Chemistry:RU-24213

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RU-24213, also known as 3-hydroxy-N-propyl-N-(phenylethyl)phenethylamine, is a dopamine receptor agonist of the phenethylamine family related to dopamine.[1][2][3] It is a selective dopamine D2-like receptor agonist.[1][3] Subsequently, however, RU-24213 was found to also act as a potent κ-opioid receptor (KOR) antagonist.[2][4] It led to the development of the diphenylethylamine series of KOR ligands.[4][5] RU-24213 was first described in the scientific literature in 1978.[4][6]

See also

References

  1. ↑ 1.0 1.1 "New classes of selective D-1 dopamine receptor antagonist provide further evidence for two directions of D-1:D-2 interaction". Neurochemistry International 20 Suppl: 135S–139S. March 1992. doi:10.1016/0197-0186(92)90226-h. PMID 1365412. 
  2. ↑ 2.0 2.1 "The dopamine D2 agonists RU 24213 and RU 24926 are also kappa-opioid receptor antagonists". Neuropharmacology 30 (4): 409–412. April 1991. doi:10.1016/0028-3908(91)90068-m. PMID 1677169. 
  3. ↑ 3.0 3.1 "Two dopamine receptors: biochemistry, physiology and pharmacology". Life Sciences 35 (23): 2281–2296. December 1984. doi:10.1016/0024-3205(84)90519-8. PMID 6390056. 
  4. ↑ 4.0 4.1 4.2 "Kappa Opioid Receptor Ligands and Pharmacology: Diphenethylamines, a Class of Structurally Distinct, Selective Kappa Opioid Ligands". Handbook of Experimental Pharmacology. 271. 2022. pp. 163–195. doi:10.1007/164_2020_431. ISBN 978-3-030-89073-5. "The synthesis of the first diphenethylamine derivative, RU 24213 (1) (Fig. 10), was reported in 1978, originally developed as a potential anti-Parkinson’s drug (Nedelec et al. 1978). RU 24213 (1) was described as a selective dopamine D2 receptor agonist (Euvrard et al. 1980), also found to bind with moderate affinity and selectivity to KOR and to have a KOR antagonist activity in vitro (Fortin et al. 1991). [...] These simple structures were used as leads for the design of small molecules targeting the KOR and featuring a diphenethylamine scaffold. [...]" 
  5. ↑ "Discovery and pharmacological evaluation of a diphenethylamine derivative (HS665), a highly potent and selective κ opioid receptor agonist". Journal of Medicinal Chemistry 55 (22): 10302–10306. November 2012. doi:10.1021/jm301258w. PMID 23134120. 
  6. ↑ "Synthèse et étude de l'activité dopaminergique de dérivés de la di (phénéthyl) amine.". European Journal of Medicinal Chemistry 13 (6): 553–563. 1978. https://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=PASCAL7960348032. Retrieved 31 January 2026. 



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