Apadoline
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| Other names | RP-60180; RP60180; RP-60,180; RP-60180A |
| Drug class | κ-Opioid receptor agonist |
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| Formula | C23H29N3OS |
| Molar mass | 395.57 g·mol−1 |
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Apadoline (INN Tooltip International Nonproprietary Name; 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
[edit ]References
[edit ]- ^ a b "Apadoline". AdisInsight. 9 October 2001. Retrieved 15 May 2026.
- ^ a b "Delving into the Latest Updates on Apadoline with Synapse". Synapse. 21 March 2026. Retrieved 15 May 2026.
- ^ a b c Barber A, Gottschlich R (October 1997). "Novel developments with selective, non-peptidic kappa-opioid receptor agonists". Expert Opinion on Investigational Drugs. 6 (10): 1351–1368. doi:10.1517/13543784.6.10.1351. PMID 15989506.
- ^ a b Szmuszkovicz J (1999). "U-50,488 and the к receptor Part II: 1991–1998". Progress in Drug Research. Basel: Birkhäuser Basel. pp. 1–51. doi:10.1007/978-3-0348-8735-9_1. ISBN 978-3-0348-9749-5.
- ^ a b Lötsch J, Ditterich W, Hummel T, Kobal G (June 1997). "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. doi:10.1097/00002826-199706000-00006. PMID 9197945.
- ^ Fardin V, Plau B, Carruette A, Guyon C, Bardon T, Taurand G, et al. (1990). "RP 60180: A novel phenothiazine with high affinity for kappa binding sites and with antinociceptive effects in rodents". Pain. 41: S192. doi:10.1016/0304-3959(90)92520-Z.
- ^ Fardin V, Jolly A, Flamand O, Carruette A, Laduron PM, Garret C (1990). "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. doi:10.1016/0014-2999(90)93890-3.
- ^ Raghubir R, Patnaik GK, Sharma SD, Mathur KB, Dhawan BN (1990). "A parentrally active highly potent analgesic peptide with reduced abuse potential". Pain. 41: S192. doi:10.1016/0304-3959(90)92521-Q.
- ^ 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
- ^ Boireau A, Dubedat P, Laduron P, Blanchard JC, Doble A, Garret C (1990). "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. doi:10.1016/0014-2999(90)93888-W.
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