Mesulergine

Last updated
Mesulergine
Mesulergine.svg
Clinical data
Other namesCU-32085
Identifiers
  • N'-(1,6-dimethylergolin-8α-yl)-N,N-dimethylsulfamide
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
ChEBI
ChEMBL
CompTox Dashboard (EPA)
Chemical and physical data
Formula C18H26N4O2S
Molar mass 362.49 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 Yes check.svgY
  • Key:JLVHTNZNKOSCNB-YSVLISHTSA-N Yes check.svgY
 X mark.svgNYes check.svgY  (what is this?)    (verify)

Mesulergine (INN Tooltip International Nonproprietary Name) (developmental code name CU-32085) is a drug of the ergoline group which was never marketed. [1] [2]

Contents

Pharmacology

Pharmacodynamics

Mesulergine activities
Target Affinity (Ki, nM)Species
5-HT1A 195–398Human
5-HT1B 631–1,288Human
5-HT1D 1,700–>10,000Human
5-HT1E NDND
5-HT1F >10,000Human
5-HT2A 19.5–151Human
5-HT2B 1.44–3.62Human
5-HT2C 1.12–48.5Human
5-HT3 >10,000Rat
5-HT4 NDND
5-HT5A 1,000Rat
5-HT5B 1,000Rat
5-HT6 776–3,800Human
5-HT7 7.9–31.6Human
D2 8–12Rat
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 on serotonin and dopamine receptors. [7] [8] [9] Specifically, it is an agonist of dopamine D2-like receptors and serotonin 5-HT6 receptors and an antagonist of serotonin 5-HT2A, 5-HT2B, 5-HT2C, and 5-HT7 receptors. [9] [ additional citation(s) needed ] It also has affinity for the 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1F, and 5-HT5A receptors. [10] [9]

Research

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

See also

References

  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. Retrieved 25 June 2025.
  4. ↑ BindingDB https://www.bindingdb.org/rwd/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50024204&submit=repeat&energyterm=&column=KI&startPg=50&Increment=50 . Retrieved 25 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. 1 2 3 Glennon 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 from the 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.


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