Pharmacology and Mechanism of Action of Suzetrigine, a Potent and Selective Na

• Tác giả: Kathleen Aertgeerts, Tiffany Healey, Nicole W Hurst, Swapna Immani, Tim Indersmitten, Sandra M Lechner, Paul A Negulescu, Jeremiah D Osteen, Tim L Tapley
• Ngôn ngữ: eng
• Thông tin xuất bản: New Zealand : Pain and therapy , 2025
• Bộ sưu tập: NCBI
• ID: 716352

Tóm tắt

INTRODUCTION: There is a high unmet need for safe and effective non-opioid medicines to treat moderate to severe pain without risk of addiction. Voltage-gated sodium channel 1.8 (Na METHODS: Preclinical pharmacology and mechanism of action studies were performed in vitro using electrophysiology and radiolabeled binding methods in cells recombinantly expressing human Na RESULTS: Suzetrigine is selective against all other Na CONCLUSIONS: The comprehensive pharmacology assessment presented here indicates that suzetrigine represents the first in a new class of non-opioid analgesics that are selective Na