Chemistry:Metergoline

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Short description: Chemical compound
Metergoline
Metergoline.svg
Clinical data
Trade namesContralac, Liserdol
Other namesMethergoline; FI-6337; [(8β)-1,6-Dimethylergolin-8-yl)methyl]carbamic acid phenylmethyl ester
Routes of
administration		Oral
ATC code
Legal status
Legal status
  • In general: ℞ (Prescription only)
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
ChEBI
ChEMBL
Chemical and physical data
FormulaC25H29N3O2
Molar mass403.526 g·mol−1
3D model (JSmol)
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Metergoline (INN, BAN), also known as methergoline and sold under the brand names Contralac (veterinary) and Liserdol (clinical), is a monoaminergic medication of the ergoline group which is used as a prolactin inhibitor in the treatment of hyperprolactinemia (high prolactin levels) and to suppress lactation.[1][2][3]

Pharmacology

Pharmacodynamics

Metergoline is a ligand of various serotonin and dopamine receptors.[4][5][6][7][8]

Site Affinity (Ki [nM]) Efficacy (Emax [%]) Action
5-HT1A 4.3 ? Agonist
5-HT1B 5.2–36 ? Partial agonist
5-HT1D 0.60–11.7 ? Partial agonist
5-HT1E 776–1,122 ? ?
5-HT1F 339–341 ? ?
5-HT2A 0.12–2.3 ? Antagonist
5-HT2B 0.71–1.8 ? Antagonist
5-HT2C 0.18–1.8 ? Antagonist
5-HT3 >5,000–7,400 ? ?
5-HT4 354 ? ?
5-HT5A 630 ? ?
5-HT5B 1,000 ? ?
5-HT6 61–400 ? ?
5-HT7 6.4–6.5 ? Antagonist
D2 ? ? Agonist
Notes: All sites are human except 5-HT3 (rat/pig), 5-HT4 (pig), and 5-HT5B (rat—no human counterpart).[4]

References

  1. ↑ Index Nominum 2000: International Drug Directory. Taylor & Francis. 2000. pp. 661–. ISBN 978-3-88763-075-1. https://books.google.com/books?id=5GpcTQD_L2oC&pg=PA661. 
  2. ↑ "Metergoline". Plumb's Veterinary Drug Handbook: Pocket. John Wiley & Sons. 21 February 2018. pp. 1057–. ISBN 978-1-119-34649-4. https://books.google.com/books?id=wshQDwAAQBAJ&pg=PA1057. 
  3. ↑ "False Pregnancy, Disorders of Pregnancy and Parturition, and Mismating". Small Animal Internal Medicine - E-Book. Elsevier Health Sciences. 2 December 2008. pp. 927–. ISBN 978-0-323-06512-2. https://books.google.com/books?id=s-TXrwyo-_YC&pg=PA927. 
  4. ↑ 4.0 4.1 Cite error: Invalid <ref> tag; no text was provided for refs named PDSPKiDatabase
  5. ↑ Cite error: Invalid <ref> tag; no text was provided for refs named pmid7938165
  6. ↑ "[3H]Metergoline: a new ligand of serotonin receptors in the rat brain". Journal of Neurochemistry 36 (2): 613–626. February 1981. doi:10.1111/j.1471-4159.1981.tb01634.x. PMID 7463079. 
  7. ↑ "Agonist activity of sumatriptan and metergoline at the human 5-HT1D beta receptor: further evidence for a role of the 5-HT1D receptor in the action of sumatriptan". European Journal of Pharmacology 227 (1): 99–102. September 1992. doi:10.1016/0922-4106(92)90149-P. PMID 1330643. 
  8. ↑ Cite error: Invalid <ref> tag; no text was provided for refs named pmid10649819

External links



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