Apadoline (; developmental code name RP-60180) is a κ-opioid receptor agonist and experimental analgesic which was under development for the treatment of cancer pain but was never marketed. It produces effects and adverse effects in humans including analgesia, drowsiness, and headache, among others. Its affinities (Ki) for the opioid receptors are 0.55nM for the κ-opioid receptor, 11.4nM for the δ-opioid receptor, and 57nM for the μ-opioid receptor. Apadoline was first described in the scientific literature by 1990.Reibaud, M., Stutzmann, J. M., Böhme, G. A., Lafforgue, J., Garret, C., & Laduron, P. M. (1990). Electrocorticograpnic profile and discriminative stimulus properties of RP 60180, a new kappa agonist. European Journal of Pharmacology, 183(6), 2331. https://scholar.google.com/scholar?cluster=6360720396979939973 It was under development by Rhône-Poulenc in the 1990s and reached phase 2 clinical trials prior to the discontinuation of its development. An analogue with greater potency, RP-61127, has also been described.

See also List of investigational analgesics κ-Opioid receptor agonist

References