| Description | 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. |
| In vitro | 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]. |
| In vivo | 与其他D2样受体激动剂相比，Cabergoline具有较长的消除半衰期(63至109小时)，其单次给药后具有持久的临床效果，并且预期能改善慢性病患者的生活质量[1]。在轻度阶段，Cabergoline注射的雌性小鼠REM睡眠周期数显著减少，比受限制的Cabergoline注射雌性小鼠少67.3%(F(1,11)=12.892, P=0.004)，尽管在暗相期间，REM睡眠周期数减少的数量最多（减少了82.3%；F(1,11)=3.667, P=0.082）。在雄性小鼠中，Cabergoline在注射后2小时内将基线催乳激素(PRL)水平从5.8±1.3 ng/mL降低至0.08 ng/mL（减少了98.5%；F(1,6)=13.192, P=0.011）。7天恢复期后，PRL水平回升至与基线水平无显著差异的值（5.0±0.60 ng/mL；F(1,6)=0.715, P=0.43）[2]。 |
| Synonyms | FCE-21336, 卡麦角林 |
| molecular weight | 451.6 |
| Molecular formula | C26H37N5O2 |
| CAS | 81409-90-7 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | DMSO: 32 mg/mL(70.86 mM) |
| References | 1. Odaka H, et al. Cabergoline, dopamine D2 receptor agonist, prevents neuronal cell death under oxidative stress via reducing excitotoxicity. PLoS One. 2014 Jun 10;9(6):e99271. 2. Jefferson F, et al. A dopamine receptor d2-type agonist attenuates the ability of stress to alter sleep in mice. Endocrinology. 2014 Nov;155(11):4411-21. |