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Mesulergine

From Wikipedia, the free encyclopedia
Chemical compound
Pharmaceutical compound
Mesulergine
Clinical data
Other namesCU-32085
Drug classDopamine agonist
Identifiers
  • N'-(1,6-dimethylergolin-8α-yl)-N,N-dimethylsulfamide
CAS Number
PubChemCID
IUPHAR/BPS
ChemSpider
UNII
ChEBI
ChEMBL
CompTox Dashboard(EPA)
Chemical and physical data
FormulaC18H26N4O2S
Molar mass362.49 g·mol−1
3D model (JSmol)
  • O=S(=O)(N(C)C)N[C@H]2C[C@@H]3c4cccc1c4c(cn1C)C[C@H]3N(C2)C
  • InChI=1S/C18H26N4O2S/c1-20(2)25(23,24)19-13-9-15-14-6-5-7-16-18(14)12(10-21(16)3)8-17(15)22(4)11-13/h5-7,10,13,15,17,19H,8-9,11H2,1-4H3/t13-,15+,17+/m0/s1 checkY
  • Key:JLVHTNZNKOSCNB-YSVLISHTSA-N checkY
 ☒NcheckY (what is this?)  (verify)

Mesulergine (INNTooltip International Nonproprietary Name) (developmental code nameCU-32085) is a drug of theergoline group which was never marketed.[1][2]

Pharmacology

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Pharmacodynamics

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Mesulergine activities
TargetAffinity (Ki, nM)Species
5-HT1A195–398Human
5-HT1B631–1,288Human
5-HT1D1,700–>10,000Human
5-HT1ENDND
5-HT1F>10,000Human
5-HT2A19.5–151Human
5-HT2B1.44–3.62Human
5-HT2C1.12–48.5Human
5-HT3>10,000Rat
5-HT4NDND
5-HT5A1,000Rat
5-HT5B1,000Rat
5-HT6776–3,800Human
5-HT77.9–31.6Human
D28–12Rat
Notes: The smaller the value, the more avidly the drug binds to the site. All proteins are human unless otherwise specified.Refs:[3][4][5][6]

Mesulergine acts onserotonin anddopamine receptors.[7][8][9] Specifically, it is anagonist of dopamineD2-like receptors and serotonin5-HT6 receptors and an antagonist of serotonin5-HT2A,5-HT2B,5-HT2C, and5-HT7 receptors.[9][additional citation(s) needed] It also hasaffinity for the5-HT1A,5-HT1B,5-HT1D,5-HT1F, and5-HT5A receptors.[10][9]

Research

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Mesulergine had entered clinical trials for the treatment ofParkinson's disease; however, further development was halted due to adversehistological abnormalities in rats.[11] It was also investigated for the treatment ofhyperprolactinemia (high prolactin levels).[12]

See also

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References

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  1. ^Elks J (14 November 2014).The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and Bibliographies. Springer. pp. 776–.ISBN 978-1-4757-2085-3.
  2. ^Morton IK, Hall JM (6 December 2012).Concise Dictionary of Pharmacological Agents: Properties and Synonyms. Springer Science & Business Media. pp. 177–.ISBN 978-94-011-4439-1.
  3. ^"Kᵢ Database".PDSP. 25 June 2025. Retrieved25 June 2025.
  4. ^BindingDBhttps://www.bindingdb.org/rwd/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50024204&submit=repeat&energyterm=&column=KI&startPg=50&Increment=50. Retrieved25 June 2025.{{cite web}}:Missing or empty|title= (help)
  5. ^Markstein R (November 1983). "Mesulergine and its 1,20-N,N-bidemethylated metabolite interact directly with D1- and D2-receptors".Eur J Pharmacol.95 (1–2):101–107.doi:10.1016/0014-2999(83)90272-8.PMID 6230246.
  6. ^Dumuis A, Bouhelal R, Sebben M, Cory R, Bockaert J (December 1988). "A nonclassical 5-hydroxytryptamine receptor positively coupled with adenylate cyclase in the central nervous system".Mol Pharmacol.34 (6):880–887.doi:10.1016/S0026-895X(25)10130-2.PMID 2849052.
  7. ^Closse A (May 1983). "[3H]Mesulergine, a selective ligand for serotonin-2 receptors".Life Sciences.32 (21):2485–2495.doi:10.1016/0024-3205(83)90375-2.PMID 6855451.
  8. ^Markstein R (November 1983). "Mesulergine and its 1,20-N,N-bidemethylated metabolite interact directly with D1- and D2-receptors".European Journal of Pharmacology.95 (1–2):101–107.doi:10.1016/0014-2999(83)90272-8.PMID 6230246.
  9. ^abcGlennon RA (January 1987). "Central serotonin receptors as targets for drug research".J Med Chem.30 (1):1–12.doi:10.1021/jm00384a001.PMID 3543362.Table II. Affinities of Selected Phenalkylamines for 5-HT1 and 5-HT2 Binding Sites
  10. ^National Institute of Mental Health. PDSD Ki Database (Internet). ChapelHill (NC): University of North Carolina. Available from:"PDSP Database - UNC". Archived fromthe original on 12 April 2021.
  11. ^Dupont E, Mikkelsen B, Jakobsen J (April 1986)."Mesulergine in early Parkinson's disease: a double blind controlled trial".Journal of Neurology, Neurosurgery, and Psychiatry.49 (4):390–395.doi:10.1136/jnnp.49.4.390.PMC 1028763.PMID 3517235.
  12. ^Bankowski BJ, Zacur HA (June 2003). "Dopamine agonist therapy for hyperprolactinemia".Clinical Obstetrics and Gynecology.46 (2):349–362.doi:10.1097/00003081-200306000-00013.PMID 12808385.S2CID 29368668.


D1-like
Agonists
PAMs
Antagonists
D2-like
Agonists
Antagonists
5-HT1
5-HT1A
5-HT1B
5-HT1D
5-HT1E
5-HT1F
5-HT2
5-HT2A
5-HT2B
5-HT2C
5-HT3–7
5-HT3
5-HT4
5-HT5A
5-HT6
5-HT7
Ergolines
(incl.lysergines)
Clavines
(6,8-dimethylergolines)
Lysergamides
(lysergic acid amides)
Ergopeptines
(peptide ergolines)
Partial ergolines
Related compounds
Natural sources
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