RWJ-394,674

Overview
RWJ-394,674 is a drug which is used in scientific research. It is a potent, orally active analgesic drug, which produces little respiratory depression. RWJ-394,674 itself is a potent and selective agonist for δ-opioid receptors, with a Ki of 0.24nM at δ and 72nM at μ. However once inside the body, RWJ-394,674 is dealkylated to its monodesethyl metabolite RWJ-413,216 which is a potent agonist at the μ-opioid receptor and has less affinity for δ (Ki 0.26nM at μ, 46.7nM at δ). The effect of RWJ-394,674 when administered in vivo thus produces potent agonist effects at both μ and δ receptors through the combined actions of the parent drug and its active metabolite, with the δ-agonist effects counteracting the respiratory depression from the μ-opioid effects, and the only prominent side effect being sedation.