ブロモクリプチン

化学名:ブロモクリプチン

CAS番号.25614-03-3

英語名:Bromocriptine

CBNumberCB6136426

MFC32H40BrN5O5

MW654.59

MOL File25614-03-3.mol

别名

ブロモエルゴクリプチン

2-ブロモ-α-エルゴクリプチン

2-ブロモ-12'-ヒドロキシ-2'-イソプロピル-5'α-(2-メチルプロピル)エルゴタマン-3',6',18-トリオン

ブロモクリプチン物理性質

融点	215-218° (dec)
比旋光度	D20 -195° (c = 1 in methylene chloride)
沸点	891.3±65.0 °C(Predicted)
比重(密度)	1.2734 (rough estimate)
屈折率	1.6400 (estimate)
酸解離定数(Pka)	pKa 4.90±0.05(80% MCS t = RT) (Uncertain)
水溶解度	2.07mg/L(温度表記なし)
CAS データベース	25614-03-3(CAS DataBase Reference)

安全性情報

毒性

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.

危険有害性情報のコード(GHS)

ブロモクリプチン化学特性,用途語,生産方法

効能
パーキンソン病治療薬, ドパミンD2受容体作動薬, プロラクチン阻害薬
化学的特性
Crystals.
使用
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.
定義
An semisynthetic ergotamine alkaloid derivative and powerful dopamine D2 agonist. It inhibits prolactin secretion and release from the pituitary and retards tumor growth.
世界保健機関（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.
危険性
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.
作用機序
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).
臨床応用
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.
副作用
Bromocriptine has a number of undesirable side effects, even causing mental disturbances in long-term use.

ブロモクリプチン上流と下流の製品情報

ブロモクリプチン生産企業

25614-03-3, ブロモクリプチンキーワード

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ブロモクリプチン

危険有害性情報のコード(GHS)

ブロモクリプチン 化学特性,用途語,生産方法

ブロモクリプチン 上流と下流の製品情報

ブロモクリプチン 生産企業

25614-03-3, ブロモクリプチン キーワード

ブロモクリプチン化学特性,用途語,生産方法

ブロモクリプチン上流と下流の製品情報

ブロモクリプチン生産企業

25614-03-3, ブロモクリプチンキーワード