Mesulergine

Mesulergine (INN) (developmental code name CU-32085) is a drug of the ergoline group which was never marketed.[1][2] It acts on serotonin and dopamine receptors.[3][4] 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. It also has affinity for the 5-HT1A, 5-HT1B, 5-HT1D, 5-HT1F, and 5-HT5A receptors.[5] The compound had entered clinical trials for the treatment of Parkinson's disease; however, further development was halted due to adverse histological abnormalities in rats.[6] It was also investigated for the treatment of hyperprolactinemia (high prolactin levels).[7]

Mesulergine
Clinical data
Other namesCU-32085
Identifiers
IUPAC name
  • 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
FormulaC18H26N4O2S
Molar mass362.49 g·mol−1
3D model (JSmol)
SMILES
  • O=S(=O)(N(C)C)N[C@H]2C[C@@H]3c4cccc1c4c(cn1C)C[C@H]3N(C2)C
InChI
  • 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 Y
  • Key:JLVHTNZNKOSCNB-YSVLISHTSA-N Y
 NY (what is this?)  (verify)

References
  1. J. Elks (14 November 2014). The Dictionary of Drugs: Chemical Data: Chemical Data, Structures and Bibliographies. Springer. pp. 776–. ISBN 978-1-4757-2085-3.
  2. I.K. Morton; Judith M. Hall (6 December 2012). Concise Dictionary of Pharmacological Agents: Properties and Synonyms. Springer Science & Business Media. pp. 177–. ISBN 978-94-011-4439-1.
  3. Closse A (May 1983). "[3H]Mesulergine, a selective ligand for serotonin-2 receptors". Life Sci. 32 (21): 2485–95. doi:10.1016/0024-3205(83)90375-2. PMID 6855451.
  4. 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): 101–7. doi:10.1016/0014-2999(83)90272-8. PMID 6230246.
  5. 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.
  6. Dupont E, Mikkelsen B, Jakobsen J (April 1986). "Mesulergine in early Parkinson's disease: a double blind controlled trial". J. Neurol. Neurosurg. Psychiatry. 49 (4): 390–5. doi:10.1136/jnnp.49.4.390. PMC 1028763. PMID 3517235.
  7. Bankowski BJ, Zacur HA (June 2003). "Dopamine agonist therapy for hyperprolactinemia". Clin Obstet Gynecol. 46 (2): 349–62. doi:10.1097/00003081-200306000-00013. PMID 12808385. S2CID 29368668.



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