Chemistry:RU-28251

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RU-28251, also known as 4,α-methylene-N,N-dipropyltryptamine (4,α-methylene-DPT), is a tricyclic dopamine receptor agonist of the simplified or partial ergoline family.[1][2][3][4][5] It is a selective D2-like receptor agonist.[4] The drug inhibits prolactin secretion in animals.[4] RU-28251 was first described in the literature by 1978.[2][6]

See also

References

  1. ↑ "Structure—Activity Relationships of Dopamine Receptor Agonists". Dopamine Receptor Agonists. Boston, MA: Springer US. 1984. pp. 87–137. doi:10.1007/978-1-4757-0310-8_4. ISBN 978-1-4757-0312-2. https://link.springer.com/10.1007/978-1-4757-0310-8_4. Retrieved 1 June 2025. "Some simpler derivatives of the ergot-type compounds also demonstrate significant DA-like activity. Such compounds include the ergoline fragment 25 (RU 28251) (Euvrard et al., 1981), which has been claimed (Bach and Kornfeld, 1978) to have OA-like properties, e.g., inhibition of prolactin secretion and displacement of OA from binding sites." 
  2. ↑ 2.0 2.1 "Bicyclic and tricyclic ergoline partial structures. Rigid 3-(2-aminoethyl)pyrroles and 3- and 4-(2-aminoethyl)pyrazoles as dopamine agonists". Journal of Medicinal Chemistry 23 (5): 481–491. May 1980. doi:10.1021/jm00179a003. PMID 7189782. 
  3. ↑ "Dopaminergic activity of some simplified ergoline derivatives". Drug Development Research 1 (2): 151–161. 1981. doi:10.1002/ddr.430010208. ISSN 0272-4391. 
  4. ↑ 4.0 4.1 4.2 "Pharmacological Validation of the Two-Dopamine-Receptor Hypothesis". Clinical Pharmacology in Psychiatry. 3. 1987. 201–213. doi:10.1007/978-3-642-71288-3_24. ISBN 978-3-642-71290-6. "Table 1. Selective ligands of each dopamine receptor [...] D-2 [...] RU-28251 [...] 3.3.3 RU-28251 RU-28251, a partial ergoline containing a tricyclic ergoline ring (Fig. 5), was both a potent inhibitor of [3H]spiroperidol binding and an inhibitor of prolactin secretion (Bach et al. 1980; Euvrard et al. 1981). In addition, this agent caused contralateral rotation in lesioned rats (Bach et al. 1980). RU-28251, however, did not alter striatal adenylate cyclase activity (Euvrard et al. 1981). As with the other D-2 agonists, replacement of the n-propyl with a methyl or hydrogen resulted in decreased agonist activity." 
  5. ↑ "Chapter 3. Antipsychotic Agents and Dopamine Agonists". Annual Reports in Medicinal Chemistry. 18. Elsevier. 1983. pp. 21–30. doi:10.1016/s0065-7743(08)60758-7. ISBN 978-0-12-040518-3. https://linkinghub.elsevier.com/retrieve/pii/S0065774308607587. Retrieved 1 June 2025. "Another ergoline analogue, RU 28251 (44), is a potent agonist in the Ungerstedt rotation model.102" 
  6. ↑ Bach NJ, Kornfeld EC, "4-(Di-n-propyl)amino-1,3,4,5-tetrahydrobenz[cd]indole", U.S. patent 4,110,339, issued 29 August 1978





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