Cabergoline
- CAS No.
- 81409-90-7
- Chemical Name:
- Cabergoline
- Synonyms
- Dostinex;CG-101;cabergoline powder;Caber;C08187;Dostine;Cabaser;Sogilen;Galastop;FCE-21336
- CBNumber:
- CB0282495
- Molecular Formula:
- C26H37N5O2
- Molecular Weight:
- 451.6
- MOL File:
- 81409-90-7.mol
- Modify Date:
- 2024/6/11 18:14:38
| Melting point | 102-104°C |
|---|---|
| Density | 1.156±0.06 g/cm3(Predicted) |
| storage temp. | 2-8°C |
| solubility | DMSO: ≥10mg/mL |
| pka | 13.05±0.46(Predicted) |
| form | powder |
| color | White to Off-White |
| optical activity | [α]/D 61 to 68°, c = 0.5 in dichloromethane |
| Stability | Hygroscopic |
| InChIKey | KORNTPPJEAJQIU-KJXAQDMKSA-N |
| SMILES | [C@]12([H])C[C@H](CN(CC=C)[C@]1([H])CC1=CNC3C=CC=C2C1=3)C(=O)N(CCCN(C)C)C(=O)NCC |&1:0,3,9,r| |
| CAS DataBase Reference | 81409-90-7(CAS DataBase Reference) |
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
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|---|---|---|---|---|---|---|---|---|---|---|
| Signal word | Warning | |||||||||
| Hazard statements | H302-H315-H319-H335 | |||||||||
| Precautionary statements | P261-P264-P270-P301+P312-P302+P352-P305+P351+P338 | |||||||||
| Hazard Codes | Xi | |||||||||
| Risk Statements | 36/37/38 | |||||||||
| Safety Statements | 26-36/37 | |||||||||
| 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) | |||||||||
| NFPA 704 |
|
Cabergoline price More Price(2)
Cabergoline Chemical Properties,Uses,Production
Description
Cabergoline is a potent, selective, and long-lasting dopamine D2 receptor agonist launched in 1993 in Belgium as a prolactin inhibitor. A single 1 mg dose of cabergoline effectively prevents puerperal lactation for up to 14 days, remarkably superior to other drugs that require a daily regimen. It has a low rate of rebound breast activity and good tolerability. Cabergoline is also in clinical trials for Parkinson's disease, breast cancer, and hyperprolactinaemia.
Chemical Properties
White Crystalline Solid
Uses
Cabergoline is an ergot derivative and a dopamine D2-receptor agonist (1,2,3). It inhibits the secretion of prolactin and growth hormone.
Definition
ChEBI: An N-acylurea that is (8R)-ergoline-8-carboxamide in which the hydrogen attached to the piperidine nitrogen (position 6) is substituted by an allyl group and the hydrogens attached to the carboxamide nitrogen are substit ted by a 3-(dimethylamino)propyl group and an N-ethylcarbamoyl group. A dopamine D2 receptor agonist, cabergoline is used in the management of Parkinson's disease and of disorders associated with hyperprolactinaemia.
General Description
Cabergoline, (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 (Dostinex), is a white powder soluble inalcohol, chloroform, and N,N-dimethylformamide; slightlysoluble in acidic solutions and in n-hexane; and insoluble inwater. Following oral administration, peak plasma concentrationsare reached within 2 to 3 hours. Cabergoline ismoderately bound to plasma proteins in a concentrationindependentmanner. The absolute bioavailability of cabergolineis unknown. Cabergoline is extensively metabolizedby the liver, predominantly via hydrolysis of the acylureabond of the urea moiety. CYP450 metabolism appears to beminimal. The major metabolites identified thus far do not contribute to the therapeutic effect of cabergoline. Lessthan 4% is excreted unchanged in the urine. Fecal excretionrepresents the main route of cabergoline elimination. Thereare no reports of interactions of cabergoline with other antiparkinsonianagents. Clarithromycin may elevate theplasma concentration of cabergoline by the inhibition ofboth CYP3A4 and P-glycoprotein.Cabergoline is a potentD2 receptor agonist and is indicated for the treatment ofhyperprolactinemic disorders, either idiopathic or causedby pituitary adenomas.
Biological Activity
Selective D 2 -like dopamine receptor agonist (K i values are 0.7, 1.5, 9.0 and 165 nM for D 2 , D 3 , D 4 and D 5 receptors respectively) that also displays high affinity for several serotonin receptor subtypes (K i = 1.2-20.0 nM for 5-HT 1A , 5-HT 1D , 5-HT 2A and 5-HT 2B ). Inhibits secretion of prolactin and growth hormone and reverses levodopa-induced dyskinesias in Parkinsonian monkeys.
Cabergoline Preparation Products And Raw materials
Raw materials
1of3
chevron_rightPreparation Products
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