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Metergoline is an ergoline (an ergot-derived compound) that works mainly as a potent antagonist at serotonin receptors, blocking both 5-HT1 and 5-HT2 subtypes, while also carrying some dopamine-agonist activity. Because it blocks serotonin so broadly, it is used as a research tool to probe serotonergic function and as a prolactin-lowering agent. It is not a stimulant or a mood booster; its character is that of a serotonin blocker.
- Potent, broad serotonin receptor blockade
- Lowers elevated prolactin
- Useful tool for serotonergic research
- Ergot-related vascular cautions
- Possible blood-pressure changes
- Mood or hormonal shifts from serotonin blockade
Mechanism
As an ergoline, metergoline interacts with several monoamine receptors, but its defining action is potent antagonism at 5-HT1 and 5-HT2 receptor families, which suppresses serotonergic signaling. Its - component, acting on -like receptors, is what lowers prolactin release from the pituitary, since dopamine normally restrains prolactin. This mixed profile makes it valuable in pharmacology for isolating serotonin's contribution to behavior and endocrine control. Being an ergot derivative, it belongs to a chemical family known for complex and sometimes problematic receptor cross-activity.
receptor fingerprint
5-HT2 receptorsantagonist
5-HT1 receptorsantagonist
-like receptorsagonist
Dosingtypical ranges, not medical advice
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Safetyrisks and cautions, not medical advice
Ergoline compounds as a class carry cautions including potential effects on blood vessels and, for some members, fibrotic changes with prolonged use, so metergoline is not a casual supplement. Blocking serotonin broadly and stimulating dopamine can affect mood, blood pressure, and hormones, and combining it with serotonergic or dopaminergic drugs is unpredictable. It should only be handled in a research or medical context. Not medical advice.
Subjective profileweighing the evidence above
Not a nootropic and not something to take off-label. It is a broad serotonin blocker used to probe the serotonin system and to lower prolactin, and the ergoline class carries vascular and fibrotic cautions that make casual use a bad idea. Research or medical context only.
Resources
This entry is here for reference.
Research
- 1.Effects of various serotonin receptor subtype-selective antagonists alone and on m-chlorophenylpiperazine-induced neuroendocrine changes in rats
- 2.Ergoline derivatives: receptor affinity and selectivity
2 listed here; entry last updated August 2026
Reviews
My notesprivate to this device
FAQ
What is metergoline mainly used for?
It is used as a research tool to block serotonin receptors and as a prolactin-lowering agent thanks to its dopamine activity.
Is it a serotonin agonist or antagonist?
Primarily an antagonist; it potently blocks 5-HT1 and 5-HT2 receptors, unlike serotonergic psychedelics that activate them.
Does the ergot origin matter?
Yes; ergoline compounds carry class cautions about vascular and fibrotic effects, so it is not a casual supplement.
Adverse effects
- Ergot-related vascular cautions
- Possible blood-pressure changes
- Mood or hormonal shifts from serotonin blockade