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RU-29717, also known as N-propyl-9-oxaergoline or as 6-propyl-9-oxaergoline (POE), is a dopamine receptor agonist and serotonin receptor modulator of the 9-oxaergoline family closely related to ergolines such as pergolide.[1] It produces effects including suppression of prolactin secretion, hypotension, emesis, stereotypy, and antiparkinsonian-like effects in animals.[1][2] In addition to its dopamine receptor agonism, RU-29717 shows affinity for serotonin receptors (e.g., 5-HT1 and 5-HT2 receptors), with much higher affinity for the serotonin 5-HT1 receptors than the related dopamine receptor agonist pergolide, though RU-29717’s affinity for serotonin 5-HT2 receptors is much lower than for serotonin 5-HT1 receptors.[1][3] Relatedly, RU-29717 also caused short-lasting head twitches in rodents, which were hypothesized to be due to serotonin receptor agonism.[1] The head-twitch response is notable in being a behavioral proxy of psychedelic effects caused by serotonin 5-HT2A receptor agonism.[4][5] RU-29717 was described in the scientific literature in 1983 and was patented in 1985.[1][6][2]

See also

References

  1. ^ a b c d e Boissier JR, Euvrard C, Oberlander C, Laurent J, Dumont C, Labrie F (February 1983). “Comparative study of central dopaminergic properties of RU 29717 (N-propyl-9-oxaergoline) and pergolide”. European Journal of Pharmacology. 87 (2–3): 183–189. doi:10.1016/0014-2999(83)90328-x. PMID 6857756. The relatively low affinity of pergolide for 5-HT receptors compared to that of RU 29717 is in keeping with the lack of biochemical evidence of altered 5-HT function (Fuller et al., 1979). It has been observed that RU 29717 induced short-lasting head-twitches in mice (results not shown). This result, favouring a 5-HT agonist property could be of value for its potential therapeutic interest (Silbergeld and Hruska, 1979).
  2. ^ a b WO 1985004582, Horn AS, ”Novel dopamine agonists”, assigned to Nelson Research and Development Co. 
  3. ^ Hazelhoff B, De Vries JB, Dijkstra D, Mulder TB, Timmermans PB, Wynberg H, et al. (May 1986). “Neuropharmacological profile of a new series of dopamine agonists: N-n-propyl-hexahydronaphthoxazines”. European Journal of Pharmacology. 124 (1–2): 93–106. doi:10.1016/0014-2999(86)90128-7. PMID 3720849.
  4. ^ Halberstadt AL, Geyer MA (2018). “Effect of Hallucinogens on Unconditioned Behavior”. Behavioral Neurobiology of Psychedelic Drugs. Current Topics in Behavioral Neurosciences. Vol. 36. pp. 159–199. doi:10.1007/7854_2016_466. ISBN 978-3-662-55878-2. PMC 5787039. PMID 28224459.
  5. ^ Alexander L, Anderson D, Baxter L, Claydon M, Rucker J, Robinson ES (October 2024). “Preclinical models for evaluating psychedelics in the treatment of major depressive disorder”. British Journal of Pharmacology bph.17370. doi:10.1111/bph.17370. PMID 39467003.
  6. ^ Nedelec L, Pierdet A, Fauveau P, Euvrard C, Proulx-Ferland L, Dumont C, et al. (April 1983). “Synthesis and central dopaminergic activities of (+/-)-hexahydro-7H-indolo[3,4-gh][1,4]benzoxazine derivatives [(+/-)-9-oxaergolines]”. Journal of Medicinal Chemistry. 26 (4): 522–527. doi:10.1021/jm00358a012. PMID 6834383.