Cabergoline (Synonyms: FCE 21336) |
| رقم الكتالوجGC10441 |
كابيرجولين هو ناهض لمستقبلات الشقران مشتق من الدوبامين D2 وله تقارب كبير لمستقبلات D2 و D3 و 5-HT2B (Ki = 0.7 و 1.5 و 1.2 على التوالي)
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 81409-90-7
Sample solution is provided at 25 µL, 10mM.
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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].
Reference:
[1] Annamaria Colao, Gaetano Lombardi & Lucio Annunziato. Cabergoline. Exp. Opin. Pharmacother. (2000) 1(3):555-574
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Cell experiment: |
Primary cortical neurons are prepared. Cabergoline (10 µM; except for experiments of dose-dependency) is applied to cortical cells at DIV 6-7. After 24-hour Cabergoline treatment (except for examination of pretreatment time-dependency of Cabergoline), H2O2 (50 µM; except for the dose-dependency of H2O2) is added. All inhibitors and antagonists, including spiperone, U0126, SB203580, SP600125, AP5, and nifedipine are applied 20 min before Cabergoline or H2O2 addition. L-glutamate is added at DIV 7-8 for cell death induction. Cell survival rate is measured by MTT assay. After the indicated treatment with drugs is completed, culture medium is replaced with 200 µL fresh medium containing 40 µl MTT solution (2.5 mg/mL, diluted in PBS) and cells are incubated at 37°C for 1.5-2.5 hours. Then, 200 µL lysis buffer containing isopropyl alcohol is applied to each well and mixed by pipetting. Each sample is moved to a 96-well plate and its absorbance at 570 nm is measured using an iMark Micro plate leader. Cell survival rate is quantitated by absorbance measurement, because MTT (yellow) is deoxidized to formazan (violet) in proportion to mitochondrial activity[1]. |
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Animal experiment: |
Mice[2] Female and male C57BL/6J mice are used.Cabergoline is dissolved in 100% pharmasolve and then diluted with 20% β-cyclodextrin in water to yield a final concentration of 0.15-0.5 mg/mL Cabergoline. Mice received a 0.3-mg/kg ip injection of Cabergoline or vehicle. All drugs are prepared within 48 hours of experiment and stored at 4°C. Solutions are allowed to reach at room temperature before injection. |
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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. |
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| Cas No. | 81409-90-7 | SDF | |
| المرادفات | FCE 21336 | ||
| Chemical Name | (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 | ||
| Canonical SMILES | C=CCN1[C@@]2([H])[C@](C3=C4C(C2)=CNC4=CC=C3)([H])C[C@@H](C(N(C(NCC)=O)CCCN(C)C)=O)C1 | ||
| Formula | C26H37N5O2 | M.Wt | 451.6 |
| الذوبان | DMSO : 250 mg/mL (553.59 mM; Need ultrasonic) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2143 mL | 11.0717 mL | 22.1435 mL |
| 5 mM | 0.4429 mL | 2.2143 mL | 4.4287 mL |
| 10 mM | 0.2214 mL | 1.1072 mL | 2.2143 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 34 reference(s) in Google Scholar.)
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