化学性质:
规格 | 1mg |
CAS | 81409-90-7 |
别名 |
|
化学名 | (6aR,9R,10aR)-7-allyl-N-(3-(dimethylamino)propyl)-N-(ethylcarbamoyl)-4,6,6a,7,8,9,10,10a-octahydroindolo[4,3-fg]quinoline-9-carboxamide |
分子式 | C26H37N5O2 |
分子量 | 451.6 |
溶解度 | Chloroform: Slightly Soluble,Methanol: Slightly Soluble |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice |
产品描述:
IC50: 0.1 nM
Unlike other pituitary hormones, prolactin (PRL) secretion is predominantly inhibited by dopamine secreted by the hypothalamus. Cabergoline is an ergoline derivative with potent, selective and long-lasting inhibitory activity on PRL secretion acting on dopamine receptors present in pituitary lactotrophes.
In vitro: Receptor binding studies have demonstrated that cabergoline has high in vitro selectivity and affinity for the subtype D2 of the dopamine receptor. In rat anterior pituitary cells, the concentration of cabergoline required to inhibit PRL secretory activity by 50% were 0.1 nmol/l [1].
In vivo: In various animal models, cabergoline markedly reduced plasma PRL levels in vivo after single or multiple doses, and the PRL-lowering effects appeared 2 - 8 h after administration lasting for 72 h or longer. In addition, a single dose of cabergoline 0.6 mg/kg to rats, inhibited the serum levels of PRL for 6 days significantly [1].
Clinical trial: Cabergoline at doses of 0.125 - 1 mg twice a week caused a dose-dependent suppression of PRL secretion in women with hyperprolactinaemia. cabergoline was shown to be more effective than bromocriptine in inducing a complete biochemical response and clinical efficacy and was better tolerated than bromocriptine in the majority of patients [1].
特别提醒:
1. 本产品仅供科研使用。请勿用于医药、临床诊断或治疗,食品及化妆品等用途。请勿存放于普通住宅区。
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标签:Cabergoline
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