Cabergoline (FCE-21336) is an ergot derived-dopamine D2-like receptor agonist. It has high affinity for D2, D3, and 5-HT2B receptors (Ki=0.7, 1.5, and 1.2, respectively).Cabergoline permits rapid and effective hormonal and tumor control by normalizing prolactin-producing pituitary adenomas levels.

Cabergoline(10 μM) is used to investigate its neuroprotective effects. MAP2 staining reveals that Cabergoline significantly suppresses the loss of neurons caused by H2O2 incubation. Pretreatment with Cabergoline inhibits H2O2-induced neuronal cell death in a dose-dependent manner. Cabergoline prevents apoptotic cell death following H2O2 exposure [1].

Cabergoline demonstrates a longer elimination half-life (63 to 109 hours) compared to other D2-like receptor agonists, offering prolonged clinical benefits from a single dose and potential enhancements in the quality of life for individuals with chronic conditions [1]. It notably reduces the number of rapid eye movement (REM) sleep bouts in female mice, achieving a 67.3% reduction (F(1,11)=12.892, P=0.004) in non-restrained subjects, with the most considerable decrease observed during the dark phase (82.3% reduction). In male mice, Cabergoline significantly lowers baseline Prolactin (PRL) levels by 98.5% (F(1,6)=13.192, P=0.011) to 0.08 ng/mL within two hours post-injection. PRL levels normalize to baseline (5.0±0.60 ng/mL; F(1,6)=0.715, P=0.43) following a seven-day recovery period [2].