Cannabaceae

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Metergoline
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
  • benzyl N-[[(6aR,9S,10aR)-4,7-dimethyl-6,6a,8,9,10,10a-hexahydroindolo[4,3-fg]quinolin-9-yl]methyl]carbamate
CAS Number
PubChem CID
IUPHAR/BPS
ChemSpider
UNII
ChEBI
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.037.881 Edit this at Wikidata
Chemical and physical data
FormulaC25H29N3O2
Molar mass403.526 g·mol−1
3D model (JSmol)
  • O=C(OCc1ccccc1)NC[C@@H]3C[C@@H]4c5cccc2c5c(cn2C)C[C@H]4N(C3)C
  • InChI=1S/C25H29N3O2/c1-27-14-18(13-26-25(29)30-16-17-7-4-3-5-8-17)11-21-20-9-6-10-22-24(20)19(12-23(21)27)15-28(22)2/h3-10,15,18,21,23H,11-14,16H2,1-2H3,(H,26,29)/t18-,21+,23+/m0/s1 checkY
  • Key:WZHJKEUHNJHDLS-QTGUNEKASA-N checkY
 ☒NcheckY (what is this?)  (verify)

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[edit]

Pharmacodynamics[edit]

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[edit]

  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.

External links[edit]

source: https://en.wikipedia.org/wiki/Liserdol

One thought on “Cannabaceae”

  1. Well, that’s interesting to know that Psilotum nudum are known as whisk ferns. Psilotum nudum is the commoner species of the two. While the P. flaccidum is a rare species and is found in the tropical islands. Both the species are usually epiphytic in habit and grow upon tree ferns. These species may also be terrestrial and grow in humus or in the crevices of the rocks.
    View the detailed Guide of Psilotum nudum: Detailed Study Of Psilotum Nudum (Whisk Fern), Classification, Anatomy, Reproduction

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