Cabergoline

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

卡麦角林是一种麦角衍生的多巴胺 D2 样受体激动剂。它对 D2、D3 和 5-HT2B 受体具有高亲和力（Ki 分别为 0.7、1.5 和 1.2）。卡麦角林通过使催乳素产生的垂体腺瘤水平正常化，可以快速有效地控制激素和肿瘤。卡麦角林可作为一种有效的药物D2、D3 和 5-HT2B 受体激动剂。

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.

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FCE-21336

GPCR/G Protein

Dopamine Receptor

D2|D3|5-HT2B

others

Infertility

81409-90-7

451.60

C26H37N5O2

>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

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(-20℃)

With Ice Pack

≥ 2 years