Cabergoline (brand names Dostinex and Cabaser), an ergot derivative, is a potent dopamine receptor agonist on D2 receptors. In vitro, rat studies show cabergoline has a direct inhibitory effect on pituitary lactotroph (prolactin) cells. It is frequently used as a first-line agent in the management of prolactinomas due to higher affinity for D2 receptor sites, less severe side effects, and more convenient dosing schedule than the older bromocriptine.

Cabergoline was invented by scientists working for the Italian drug company Farmitalia-Carlo Erba SpA in Milan in 1981/82, who were experimenting with semisynthetic derivatives of the ergot alkaloids. Farmitalia-Carlo Erba was acquired by Pharmacia in 1992, which in turn was acquired by Pfizer in 2002. The drug was approved by the FDA on December 23, 1996. It went generic in late 2005 following US patent expiration.

Farmitalia filed a patent application for Cabergoline in 1982, and U.S. Patent 4,526,892 issued in July 1985.

Although cabergoline is commonly described principally as a dopamine D₂ receptor agonist, it also possesses significant affinity for the D₃, D₄, 5-HT_1A, 5-HT_2A, 5-HT_2B, 5-HT_2C, α_2B- receptors, and moderate/low affinity for the D₁ and 5-HT₇ receptors. Cabergoline functions as an agonist at all receptors except for 5-HT₇ and α_2B-, where it acts as an antagonist.