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Bromerguride

Bromerguride, also known as 2-bromolisuride, is an antidopaminergic and serotonergic agent of the ergoline group which was described as having atypical antipsychotic properties but was never marketed. It was the first antidopaminergic ergoline derivative to be discovered. The pharmacodynamic actions of bromerguride are said to be "reversed" relative to its parent compound lisuride, a dopaminergic agent.

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Jul 10, 2026
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Bromerguride
Clinical data
Other names2-Bromolisuride; 2-Br-LIS; Βromolisuride; Bromuride; ZK-95451; 3-(2-Βromo-9,10-didehydro-6-methyl-8α-ergolinyl)-1,1-diethylurea
Identifiers
  • 3-[(6aR,9S)-5-bromo-7-methyl-6,6a,8,9-tetrahydro-4H-indolo[4,3-fg]quinolin-9-yl]-1,1-diethylurea
CAS Number
PubChem CID
ChemSpider
UNII
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC20H25BrN4O
Molar mass417.351 g·mol−1
3D model (JSmol)
  • CCN(CC)C(=O)N[C@@H]1CN([C@@H]2CC3=C(NC4=CC=CC(=C34)C2=C1)Br)C
  • InChI=1S/C20H25BrN4O/c1-4-25(5-2)20(26)22-12-9-14-13-7-6-8-16-18(13)15(19(21)23-16)10-17(14)24(3)11-12/h6-9,12,17,23H,4-5,10-11H2,1-3H3,(H,22,26)/t12-,17+/m0/s1
  • Key:SBHNNNRQZGYOAU-YVEFUNNKSA-N

Bromerguride (INNTooltip International Nonproprietary Name), also known as 2-bromolisuride, is an antidopaminergic and serotonergic agent of the ergoline group which was described as having atypical antipsychotic properties but was never marketed.12345 It was the first antidopaminergic ergoline derivative to be discovered.1 The pharmacodynamic actions of bromerguride are said to be "reversed" relative to its parent compound lisuride, a dopaminergic agent.6

See also

See also

References

References

  1. Wachtel H, Kehr W, Sauer G (December 1983). "Central antidopaminergic properties of 2-bromolisuride, an analogue of the ergot dopamine agonist lisuride". Life Sci. 33 (26): 2583–97. doi:10.1016/0024-3205(83)90342-9. PMID 6607392.
  2. Krause W, Sauerbrey N, Gräf KJ (1986). "Pharmacokinetics and pharmacodynamics in man of the dopamine antagonist ergot derivative, bromerguride". Eur J Clin Pharmacol. 31 (2): 165–8. doi:10.1007/BF00606653. PMID 3803415. S2CID 25185807.
  3. Fink H, Morgenstern R, Ott T (February 1991). "2-Bromolisuride, an ergot derivative, with dopamine antagonistic and serotonin agonistic properties". Pharmacol Biochem Behav. 38 (2): 321–5. doi:10.1016/0091-3057(91)90285-a. PMID 1905409. S2CID 46024181.
  4. Assié MB, Cosi C, Koek W (September 1997). "5-HT1A receptor agonist properties of the antipsychotic, nemonapride: comparison with bromerguride and clozapine". Eur J Pharmacol. 334 (2–3): 141–7. doi:10.1016/s0014-2999(97)01207-7. PMID 9369342.
  5. Löschmann PA, Horowski R, Wachtel H (1992). "Bromerguride--an ergoline derivative with atypical neuroleptic properties". Clin Neuropharmacol. 15 Suppl 1 Pt A: 263A–264A. doi:10.1097/00002826-199201001-00137. PMID 1354031. S2CID 34842719.
  6. Hilderbrand M, Hümpel M, Krause W, Täuber U (1987). "Pharmacokinetics of bromerguride, a new dopamine-antagonistic ergot derivative in rat and dog". Eur J Drug Metab Pharmacokinet. 12 (1): 31–40. doi:10.1007/BF03189859. PMID 3609071. S2CID 22838914.