RU-28251

Last updated

RU-28251
RU-28251.svg
Clinical data
Other namesRU28251
Drug class Dopamine receptor agonist; D2-like receptor agonist; Prolactin inhibitor
ATC code
  • None
Identifiers
  • N,N-dipropyl-1,3,4,5-tetrahydrobenzo[cd]indol-4-amine
PubChem CID
ChemSpider
ChEMBL
Chemical and physical data
Formula C17H24N2
Molar mass 256.393 g·mol−1
3D model (JSmol)
  • CCCN(CCC)C1CC2=C3C(=CNC3=CC=C2)C1
  • InChI=1S/C17H24N2/c1-3-8-19(9-4-2)15-10-13-6-5-7-16-17(13)14(11-15)12-18-16/h5-7,12,15,18H,3-4,8-11H2,1-2H3
  • Key:YBHBWJNGSCDSMJ-UHFFFAOYSA-N

RU-28251 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. ↑ Kaiser C (1984). "Structure—Activity Relationships of Dopamine Receptor Agonists". Dopamine Receptor Agonists. Boston, MA: Springer US. pp. 87–137. doi:10.1007/978-1-4757-0310-8_4. ISBN   978-1-4757-0312-2 . 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. 1 2 Bach NJ, Kornfeld EC, Jones ND, Chaney MO, Dorman DE, Paschal JW, et al. (May 1980). "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. doi:10.1021/jm00179a003. PMID   7189782.
  3. ↑ Euvrard C, Ferland L, Fortin M, Oberlander C, Labrie F, Boissier JR (1981). "Dopaminergic activity of some simplified ergoline derivatives". Drug Development Research. 1 (2): 151–161. doi:10.1002/ddr.430010208. ISSN   0272-4391.
  4. 1 2 3 Goldman ME, Kebabian JW (1987). "Pharmacological validation of the two-dopamine-receptor hypothesis". Psychopharmacology Series. 3: 201–213. doi:10.1007/978-3-642-71288-3_24. PMID   2950520. 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. ↑ Paulis TD (1983). "Chapter 3. Antipsychotic Agents and Dopamine Agonists". Annual Reports in Medicinal Chemistry. Vol. 18. Elsevier. pp. 21–30. doi:10.1016/s0065-7743(08)60758-7. ISBN   978-0-12-040518-3 . Retrieved 1 June 2025. Another ergoline analogue, RU 28251 (44), is a potent agonist in the Ungerstedt rotation model.102
  6. ↑ U.S. 4,110,339,Bach NJ, Kornfeld EC,"4-(Di-n-propyl)amino-1,3,4,5-tetrahydrobenz[cd]indole",issued 29 August 1978, assigned to Eli Lilly and Co.



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