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]
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Trade names | Contralac, Liserdol |
Other names | Methergoline; FI-6337; [(8β)-1,6-Dimethylergolin-8-yl)methyl]carbamic acid phenylmethyl ester |
Routes of administration | Oral |
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ECHA InfoCard | 100.037.881 |
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Formula | C25H29N3O2 |
Molar mass | 403.526 g·mol−1 |
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Metergoline is a ligand of various serotonin and dopamine receptors.[4][5][6][7][8]
Site | Affinity (Ki [nM]) | Efficacy (Emax [%]) | Action |
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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] |