Bromocriptine
![Bromocriptine Structure](CAS/GIF/25614-03-3.gif)
- CAS No.
- 25614-03-3
- Chemical Name:
- Bromocriptine
- Synonyms
- Parlodel;bromoergocryptine;BROMOCRITINE;bromocryptine;2-bromo-ergocryptin;Kripton;SAN 15-754;bromocriptin;,6’,18-trione;BROMOCRIPTINE
- CBNumber:
- CB6136426
- Molecular Formula:
- C32H40BrN5O5
- Molecular Weight:
- 654.59
- MOL File:
- 25614-03-3.mol
- Modify Date:
- 2024/5/15 13:45:27
Melting point | 215-218° (dec) |
---|---|
alpha | D20 -195° (c = 1 in methylene chloride) |
Boiling point | 891.3±65.0 °C(Predicted) |
Density | 1.2734 (rough estimate) |
refractive index | 1.6400 (estimate) |
pka | pKa 4.90±0.05(80% MCS t = RT) (Uncertain) |
Water Solubility | 2.07mg/L(temperature not stated) |
CAS DataBase Reference | 25614-03-3(CAS DataBase Reference) |
SAFETY
Risk and Safety Statements
Symbol(GHS) | ![]() ![]() GHS07,GHS08 |
---|---|
Signal word | Warning |
Hazard statements | H361-H362-H302 |
Precautionary statements | P201-P202-P281-P308+P313-P405-P501-P264-P270-P301+P312-P330-P501-P201-P260-P263-P264-P270-P308+P313 |
Toxicity | An ergot alkaloid derivative that exhibits potent dopamine agonist properties, particularly at D2 dopamine receptors. Bromocriptine, like dopamine, inhibits prolactin release from the pituitary and so is used in endocrine disorders, such as hyperprolactinemia. It is also used in the treatment of Parkinson’s disease. A large “first-pass” effect is seen with bromocriptine, and peak concentrations occur about 1.5-3 h after ingestion, with a half-life of about 3 h. Nausea, vomiting, and orthostatic hypotension are among the acute adverse effects. Long-term use has been associated with dyskinesias, constipation, psychoses, digital spasm, and erythromelalgia. The LD50 in rabbits exceeds 1 g/kg, p.o., and 12 mg/kg, i.v. |
Bromocriptine Chemical Properties,Uses,Production
Chemical Properties
Crystals.
Uses
Bromocriptine, a dopaminomimetic that is a dopamine D2 receptor agonist, possesses expressed antiparkinsonian activity. It is used for treating all phases of idiopathic and postencephalic Parkinsonism.
Definition
An semisynthetic ergotamine alkaloid derivative and powerful dopamine D2 agonist. It inhibits prolactin secretion and release from the pituitary and retards tumor growth.
World Health Organization (WHO)
Bromocriptine, a semisynthetic ergot alkaloid derivative and prolactin inhibitor was introduced into medicine in 1976. It is used in the prevention of lactation, but because of the risk of rebound effect and since only 10% of women benefit therapeutically from such intervention, the United States Food and Drug Administration has requested manufacturers to no longer indicate preparations containing bromocriptine for this purpose. The World Health Organization is not aware of similar action having been taken elsewhere.
Hazard
Poison; teratogen; developmental abnor- malities of the respiratory system,musculoskeletal system, rogenital system, craniofacial area, and body wall; teratogen; mutagen; questionable car- cinogen; tumorigen; causes nausea, vomiting, orthostatic hypotension; constipation, dyskinesias, psychoses, digital spasm, erythromelalgia.
Mechanism of action
Bromocriptine is absorbed after oral administration, but approximately 90% of a dose undergoes extensive first-pass hepatic metabolism, with the remainder hydrolyzed in the liver to inactive metabolites that are eliminated mostly in the bile. The half-life is relatively short (~3 hours).
Clinical Use
Bromocriptine is an ergot peptide derivative that is a partial agonist at D1-type and a full agonist at D2-type postsynaptic dopamine receptors, usually given in combination with levodopa therapy. It was the first direct dopamine receptor agonist used in treatment of Parkinson's disease after its development as an inhibitor of prolactin release (via activation of anterior pituitary D2 receptors). At low doses (typically 1–5 mg/day), bromocriptine is an effective prolactin inhibitor, and at higher doses (typically 10–20 mg/day), the antiparkinsonism and mood-elevating effects of bromocriptine become apparent.
Side effects
Bromocriptine has a number of undesirable side effects, even causing mental disturbances in long-term use.
Bromocriptine Preparation Products And Raw materials
Supplier | Tel | Country | ProdList | Advantage | Inquiry |
---|---|---|---|---|---|
CLEARSYNTH LABS LTD. | +91-22-45045900 | Hyderabad, India | 6351 | 58 | Inquiry |
Pharma Affiliates | 172-5066494 | Haryana, India | 6761 | 58 | Inquiry |
Pharmaffiliates Analytics and Synthetics P. Ltd | +91-172-5066494 | Haryana, India | 6773 | 58 | Inquiry |
Hebei Yanxi Chemical Co., Ltd. | +86-17531190177; +8617531190177 | China | 6011 | 58 | Inquiry |
hebei hongtan Biotechnology Co., Ltd | +86-86-1913198-3935 +8617331935328 | China | 973 | 58 | Inquiry |
career henan chemical co | +86-0371-86658258 +8613203830695 | China | 29901 | 58 | Inquiry |
Shanghai Longyu Biotechnology Co., Ltd. | +8613917842738 | China | 2534 | 58 | Inquiry |
Chongqing Chemdad Co., Ltd | +86-023-6139-8061 +86-86-13650506873 | China | 39916 | 58 | Inquiry |
Xi'an MC Biotech, Co., Ltd. | 029-89275612 +8618991951683 | China | 2255 | 58 | Inquiry |
Dorne Chemical Technology co. LTD | +86-86-13583358881 +8618560316533 | China | 3149 | 58 | Inquiry |
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