Cabergoline

Cabergoline 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 acts as a potent agonist of D2, D3 and 5-HT2B receptors. 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. The detection of apoptotic nuclear condensation suggested that Cabergoline prevents apoptotic cell death following H2O2 exposure[1].Cabergoline has a longer elimination half-life (63 to 109 h) compared with other D2-like receptor agonists, both a long-lasting clinical effect following single-dose administration. And an improvement in the quality of life of patients with chronic diseases are expected[1]. The most significant reduction in rapid eye movement (REM) sleep bout number occurred during the light phase. In which Cabergoline-injected female handled mice has 67.3% less REM sleep bouts (F (1,11) =12.892, P=0.004) than Cabergoline-injected females that are restrained, although the greatest number in reduction of REM sleep bouts occurr during the dark phase (82.3% fewer REM sleep bouts; F (1,11) =3.667, P=0.082) . In male mice, Cabergoline reduces baseline Prolactin (PRL) levels (98.5%; F (1,6) =13.192, P=0.011) from 5.8±1.3 to 0.08 ng/mL within 2 hours of injection. PRL levels return to values that are not different from baseline (5.0±0.60 ng/mL; F (1,6) =0.715, P=0.43), after a 7-day recovery period.

81409-90-7

FCE-21336

Pharmacology & Drug Discovery

>98% (HPLC)

DMSO:32 mg/mL (70.86 mM)

[H][C@@]12Cc3c[nH]c4cccc (c34) [C@@]1 ([H]) C[C@H] (CN2CC=C) C (=O) N (CCCN (C) C) C (=O) NCC

C26H37N5O2

451.6

Storage temperature: -20°C. Stability: ≥ 2 years