Drug Discovery for Peripheral Nervous System Channelopathies

Treatment of pain remains challenging. Understanding channelopathies promises to improve pain management. Creative Bioarray is dedicated to helping clients develop drugs to treat peripheral nervous system (PNS) channelopathies, including genetic mutations in voltage-gated sodium, potassium, and transient receptor potential channels. We focus on the discovery of ion channel modulators, opening the way for the development of personalized therapies with higher efficacy and fewer side effects.

Introduction

Chronic pain represents a substantial health burden, affecting one in five people in Europe; for 40% of these people, undertreatment remains a problem. A common acquired chronic pain state is associated with altered expression and dysfunction of ion channels. Variations in ion channels modulate the risk, severity, and persistence of pain after an injury. At present, various types of PNS channelopathies have been identified.

Some channelopathies increase pain sensitivity and partially reduce pain sensitivity, for example, the three voltage-gated sodium channels Na_v1.7, Na_v1.8, and Na_v1.9 have important roles in acute pain perception. Identifying the important role of channelopathies in pain mechanisms can provide basic knowledge for the development of analgesic drugs, which is expected to improve the quality of treatment.

Fig. 1 Structure and functional components of a nociceptor. (Bennett, 2014)

Drug Development for PNS Channelopathies

PNS channelopathies include hereditary erythromelalgia (IEM), paroxysmal extreme pain disorder (PEPD), painful small fiber neuropathy (SFN), and familial episodic pain syndrome (FEPS). Various genes encoding ion channels including SCN9A (Na_v1.7), SCN10A (Na_v1.8), SCN11A (Na_v1.9), and TRPA1 (Trpa1) have been shown to be involved in the development of these channelopathies. We aim to help clients develop a variety of ion channel modulators for pain relief through different mechanisms of action, such as calcium channel blockers and Nav blockers. Our drug development services include, but are not limited to:

Analysis of the location and function of channel subunits involved in PNS channelopathies.
Analysis of the consequences of channel subunit mutations on biophysical properties of nociceptors.
Development of animal models of PNS channelopathies.
Development of selective and/or potent sodium channel blockers for inflammatory and neuropathic pain.
Development of capsaicin or lidocaine patches, botulinum toxin, and cannabinoids.

Advantages

Integrated, multidisciplinary drug discovery expertise
Unparalleled scope of capabilities in targets and therapeutic areas
Comprehensive laboratory services and efficient technical support
Facilities around the world to support your discovery programs

With extensive experience in the field of drug development and advanced ion channel analysis platform, Creative Bioarray has made great progress in drug development for PNS channelopathies caused by channel dysfunction. We look forward to helping clients design pharmacogenetic strategies to identify the most effective drug for diverse mutations. If you are interested in our services, please contact us for more details.

Reference

Bennett, D. L. H.; Woods, C. G. Painful and painless channelopathies. The Lancet Neurology, 2014, 13(6): 587-599.

For Research Use Only.