タフルプロスト

危険有害性情報のコード(GHS)

• 絵表示(GHS)

  

• 注意喚起語

  Danger

• 危険有害性情報

  H302：飲み込むと有害

  H319：強い眼刺激

  H360：生殖能または胎児への悪影響のおそれ

  H370：臓器の障害

  H372：長期にわたる、または反復暴露により臓器の障 害

  H413：長期的影響により水生生物に有害のおそれ

• 注意書き

  P260：粉じん/煙/ガス/ミスト/蒸気/スプレーを吸入しないこ と。

  P264：取扱い後は皮膚をよく洗うこと。

  P264：取扱い後は手や顔をよく洗うこと。

  P270：この製品を使用する時に、飲食または喫煙をしないこ と。

  P280：保護手袋/保護衣/保護眼鏡/保護面を着用するこ と。

  P301+P312：飲み込んだ場合：気分が悪い時は医師に連絡する こと。

  P305+P351+P338：眼に入った場合：水で数分間注意深く洗うこと。次にコ ンタクトレンズを着用していて容易に外せる場合は外す こと。その後も洗浄を続けること。

  P307+P311：暴露した場合：医師に連絡すること。

  P314：気分が悪い時は、医師の診断/手当てを受けること。

  P321：特別な処置が必要である（このラベルの．．． を見よ）。

  P330：口をすすぐこと。

  P405：施錠して保管すること。

  P501：内容物/容器を．．．に廃棄すること。

タフルプロスト 化学特性,用途語,生産方法

• 効能

  抗緑内障薬, プロスタグランジンF受容体作動薬

• 商品名

  タプロス (参天製薬)

• 説明

  Glaucoma is second only to cataracts as a causative factor of blindness. By 2010, it is estimated that approximately 60 million people worldwide will be afflicted by glaucoma, so effective treatments should garner a large market. PG analogs have been widely used for lowering IOP by increasing uveoscleral outflow through agonism of the prostanoid FP receptor, and currently marketed versions include latanoprost, unoprostone isopropyl ester, bimatoprost, and travoprost. Compared to the carboxylic acid of latanaprost (K_i=4.7 nM), the carboxylic acid of tafluprost displayed a 10-fold greater affinity for the prostanoid FP receptor (K_i=0.4 nM). The synthesis of tafluprost begins with a Wittig condensation of the protected bicyclic lactone carbaldehyde with a dimethyl phosphonate ketone derivative.
  Compared to the carboxylic acid of latanaprost (Ki 4.7 nM), the carboxylic acid of tafluprost displayed a 10-fold greater affinity for the prostanoid FP receptor (Ki 0.4 nM). The synthesis of tafluprost begins with a Wittig condensation of the protected bicyclic lactone carbaldehyde with a dimethyl phosphonate ketone derivative. The bottom appendage is then completed by the fluorination of the ketone with morpholino-sulfur trifluoride. Hydrolysis of the benzoate ester protecting group liberates the hydroxy group, and reduction of the lactone is accomplished with aluminum hydride to generate the lactol. Condensation of this intermediate with the phosphonium salt of the acid side chain generates the free acid, or active ingredient, which is subsequently esterified with 2-iodopropane in the presence of DBU. .

• 使用

  Tafluprost is a novel prostanoid used in the treatment of glaucoma and is the first prostanoid to be released in a preservative free-formula.

• 定義

  ChEBI: Tafluprost is a prostaglandin Falpha that is prostaglandin F2alpha in which the carboxylic acid function has been converted to the corresponding isopropyl ester and the 3-hydroxy-1-octenyl side-chain is substituted by 3,3-difluoro-4-phenoxybut-1-enyl. Used for treatment of elevated intraocular pressure in patients with open-angle glaucoma or ocular hypertension. It has a role as a prostaglandin receptor agonist. It is a prostaglandins Falpha, an organofluorine compound and an isopropyl ester. It is functionally related to a prostaglandin F2alpha.

• Mode of action

  Tafluprost(209860-87-7) is a Prostaglandin Analog. The mechanism of action of tafluprost is as a Prostaglandin Receptor Agonist. It is believed that prostanoid FP-receptor agonists such as tafluprost reduce IOP by increasing the uveoscleral outflow of aqueous humor. There is some evidence that tafluprost may lower IOP by interaction with the EP3 receptor.
  DB08819

タフルプロスト 生産企業

Global(263)Suppliers

タフルプロスト スペクトルデータ(¹HNMR)

209860-87-7, タフルプロスト キーワード