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
External links