Metergoline
Chemical compound
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.
01Pharmacology
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). | |||
Sources and credits
This article is adapted from the Wikipedia article “Metergoline”, written by its contributors and licensed under CC BY-SA 4.0. Fathomly has changed the layout, removed citation markers, navigation and maintenance notices, and adjusted punctuation. This adapted version is shared under the same license. For references, see the original article.
Images, from Wikimedia Commons:
- Metergoline.svg by Benrr101, Public domain
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