ジノプロストン 化学特性,用途語,生産方法
外観
白色~ほとんど白色, 結晶~粉末
溶解性
エタノールに溶けやすく、水に極めて溶けにくい。メタノール,エタノールに易溶。
解説
動物,ヒトの組織に広く見出されるC
20の生理活性物質の総称.PGと略記される.シクロペンタンの五員環と,C
7およびC
8からなる2本の側鎖をもつモノカルボン酸.五員環および側鎖にある酸素置換基-OH,=O,-OO-の種類によって,A,B,D,Eなどに分類される.また,ジホモ-γ-リノレン酸由来のタイプ1,アラキドン酸由来のタイプ2,エイコサペンタエン酸由来のタイプ3に分けられ,PGE
1などと添字で表される.生体内ではおもにタイプ2がつくられる.PGEは子宮収縮薬,PGF
2αは腸管運動促進薬として広く用いられる.また,Dは睡眠の誘発,Iは血小板凝集の阻止の作用がある.
用途
薬理・生理作用研究用。
効能
分娩誘発薬, プロスタグランジンE2受容体作動薬
商品名
プロスタグランジンE2 (科研製薬); プロスタグランジンE2 (科研製薬)
使用上の注意
吸湿性あり
化学的特性
White to pale yellowish-cream powder. Melting point 64-66°C, specific rotation -61°(26°C, c=1, THF). Easily hydrolyzed at pH<4 or pH>8. Soluble in chloroform, ethyl acetate, methanol, absolute ethanol and other organic solvents, slightly soluble in water.
使用
The most common and most biologically potent of mammalian prostaglandins. Isolated from sheep prostate. Oxytocic; abortifacient.
定義
ChEBI: Prostaglandin F2alpha in which the hydroxy group at position 9 has been oxidised to the corresponding ketone. Prostaglandin E2 is the most common and most biologically potent of mammalian prostagland
ns.
世界保健機関(WHO)
Dinoprostone, prostaglandin E2, was introduced into medicine in
1971 and is primarily used for cervical ripening during the induction of labour. It is
available in various formulations for oral, parenteral and vaginal administration.
Tablets, ampoules and vaginal dosage forms (tablets, pessaries, gel) remain
registered in many countries.
一般的な説明
PGE2 Dinoprostone (Prostin E2;Cervidil) is a naturally occurring prostaglandin that is administeredin a single dose of 10 mg by controlled-release(0.3 mg/hr) vaginal insert to induce cervical ripening. Use ofthis agent will potentiate the effects of oxytocin.
生物活性
Endogenous prostaglandin and primary product of arachidonic acid/cyclooxygenase pathway. Binds with high affinity to EP 1 , EP 2 , EP 3 and EP 4 receptors (K d values range between ~ 1-10 nM). Influences a wide range of processes including inflammation, smooth muscle relaxation, fertility and gastric mucosal integrity. Regulates vertebrate hematopoietic stem cell (HSC) homeostasis.
安全性プロファイル
Poison by
subcutaneous and intravenous routes.
Moderately toxic by ingestion and
intraperitoneal routes. An experimental
teratogen. Human reproductive effects by
intravenous, intraplacental, and intravaginal
routes: changes in the uterus, cervix and
vagina; termination of pregnancy; and
changes in ferthty. Experimental
reproductive effects. Mutation data
reported. When heated to decomposition it
emits acrid smoke and irritating fumes.
ジノプロストン 上流と下流の製品情報
原材料
準備製品