Chemistry:Apadoline

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Apadoline (INN; 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.[1][2][3][4] It produces effects and adverse effects in humans including analgesia, drowsiness, and headache, among others.[3][5] Its affinities (Ki) for the opioid receptors are 0.55 nM for the κ-opioid receptor, 11.4 nM for the δ-opioid receptor, and 57 nM for the μ-opioid receptor.[5] Apadoline was first described in the scientific literature by 1990.[6][7][8][9][10] It was under development by Rhône-Poulenc in the 1990s and reached phase 2 clinical trials prior to the discontinuation of its development.[1][2] An analogue with greater potency, RP-61127, has also been described.[4][3]

See also

References

  1. ↑ 1.0 1.1 "Apadoline". 9 October 2001. https://adisinsight.springer.com/drugs/800003488. 
  2. ↑ 2.0 2.1 "Delving into the Latest Updates on Apadoline with Synapse". 21 March 2026. https://synapse.patsnap.com/drug/4272f5bd58c84b4a8de475a4980f1059. 
  3. ↑ 3.0 3.1 3.2 "Novel developments with selective, non-peptidic kappa-opioid receptor agonists". Expert Opinion on Investigational Drugs 6 (10): 1351–1368. October 1997. doi:10.1517/13543784.6.10.1351. PMID 15989506. 
  4. ↑ 4.0 4.1 "U-50,488 and the к receptor Part II: 1991–1998". Progress in Drug Research. Basel: Birkhäuser Basel. 1999. pp. 1–51. doi:10.1007/978-3-0348-8735-9_1. ISBN 978-3-0348-9749-5. 
  5. ↑ 5.0 5.1 "Antinociceptive effects of the kappa-opioid receptor agonist RP 60180 compared with pentazocine in an experimental human pain model". Clinical Neuropharmacology 20 (3): 224–233. June 1997. doi:10.1097/00002826-199706000-00006. PMID 9197945. 
  6. ↑ "RP 60180: A novel phenothiazine with high affinity for kappa binding sites and with antinociceptive effects in rodents". Pain 41: S192. 1990. doi:10.1016/0304-3959(90)92520-Z. https://scholar.google.com/scholar?cluster=12704366127619515978. 
  7. ↑ "RP 60180, a new phenothiazine with high affinity for opiate kappa binding sites in animal and human brain". European Journal of Pharmacology 183 (6): 2332. 1990. doi:10.1016/0014-2999(90)93890-3. https://scholar.google.com/scholar?cluster=3112637485516656921. 
  8. ↑ "A parentrally active highly potent analgesic peptide with reduced abuse potential". Pain 41: S192. 1990. doi:10.1016/0304-3959(90)92521-Q. https://scholar.google.com/scholar?cluster=5905358542592960614. 
  9. ↑ 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
  10. ↑ "Effects of RP 60180, a kappa-receptor agonist, on dopamine metabolism and utilization in rat and guinea-pig brain". European Journal of Pharmacology 183 (6): 2330. 1990. doi:10.1016/0014-2999(90)93888-W. https://scholar.google.com/scholar?cluster=9936098597969388256. 



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