraged the IonFlux Mercury to screen and determine the EC50 for a subset of 12 sodium ion channel blockers and 7 β-blockers.
Over the past decade, our understanding of ion channel function has significantly advanced thanks to groundbreaking developments in molecular genetics and cellular electrophysiology. This newfound knowledge has shed light on the crucial role that ion channels play in the sensory nervous system, where they are widely distributed.
IonFlux Mercury systems are especially well-suited for neuronal voltage-gated and ligand-gated patch clamp research. Ion channels can be transfected into recombinant cell lines or induced pluripotent stem cells (iPSC).
Important IonFlux Mercury Characteristics:
Fast solution exchange
READY FOR Optogenetics assays
Nicotinic Acetylcholine Receptors
Transient Receptor Potential Channels
Investigating Potent Blockers of TRPM8
IonFlux 16 was used in a recent study aiming to discover novel TRPM8 channel block using automated patch clamp combined with ligand-based virtual screening.
Screening positive allosteric modulators for NMDA Receptors
NMDAR hypofunction is implicated in the pathophysiology of schizophrenia. Positive allosteric modulators (PAMs) are molecules capable of enhancing a receptor's signal. In a recent study, IonFlux HT technology was used in a screening pipeline to identify GluN2A selective NMDAR PAMs.
Identifying potential analgesic candidates
Glycine receptors play a key role in mediating inhibitory neurotransmission and hence contribute to the regulation of pain signaling in the dorsal horn. This recent study used IonFlux HT technology to identify positive allosteric modulators for GlyRα3.