Chemistry:Mesulergine

From HandWiki

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

Pharmacology

Pharmacodynamics

Mesulergine activities
Target Affinity (Ki, nM) Species
5-HT1A 195–398 Human
5-HT1B 631–1,288 Human
5-HT1D 1,700–>10,000 Human
5-HT1E ND ND
5-HT1F >10,000 Human
5-HT2A 19.5–151 Human
5-HT2B 1.44–3.62 Human
5-HT2C 1.12–48.5 Human
5-HT3 >10,000 Rat
5-HT4 ND ND
5-HT5A 1,000 Rat
5-HT5B 1,000 Rat
5-HT6 776–3,800 Human
5-HT7 7.9–31.6 Human
D2 8–12 Rat
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. ↑ The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and Bibliographies. Springer. 14 November 2014. pp. 776–. ISBN 978-1-4757-2085-3. https://books.google.com/books?id=0vXTBwAAQBAJ&pg=PA776. 
  2. ↑ Concise Dictionary of Pharmacological Agents: Properties and Synonyms. Springer Science & Business Media. 6 December 2012. pp. 177–. ISBN 978-94-011-4439-1. https://books.google.com/books?id=tsjrCAAAQBAJ&pg=PA177. 
  3. ↑ "Kᵢ Database". 25 June 2025. https://pdspdb.unc.edu/kidb2/kidb/web/kis-results/index?KisResultsSearch%5Binput_receptors%5D=&KisResultsSearch%5Binput_sources%5D=&KisResultsSearch%5Binput_species%5D=&KisResultsSearch%5Binput_hot_ligands%5D=&KisResultsSearch%5Binput_test_ligands%5D=&KisResultsSearch%5Binput_test_ligands%5D%5B%5D=1206&KisResultsSearch%5Binput_citations%5D=&KisResultsSearch%5BsearchType%5D=&KisResultsSearch%5Bki_val_from%5D=&KisResultsSearch%5Bki_val_to%5D=&KisResultsSearch%5Bcustom_ki_val%5D=. 
  4. ↑ "Error: no |title= specified when using {{Cite web}}". https://www.bindingdb.org/rwd/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50024204&submit=repeat&energyterm=&column=KI&startPg=50&Increment=50. 
  5. ↑ "Mesulergine and its 1,20-N,N-bidemethylated metabolite interact directly with D1- and D2-receptors". Eur J Pharmacol 95 (1–2): 101–107. November 1983. doi:10.1016/0014-2999(83)90272-8. PMID 6230246. 
  6. ↑ "A nonclassical 5-hydroxytryptamine receptor positively coupled with adenylate cyclase in the central nervous system". Mol Pharmacol 34 (6): 880–887. December 1988. doi:10.1016/S0026-895X(25)10130-2. PMID 2849052. 
  7. ↑ "[3H]Mesulergine, a selective ligand for serotonin-2 receptors". Life Sciences 32 (21): 2485–2495. May 1983. doi:10.1016/0024-3205(83)90375-2. PMID 6855451. 
  8. ↑ "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. November 1983. doi:10.1016/0014-2999(83)90272-8. PMID 6230246. 
  9. ↑ 9.0 9.1 9.2 "Central serotonin receptors as targets for drug research". J Med Chem 30 (1): 1–12. January 1987. 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". http://pdsp.med.unc.edu/pdsp.php. 
  11. ↑ "Mesulergine in early Parkinson's disease: a double blind controlled trial". Journal of Neurology, Neurosurgery, and Psychiatry 49 (4): 390–395. April 1986. doi:10.1136/jnnp.49.4.390. PMID 3517235. 
  12. ↑ "Dopamine agonist therapy for hyperprolactinemia". Clinical Obstetrics and Gynecology 46 (2): 349–362. June 2003. doi:10.1097/00003081-200306000-00013. PMID 12808385. 




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