產品描述: | Cabergoline is an ergot derived-dopamine D2-like receptor agonist that has high affinity for?D2,?D3, and?5-HT2B?receptors (Ki=0.7, 1.5, and 1.2, respectively). |
靶點: |
D3 Receptor;D2 Receptor;DopamineReceptor;5-HTReceptor;Autophagy |
體內研究: |
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. 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. After a 7-day recovery period, 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). |
參考文獻: |
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. |
溶解性: |
Soluble in DMSO |
保存條件: |
2-8℃ |
配置溶液濃度參考: |
|
1mg |
5mg |
10mg |
1 mM |
2.214 ml |
11.072 ml |
22.143 ml |
5 mM |
0.443 ml |
2.214 ml |
4.429 ml |
10 mM |
0.221 ml |
1.107 ml |
2.214 ml |
50 mM |
0.044 ml |
0.221 ml |
0.443 ml |
|
注意: |
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