Open AccessEN3427
Author(s) -
Manish Banerjee,
Atul Kumar Baranwal,
Soumya Saha,
Ashis Kumar Saha,
Tony Priestley
Publication year - 2015
Publication title -
anesthesia and analgesia/anesthesia and analgesia
Language(s) - Uncategorized
Resource type - Journals
SCImago Journal Rank - 1.404
H-Index - 201
eISSN - 1526-7598
pISSN - 0003-2999
DOI - 10.1213/ane.0000000000000629
Subject(s) - medicine , lidocaine , local anesthetic , nociceptor , nociception , anesthesia , anesthetic , noxious stimulus , pharmacology , neuropharmacology , in vivo , analysis of variance , neuroscience , receptor , microbiology and biotechnology , biology
Currently approved local anesthetic drugs provide relatively brief local anesthesia that is appropriate and even desirable in some settings, but an extended duration of action beyond their capabilities would be a distinct benefit in other clinical situations. We implemented a drug discovery program that sought to identify novel local anesthetic molecules that specifically demonstrated a long-acting, preferential action on nociceptor sensory afferents that expressed transient receptor potential (TRP) channels. The hypothesis we tested was whether relatively membrane-impermeant local anesthetic molecules could confer long-lasting anesthesia if neuronal access was facilitated by TRP channel activation. The current work describes in vivo studies on a lead molecule that emerged from the discovery program, EN3427, in several rodent pain models.