Trailing Arbutus – Epigaea repens

by | Dec 10, 2023 | NE Native Shrubs

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Metergoline (INNTooltip INN, BANTooltip British Approved Name), 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]

Activities of metergoline at various sites[4][5][9][10][11][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.
  2. ^ Plumb DC (21 February 2018). "Metergoline". Plumb's Veterinary Drug Handbook: Pocket. John Wiley & Sons. pp. 1057–. ISBN 978-1-119-34649-4.
  3. ^ Johson CA (2 December 2008). "False Pregnancy, Disorders of Pregnancy and Parturition, and Mismating". In Nelson RW, Couto CG (eds.). Small Animal Internal Medicine - E-Book. Elsevier Health Sciences. pp. 927–. ISBN 978-0-323-06512-2.
  4. ^ a b c "PDSP Database - UNC". pdsp.unc.edu. Archived from the original on 16 April 2021. Retrieved 15 January 2022.
  5. ^ a b Hoyer D, Clarke DE, Fozard JR, Hartig PR, Martin GR, Mylecharane EJ, et al. (June 1994). "International Union of Pharmacology classification of receptors for 5-hydroxytryptamine (Serotonin)". Pharmacological Reviews. 46 (2): 157–203. PMID 7938165.
  6. ^ Hamon M, Mallat M, Herbet A, Nelson DL, Audinot M, Pichat L, Glowinski J (February 1981). "[3H]Metergoline: a new ligand of serotonin receptors in the rat brain". Journal of Neurochemistry. 36 (2): 613–626. doi:10.1111/j.1471-4159.1981.tb01634.x. PMID 7463079. S2CID 20259621.
  7. ^ Miller KJ, King A, Demchyshyn L, Niznik H, Teitler M (September 1992). "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. doi:10.1016/0922-4106(92)90149-P. PMID 1330643.
  8. ^ a b Webster J (December 1999). "Dopamine agonist therapy in hyperprolactinemia". The Journal of Reproductive Medicine. 44 (12 Suppl): 1105–1110. PMID 10649819.
  9. ^ Pertz H, Eich E (1999). "Ergot Alkaloids and their Derivatives as Ligands for Serotoninergic, Dopaminergic, and Adrenergic Receptors" (PDF). Ergot. pp. 432–462. doi:10.1201/9780203304198-21. ISBN 9780429219764. Archived from the original (PDF) on 2021-04-16.
  10. ^ Pauwels PJ (September 1997). "5-HT 1B/D receptor antagonists". General Pharmacology. 29 (3): 293–303. doi:10.1016/s0306-3623(96)00460-0. PMID 9378233.
  11. ^ Hutcheson JD, Setola V, Roth BL, Merryman WD (November 2011). "Serotonin receptors and heart valve disease--it was meant 2B". Pharmacology & Therapeutics. 132 (2): 146–157. doi:10.1016/j.pharmthera.2011.03.008. PMC 3179857. PMID 21440001.

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