Targeting of sodium channel blockers into nociceptors to produce long‐duration analgesia: a systematic study and review

• Published in: British journal of pharmacology Vol. 164; no. 1; pp. 48 - 58
• Main Authors: Roberson, DP, Binshtok, AM, Blasl, F, Bean, BP, Woolf, CJ
• Format: Journal Article
• Language: English
• Published: Oxford, UK Blackwell Publishing Ltd 01.09.2011; Nature Publishing Group
• Subjects: Analgesics - pharmacokinetics; Analgesics - pharmacology; Animals; Anticonvulsants. Antiepileptics. Antiparkinson agents; Biological and medical sciences; differential block; Drug Delivery Systems - methods; lidocaine; Lidocaine - analogs & derivatives; Lidocaine - pharmacokinetics; Lidocaine - pharmacology; long‐duration analgesia; Male; Medical sciences; nerve block; Neuropharmacology; Nociceptors - drug effects; Nociceptors - metabolism; Pain - drug therapy; Pain - metabolism; Pharmacology. Drug treatments; QX‐314; Rats; regional anaesthesia; Reviews; Rodents; Sensory Receptor Cells - metabolism; sodium channel blockers; Sodium Channel Blockers - pharmacokinetics; Sodium Channel Blockers - pharmacology; targeted delivery; TRPV Cation Channels - antagonists & inhibitors; TRPV Cation Channels - metabolism; TRPV1 channels; Targeting; Targeted therapy; sodium channel blockers; long-duration analgesia; Systematic review; targeted delivery; Anticonvulsant; Review; regional anaesthesia; differential block; Target; Nociceptor; TRPV1 vanilloid receptor; Regional anesthesia; QX-314; Duration; Antiarrhythmic agent; Local anesthetic; Analgesia; VR1 vanilloid receptor; TRPV1 channels; Organic amide; Sodium channel blocker; Lidocaine; nerve block

BACKGROUND AND PURPOSE We have developed a strategy to target the permanently charged lidocaine derivative lidocaine N‐ethyl bromide (QX‐314) selectively into nociceptive sensory neurons through the large‐pore transient receptor potential cation channel subfamily V (TRPV1) noxious heat detector chan...