Cabergolin

Cabergoline (an ergot derivative) is a powerful dopamine receptor agonist that specifically targets D2 receptors. In bodybuilding, it is commonly used by men to manage side effects, particularly gynecomastia and sexual dysfunction, which can arise from elevated prolactin levels caused by the use of 19-nor anabolic steroids like nandrolone or trenbolone.

Prolactin secretion from the anterior pituitary is primarily regulated by inhibitory control from the hypothalamus, likely through dopamine release. Cabergoline works by binding to D2 receptors, which leads to a direct reduction in prolactin secretion by pituitary lactotrophs.

In addition to its prolactin-lowering effects, cabergoline is also used to address other dopamine-related issues, such as difficulty concentrating, attention deficit disorders, and depression. Due to its long half-life, a dosage of approximately 0.25 mg per week is typically sufficient to achieve the anti-prolactin, pro-sexual, antidepressant, and cognitive benefits of cabergoline.