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Metergoline

Chemical compound

Summary

Chemical compound

| Drugs.com =

| elimination_half-life =

Metergoline (, ), 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.

Pharmacology

Pharmacodynamics

Metergoline is a ligand of various serotonin and dopamine receptors.

Site	Affinity (Ki [nM])	Efficacy (Emax [%])	Action
5-HT1A	4.3	?	Antagonist
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).

References

(2000). "Index Nominum 2000: International Drug Directory". Taylor & Francis.
(21 February 2018). "Plumb's Veterinary Drug Handbook: Pocket". John Wiley & Sons.
(2 December 2008). "Small Animal Internal Medicine - E-Book". Elsevier Health Sciences.
(February 1981). "[3H]Metergoline: a new ligand of serotonin receptors in the rat brain". Journal of Neurochemistry.
(September 1992). "Agonist activity of sumatriptan and metergoline at the human 5-HT_1D beta receptor: further evidence for a role of the 5-HT_1D receptor in the action of sumatriptan". European Journal of Pharmacology.
(January 1987). "Central serotonin receptors as targets for drug research". J Med Chem.
"PDSP Database - UNC".
(June 1994). "International Union of Pharmacology classification of receptors for 5-hydroxytryptamine (Serotonin)". Pharmacological Reviews.
(1999). "Ergot".
(September 1997). "5-HT 1B/D receptor antagonists". General Pharmacology.
(November 2011). "Serotonin receptors and heart valve disease--it was meant 2B". Pharmacology & Therapeutics.
(December 1999). "Dopamine agonist therapy in hyperprolactinemia". The Journal of Reproductive Medicine.

Wikipedia Source

This article was imported from Wikipedia and is available under the Creative Commons Attribution-ShareAlike 4.0 License. Content has been adapted to SurfDoc format. Original contributors can be found on the article history page.

antipsychotics carbamates dopamine-agonists ergolines hallucinogen-antidotes prolactin-inhibitors serotonin-receptor-antagonists

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