Chemistry:Mesulergine

From HandWiki
Short description: Chemical compound
Mesulergine
Mesulergine.svg
Clinical data
Other namesCU-32085
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
ChEBI
ChEMBL
Chemical and physical data
FormulaC18H26N4O2S
Molar mass362.49 g·mol−1
3D model (JSmol)
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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]

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. "[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. 
  4. "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. 
  5. 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. 
  6. "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. 
  7. "Dopamine agonist therapy for hyperprolactinemia". Clinical Obstetrics and Gynecology 46 (2): 349–362. June 2003. doi:10.1097/00003081-200306000-00013. PMID 12808385.