RU-28251
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| Other names | RU28251 |
| Drug class | Dopamine receptor agonist; D2-like receptor agonist; Prolactin inhibitor |
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| Chemical and physical data | |
| Formula | C17H24N2 |
| Molar mass | 256.393 g·mol−1 |
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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
[edit]- Partial ergoline
- Bay R 1531 (LY-197206)
- LY-293284
- LY-178210
- RU-27849
- RU-28306
References
[edit]- ^ 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.
- ^ a b 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.
- ^ 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.
- ^ a b c 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.
- ^ 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
- ^ 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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