Open AccessNovel Opioid Analgesics for the Development of Transdermal Opioid Patches That Possess Morphine-Like Pharmacological Profiles Rather Than Fentanyl: Possible Opioid Switching Alternatives Among Patch Formula
Author(s) -
Akane Komatsu,
Kanako Miyano,
Daisuke Nakayama,
Yusuke Mizobuchi,
Eiko Uezono,
Kaori Ohshima,
Yusuke Karasawa,
Yui Kuroda,
Miki aka,
Kazuya Yamaguchi,
Masako Iseki,
Yasuhito Uezono,
Masakazu Hayashida
Publication year - 2022
Publication title -
anesthesia and analgesia/anesthesia and analgesia
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.404
H-Index - 201
eISSN - 1526-7598
pISSN - 0003-2999
DOI - 10.1213/ane.0000000000005954
Subject(s) - fentanyl , analgesic , pharmacology , medicine , opioid , morphine , transdermal , opioid receptor , agonist , tail flick test , anesthesia , receptor , nociception
Transdermal fentanyl is widely used in the treatment of severe pain because of convenience, safety, and stable blood concentrations. Nevertheless, patients often develop tolerance to fentanyl, necessitating the use of other opioids; transdermal buprenorphine patch is widely used as an analgesic agent, though available formulation does not provide comparable analgesic effect as transdermal fentanyl patch. Opioids bind to the opioid receptor (OR) to activate both G protein-mediated and β-arrestin-mediated pathways. We synthesized morphine-related compounds with high transdermal absorbability (N1 and N2) and evaluated their OR activities pharmacologically in comparison with fentanyl and morphine.