Host: The Japanese Society of Toxicology
Name : The 50th Annual Meeting of the Japanese Society of Toxicology
Date : June 19, 2023 - June 21, 2023
In life-threatening scenarios, enhanced noradrenaline release induces endogenous analgesia through α2 adrenoceptors of the descending pain inhibitory system. Although α2-adrenergic agonists such as dexmedetomidine have analgesic and opioid-sparing effects, their use is restricted to hospital settings due to potential risks of acute hypertension/hypotension and bradycardia.Recently we found that a newly identified α2B subtype-specific antagonist, promotes noradrenaline release in murine spinal fluid and produces analgesic effects by stimulating the α2A-dependent pain inhibitory pathway. Orally administered ADRIANA has potent analgesic effects in several nociceptive pain models of mice and non-human primates. Genetic loss of the α2B adrenoceptor neutralizes the analgesic effect of ADRIANA in mice. As ADRIANA showed no significant adverse effects in non-clinical tests, we started a phase I/II clinical trial (jRCT2051220144) of the oral tablet of ADRIANA to examine the safety profile and the suppressive effect on postoperative pain in human.
