トリフルオロペラジン·塩酸塩 化学特性,用途語,生産方法
外観
白色～ほとんど白色粉末～結晶
効能
統合失調症治療薬, 催眠鎮静薬, ドパミンD2受容体拮抗薬
説明
Trifluoperazine (TFP) is a phenothiazine compound with anti-
adrenergic and anti-
dopaminergic actions typical of antipsychotic agents. It antagonizes adrenergic receptors, with selectivity for α
1 over the α
2 subtypes (K
is = 24, 653, 163, and 391 nM for α
1A, α
2A, α
2B, and α
2C, respectively). TFP binds with much higher affinity to the dopamine D
2-
like receptor (K
d = 0.96 nM) compared to the dopamine D
4-
like and the serotonin 5-
HT
2A receptors (K
ds = 44 and 135 nM, respectively). Furthermore, TFP antagonizes calmodulin (CaM) and alters the calcium-
binding properties of calsequestrin (CSQ). TFP has been shown to activate type-
2 ryanodine receptors independently of its CaM and CSQ activity.
化学的特性
Cream Fine Powder
使用
Trifluoperazine dihydrochloride has been used as a calmodulin
kinase antagonist in cultured
Aplysia californica neurons. Trifluoperazine dihydrochloride has also been used as a PMCA inhibitor in mouse duodenal tissues to block the transcellular active calcium flux.
一般的な説明
Trifluoperazinehydrochloride, 10-[3-(4-Methyl-1-piperazinyl)propyl-[2-(trifluoromethyl)phenothiazine dihydrochloride (Stelazine).The absorption of trifluoperazine is erratic and variable andit is widely distributed into tissues. The excretion of trifluoperazineoccurs 50% via kidneys and the other 50% isthrough enterohepatic circulation. The metabolism and druginteractions of trifluoperazine are the same as with the otherphenothiazines. Trifluoperazine does not show any specificdrug interactions. Trifluoperazine is indicated for the managementof schizophrenia and short-term treatment ofnonpsychotic anxiety.
安全性プロファイル
Poison by intravenous
and intraperitoneal routes. Moderately toxic
by ingestion. Experimental reproductive
effects. Human mutation data reported.
When heated to decomposition it emits very
toxic fumes of F-, NOx, SOx, and HCl. See
also FLUORIDES.
純化方法
Recrystallise the salt from absolute EtOH, filter the crystals, dry them in vacuo and store them in tightly stoppered bottles because it is hygroscopic. It is soluble in H2O but insoluble in *C6H6, Et2O and alkaline aqueous solution. It has UV at 258 and 307.5nm (log 4.50 and 3.50) in EtOH (neutral species). [Craig max et al. J Org Chem 22 709 1957.] It is a calmodulin inhibitor [Levene & Weiss J Parmacol Exptl Ther 208 454 1978] and is a psychotropic agent [Fowler Arzneim.-Forsch 27 866 1977]. [Beilstein 27 III/IV 1353.]
トリフルオロペラジン·塩酸塩 上流と下流の製品情報
原材料
準備製品