12'-ヒドロキシ-2'-イソプロピル-5'α-イソブチルエルゴタマン-3',6',18-トリオン 化学特性,用途語,生産方法
化学的特性
Pale Yellow Solid
使用
An impurity of 2-Bromo α-Ergocriptine Mesylate (B682600).
定義
ChEBI: Ergotaman bearing hydroxy, isopropyl, and 2-methylpropyl groups at the 12', 2' and 5' positions, respectively, and oxo groups at positions 3', 6', and 18. It is a natural ergot alkaloid. Ergocryptine discussed in the literature prior to 1967, when b
ta-ergocryptine was separated from alpha-ergocryptine, is now referred to as alpha-ergocryptine.
一般的な説明
One of the biologically most important ergot alkaloids is α-ergocryptine. Its semisynthetic derivative, the so-called bromocryptine, is one of the most widely used drugs in this family (e.g., as a prolactin inhibitor or an anti-Parkinsonian)[2].
毒性学
A study describes the metabolic changes observed in a dietary subacute toxicity experiment with the ergot alkaloid α-ergocryptine in Sprague±Dawley rats. The rats were fed 0, 4, 20, 100 or 500 mg ergocryptine/kg diet for 28±32 days (equal to 0, 0.36, 1.7, 8.9 and 60 mg ergocryptine/kg body weight/day for females and 0, 0.34, 1.4, 6.6 and 44 mg ergocryptine/kg body weight/day for males). Total cholesterol and high-density lipoprotein (HDL)-cholesterol was decreased dose-dependently in females, but the ratio HDL-cholesterol/total cholesterol was only decreased at 20 mg/kg body weight. Triglycerides and glucose concentrations were decreased in the highest dose groups of both sexes. Serum urea concentrations were increased in the 20, 100 and 500 mg/kg dose groups. Insulin, glucagon and liver glycogen were increased in the highest dose group at the end of the study when the animals were allowed to eat prior to blood sampling and necropsy. Prolactin, T4 and FT4 were decreased in the 20, 100 and 500 mg/kg dose groups of both sexes. Follicle-stimulating hormone (FSH) was decreased in the 20, 100 and 500 mg/kg female dose groups and luteinizing hormone (LH) was increased in the 20, 100 and 500 mg/kg male dose groups[1].
純化方法
It crystallises with solvent of crystallisation, from acetone, *benzene or methanol. [Stadler et al. Helv Chim Acta 52 1549 1969, Beilstein 25 III/IV 964, 27 II 860.]
12'-ヒドロキシ-2'-イソプロピル-5'α-イソブチルエルゴタマン-3',6',18-トリオン 上流と下流の製品情報
原材料
準備製品