C08187
Cabergoline
CAS: 81409-90-7
Molecular Formula: C26H37N5O2
C08187 - Names and Identifiers
| Name | Cabergoline |
| Synonyms | C08187 Cabaser Dostine Dostinex FCE-21336 CABERGOLINE Cabergoline (8-beta)-(2-propenyl) FCE-21336,Cabaser,Dostinex n-(3-(dimethylamino)propyl)-n-((ethylamino)carbonyl)-6-ergoline-8-carboxamid 6-allyl-n-[3-(dimethylamino)propyl]-n-(ethylcarbamoyl)ergoline-8-carboxamide (8β,10ξ)-N-[3-(dimethylamino)propyl]-N-(ethylcarbamoyl)-6-prop-2-en-1-ylergoline-8-carboxamide (8beta)-N-[3-(dimethylamino)propyl]-N-(ethylcarbamoyl)-6-(prop-2-en-1-yl)ergoline-8-carboxamide (8b)-N-[3-(Dimethylamino)propyl]-N-[(ethylamino)carbonyl]-6-(2-propen-1-yl)- ergoline-8-carboxamide |
| CAS | 81409-90-7 |
| EINECS | 200-419-0 |
| InChI | InChI=1/C26H37N5O2/c1-5-11-30-17-19(25(32)31(26(33)27-6-2)13-8-12-29(3)4)14-21-20-9-7-10-22-24(20)18(16-28-22)15-23(21)30/h5,7,9-10,16,19,21,23,28H,1,6,8,11-15,17H2,2-4H3,(H,27,33)/t19-,21?,23-/m1/s1 |
| InChIKey | KORNTPPJEAJQIU-KJXAQDMKSA-N |
C08187 - Physico-chemical Properties
| Molecular Formula | C26H37N5O2 |
| Molar Mass | 451.6 |
| Density | 1.156±0.06 g/cm3(Predicted) |
| Melting Point | 102-104°C |
| Solubility | DMSO: ≥10mg/mL |
| Appearance | powder |
| Color | White to Off-White |
| pKa | 13.05±0.46(Predicted) |
| Storage Condition | 2-8°C |
| Stability | Hygroscopic |
| Refractive Index | 1.594 |
| Physical and Chemical Properties | white crystals were obtained from diethyl ether, melting point 102-104 °c. Acute toxicity LD50 mice (mg/kg):>400 oral. |
| Use | Long-acting dopamine antagonists. For the treatment of primary or pituitary adenoma caused by high prolactin. |
C08187 - Risk and Safety
| Hazard Symbols | Xi - Irritant |
| Risk Codes | 36/37/38 - Irritating to eyes, respiratory system and skin. |
| Safety Description | S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S36/37 - Wear suitable protective clothing and gloves. |
| WGK Germany | 3 |
| RTECS | KE6167600 |
| HS Code | 2939690000 |
| Toxicity | Sol in ethyl alcohol, chloroform, DMF; slightly sol in 0.1 N HCl; very slightly sol in n-hexane. Insol in water. LD50 orally in male mice: >400 mg/kg (Brambilla) |
C08187 - Preparation solution concentration reference
| 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 |
| 5 mM | 0.044 ml | 0.221 ml | 0.443 ml |
Last Update：2024-01-02 23:10:35
C08187 - Reference Information
| dopamine agonist | Cabergoline, commonly known as Caber in the community, is a dopamine agonist, used to reduce the level of prolactin in the body. Many athletes use it to fight elevated levels of prolactin in drugs such as carcasses and Qulong. This is especially important for people who are prolactin sensitive and want to avoid the unpleasant side effects that often come from these compounds. It is not a new drug and has been in existence for 36 years since the success of the Erba Spa in Farmitalia-Carlo. Later, the drug was acquired by a company called Pharmacia. Cabergoline (trademark: Dostinex) is a long-acting dopamine antagonist, for early and late Parkinson's disease and primary and pituitary tumor caused by hyperprolactinism and inhibit physiological lactation and treatment of hyperprolactinemia related diseases. |
| function and use | cabergoline is an ergot alkaloid derivative, which is a dopamine receptor agonist, the effect was similar to that of bromocriptine. It is characterized by a strong, long-acting and selective, with a high affinity for the D2 dopamine receptor. And has a strong and lasting role in the inhibition of mammary gland secretion. This product is easy to absorb, the peak time of plasma concentration is 1~3 hours, the plasma protein binding rate is 40%, the half-life is 63~100 hours. This product is extensively metabolized by hydrolysis, mainly through bile and feces. Mainly used for Parkinson's disease, Parkinson's syndrome, hyperprolactinemia. This product can reduce the long-term use of levodopa and the emergence of the "switch phenomenon" severity, a "on" State of the time increased significantly, and reduce the need for levodopa by 18%. |
| indication | , it is used for hyperprolactinism caused by primary and pituitary adenomas; 3. Inhibition of physiological lactation and treatment of hyperprolactinemia-related diseases.|
| side effects | The most common side effects of ergocarine include: Head Pain, Nausea and Vomit, it occurred in 26, 27 and 2% of the patients who received the drug during a clinical trial, respectively. Other potential side effects include (but are not limited to) constipation, dry mouth, Abdominal Pain, Diarrhea, dizziness, fatigue, Anxiety, anorexia, malaise, depression, Sleep Initiation and Maintenance Disorders, hot flashes, palpitations, hypotension, breast pain and acne, but Nausea and Head Pain are the most prominent side effects. Many of the side effects are related to the dose of administration, and the reason for further administration is to start work at the lowest therapeutic dose. The prescribing information did not mention that death was a clear consequence of overdose, but it clearly listed hallucinations, hypotension and Nasal Congestion. Please note that patients with an overdose may need to take action to raise blood pressure. |
| drug interaction | 1. When combined with levodopa in the treatment of Parkinson's disease, it can enhance the curative effect, so it should be reduced appropriately. Second, when combined with macrolides can increase the blood concentration, and can appear signs of excessive dopamine. Three, when combined with antihypertensive drugs, can strengthen the antihypertensive effect, the dosage of antihypertensive drugs should be reduced. Four, oral hormonal contraceptives can cause amenorrhea or galactorrhea, interference effect, not combined. Five, haloperidol, methyldopa, monoamine oxidase inhibitors, methoxychlorproclamide, phenothiazines, reserpine and thiazoles can increase serum prolactin levels, interference effect, must be combined, should be appropriate to adjust the dose. Six, when combined with other ergot alkali derivatives, can make the occasional cause of hypertension, but more rare. Seven, when combined with alcohol, may reduce the tolerance of the drug, so the drug is prohibited during drinking. Eight, butyrylbenzene antipsychotic drugs or H2-receptor blocking drugs with the combination can increase the concentration of prolactin and reduce the efficacy. |
| biological activity | Cabergoline (FCE-21336) is a long-acting dopamine agonist and prolactin inhibitor. |
| Target | Value |
| D2 receptor () | 0.7 nM |
| 5-HT2 () | 1.2 nM |
| 5-HT2B () | 1.2 nM |
| D3 receptor () | 1.5 nM |
| D4 receptor () | 9 nM |
| Use | long-acting dopamine antagonist. For the treatment of primary or pituitary adenoma caused by high prolactin. |
| production method | 6-(2-propenyl) ergoline -8 β-carboxylic acid (I) and carbodiimide in tetrahydrofuran reaction, available cabergoline. |
Last Update：2024-04-09 02:00:12
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Mobile: 86+15671228036
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Product Name: Cabergoline Request for quotation
CAS: 81409-90-7
Tel: 0086-551-65418684
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Mobile: 0086 189 4982 3763
QQ: 2881500840
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CAS: 81409-90-7
Tel: 0086-551-65418684
Email: sales@tnjchem.com
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