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Metergoline is an ergot-derived small molecule drug that acts as a ligand for serotonin and dopamine receptors. It functions primarily as an antagonist at various serotonin (5-HT) receptor subtypes—including 5-HT1A, 5-HT2A, 5-HT2B, 5-HT2C, and 5-HT7—and as an agonist at dopamine receptors. Its main clinical use is to inhibit prolactin secretion in conditions such as hyperprolactinemia. It has also been studied for the treatment of seasonal affective disorder and premenstrual dysphoric disorder due to its effects on monoaminergic neurotransmission[1][2][4].
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