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79712-55-3

中文名稱 他齊茶堿
英文名稱 Tazifylline
CAS 79712-55-3
分子式 C23H32N6O3S
分子量 472.6
MOL 文件 79712-55-3.mol
79712-55-3 結(jié)構(gòu)式 79712-55-3 結(jié)構(gòu)式

基本信息

中文別名
他齊茶堿
(鹵)-TAZIFYLLINE
(&PLUSMN
)-TAZIFYLLINE
英文別名
Tazifilina
Tazifylline
Tazifyllinum
Tazifylline [inn]
Tazifyllinum [latin]
Tazifilina [spanish]
79712-53-1 (Dihydrochloride)
3,7-Dihydro-7-[2-hydroxy-3-[4-[3-(phenylthio)propyl]piperazin-1-yl]propyl]-1,3-dimethyl-1H-purine-2,6-dione
1H-Purine-2,6-dione, 3,7-dihydro-7-(2-hydroxy-3-(4-(3-(phenylthio)propyl)-1-piperazinyl)propyl)-1,3-dimethyl-

物理化學(xué)性質(zhì)

沸點705.1±70.0 °C(Predicted)
密度1.34±0.1 g/cm3(Predicted)
儲存條件-20°C儲存
溶解度溶于二甲基亞砜
酸度系數(shù)(pKa)14.27±0.20(Predicted)

常見問題列表

生物活性
(±)-Tazifylline 是一種有效的,選擇性的長效組胺 H1 受體拮抗劑。
靶點

H1-receptor

體外研究

Tazifylline potently inhibits contractions evoked by stimulation of histamine H1-receptors in isolated guinea pig ilea and exhibits high affinity for these receptors in radioligand binding studies in vitro Tazifylline has much lower affinity for histamine H2-receptors, alpha- and beta-adrenoceptors, 5-hydroxytryptamine and muscarinic receptor subtypes. Tazifylline poorly inhibits the release of histamine from rat peritoneal mast cells.

體內(nèi)研究

In rats, guinea pigs and dogs the antihistaminic effect of Tazifylline is rapid in onset and long-lived. In anesthetized guinea pigs, Tazifylline markedly inhibits histamine-induced bronchoconstriction and protects conscious animals from the lethal effect of large doses of the amine. In conscious rats, Tazifylline is more potent in reducing the inflammatory effects of intradermal histamine than that evoked by anaphylactic reaction. In conscious dogs, orally administered Tazifylline inhibits histamine-induced skin inflammation for long periods of time and in anesthetized animals attenuated that portion of the histamine-evoked hypotension attributable to stimulation of H1-receptors. Large oral doses of Tazifylline does not reduce spontaneous locomotor activity in mice, nor do they produce overt symptoms of behavioral depression in conscious rats.

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