セビメリン 塩酸塩 ヘミ水和物
セビメリン 塩酸塩 ヘミ水和物 物理性質
- 貯蔵温度 :
- -20°C
- 溶解性:
- H2O: ≥25mg/mL
- 外見 :
- 粉
- 色:
- 白から黄褐色
- InChIKey:
- ZSTLCHCDLIUXJE-MMPAUJBDSA-N
安全性情報
- リスクと安全性に関する声明
- 危険有害性情報のコード(GHS)
主な危険性 |
T |
|
|
Rフレーズ |
25 |
|
|
Sフレーズ |
45 |
|
|
RIDADR |
UN 2811 6.1 / PGIII |
|
|
WGK Germany |
3 |
|
|
絵表示(GHS) |
|
注意喚起語 |
危険 |
危険有害性情報 |
コード |
危険有害性情報 |
危険有害性クラス |
区分 |
注意喚起語 |
シンボル |
P コード |
H301 |
飲み込むと有毒 |
急性毒性、経口 |
3 |
危険 |
|
P264, P270, P301+P310, P321, P330,P405, P501 |
|
注意書き |
P301+P310 |
飲み込んだ場合:直ちに医師に連絡すること。 |
|
セビメリン 塩酸塩 ヘミ水和物 価格
もっと(2)
メーカー |
製品番号 |
製品説明 |
CAS番号 |
包装 |
価格 |
更新時間 |
購入 |
Sigma-Aldrich Japan
|
SML0007 |
セビメリン 塩酸塩 ヘミ水和物 ≥95% (HPLC, NMR)
Cevimeline hydrochloride hemihydrate ≥95% (HPLC, NMR) |
153504-70-2 |
5mg |
¥23000 |
2024-03-01 |
購入 |
Sigma-Aldrich Japan
|
SML0007 |
セビメリン 塩酸塩 ヘミ水和物 ≥95% (HPLC, NMR)
Cevimeline hydrochloride hemihydrate ≥95% (HPLC, NMR) |
153504-70-2 |
25mg |
¥88600 |
2024-03-01 |
購入 |
セビメリン 塩酸塩 ヘミ水和物 化学特性,用途語,生産方法
効能
唾液分泌促進薬, ムスカリン受容体作動薬
商品名
エボザック (第一三共); サリグレン (日本化薬)
説明
Although it was initially developed as a cognition enhancer, cevimeline was launched in
the US for the treatment of dry mouth symptoms (xerostomia) in patients with Sjogren’s
syndrome. Cevimeline is a racemic mixture of cis-oxathiolanes that can be obtained with a
three step synthesis starting from quinuclidin-3-one followed by separation from its 9-12-
fold less potent trans-diastereomer, This conformationally rigid analog of acetylcholine is a dual muscarinic M
1/M
3 agonist, selective versus M
2, M
4 and M
5 receptors. It is the fifth M,
agonist that has failed in clinical trials against Alzheimer’s disease. On the contrary, the
sialagogic effects of cevimeline caused by its stimulation of M
3 receptors in salivary and
lacrimal glands were demonstrated in randomized double-blind placebo-controlled clinical
trials (30 mg t.i.d. oral dose). Cevimeline (l-3 mg/kg i.v.) was as potent in dogs as
pilocarpine (0.1-0.3 mg/kg i.v.), the only prior drug efficacious against xerostomia
associated with Sjogren’s syndrome, but the effects of cevimeline lasted around 2-fold
longer. No cardiovascular side effects were reported with cevimeline, unlike pilocarpine
which has a 40-fold higher affinrty for the M
2 receptor. Cevimeline seems to bind
extensively to tissues (volume of distribution 6 L/kg in man) since it was found to be less
than 20% bound to human plasma proteins. It is metabolized into the cis and transsulfoxide,
a glucuronide conjugate and the N-oxide.
使用
Treatment of
cancer.
一般的な説明
Cevimeline (Evoxac) iscis-2 -methylspiro {1-azabicyclo [2.2.2] octane-3, 5' -[1,3]oxathiolane} hydrochloride, hydrate (2:1). Cevimeline has amolecular weight of 244.79 and is a white to off white crystallinepowder. It is freely soluble in alcohol, chloroform, andwater. Cevimeline is a cholinergic agonist which binds to theM3 muscarinic receptor subtype, which results in an increasesecretion of exocrine glands, such as salivary and sweatglands. Because of these effects, it was approved for use in thetreatment of dry mouth associated with Sj?gren syndrome. Bystimulating the salivary muscarinic receptors cevimeline promotessecretion thereby alleviating dry-mouth in these patients.Cevimeline is metabolized by the isozymes CYP2D6and CYP3A3 and CYP3A4. It has a half-life of 5 hours.
セビメリン 塩酸塩 ヘミ水和物 上流と下流の製品情報
原材料
準備製品
セビメリン 塩酸塩 ヘミ水和物 生産企業
Global( 97)Suppliers
153504-70-2(セビメリン 塩酸塩 ヘミ水和物)キーワード:
- 153504-70-2
- (2R,5R)-2-Methylspiro[1,3-oxathiolane-5,8'-1-azabicyclo[2.2.2]octane] hydrate dihydrochloride
- CeviMeline hydrochloride heMihydrates
- Cevimeline HCl 1/2H2o
- cis-2-Methylspiro(1,3-oxathiolane-5,3')quinuclidine hydrochloride hydrate (2:2:1)
- Unii-p81Q6V85np
- Cevimeline HCl hemihydrate
- CevimelineHCl
- Cevimelinehydrochloride
- C07772
- Cevimeline hydrochloride hemihydrate
- Spiro[1-azabicyclo[2.2.2]octane-3,5'-[1,3]oxathiolane], 2'-methyl-, hydrochloride, hydrate (2:1), cis-
- Spiro[1-azabicyclo[2.2.2]octane-3,5'-[1,3]oxathiolane], 2'-methyl-, hydrochloride, hydrate (2:2:1), (2'R,3R)-rel-
- (+/-)-cis-2-Methylspiro[1,3-oxathiolane-5,3'-quinuclidine] hydrochloride hemihydrate
- AF-102B,SNI-2011
- Cevimeline hydrochloride(AF-102B, Evoxac)
- CS-646
- Cevimeline hydrochloride hemihydrate >=95% (HPLC, NMR)
- rac,cis-Cevimeline Hydrochloride Hemihydrate
DISCONTINUED, offer C283500
- Cevimeline Hydrochloride (100 mg)
- セビメリン 塩酸塩 ヘミ水和物
- セビメリン塩酸塩水和物
- セビメリン塩酸塩水和物 (JAN)
- 塩酸セビメリン水和物
- rac-(2R*,5R*)-2-メチルスピロ[1,3-オキサチオラン-5,3′-キヌクリジン]・塩酸塩・0.5水和物