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1394-48-5

中文名稱 關(guān)附甲素
英文名稱 Guan-fu base A
CAS 1394-48-5
分子式 C24H31NO6
分子量 429.51
MOL 文件 1394-48-5.mol
更新日期 2024/12/16 10:53:14
1394-48-5 結(jié)構(gòu)式 1394-48-5 結(jié)構(gòu)式

基本信息

中文別名
關(guān)附素A
關(guān)附甲素
關(guān)白附子甲素
關(guān)附甲素對(duì)照品
關(guān)附甲素標(biāo)準(zhǔn)品
鹽酸關(guān)附甲素標(biāo)準(zhǔn)品
關(guān)附甲素,關(guān)白附子甲素
鹽酸關(guān)附甲素,關(guān)白附子甲素
英文別名
Acehytisine
Guan-fu base A
Kwan-fu base A
Guan-fu base A USP/EP/BP
(2α,11α,13R)-Hetisan-2,11,13,14-tetrol 2,11-diacetate
Hetisan-2,11,13,14-tetrol,2,13-diacetate, (2a,11a,13R)-
Hetisan-2,11,13,14-tetrol, 2,13-diacetate, (2α,11α,13R)-
(2alpha,11alpha,13R)-Hetisan-2,11,13,14-tetrol 2,13-diacetate
所屬類別
生物化工:中草藥成分

物理化學(xué)性質(zhì)

外觀性狀白色結(jié)晶,可溶于甲醇、乙醇、DMSO等有機(jī)溶劑,來(lái)源于毛茛科植物黃花烏頭的塊根(關(guān)白附)。
沸點(diǎn)541.5±50.0 °C(Predicted)
密度1.43±0.1 g/cm3(Predicted)
儲(chǔ)存條件4°C, away from moisture and light
酸度系數(shù)(pKa)12.97±0.70(Predicted)
形態(tài)Solid
顏色White to off-white

應(yīng)用領(lǐng)域

用途1
關(guān)附甲素具有抗心律失常的作用。

常見(jiàn)問(wèn)題列表

概述
關(guān)附甲素是中藥毛茛科黃花烏頭中的主要活性物質(zhì)之一。臨床前藥理研究表明:鹽酸關(guān)附甲素可對(duì)抗高鈣、結(jié)扎冠狀動(dòng)脈及烏頭堿誘發(fā)的室性心動(dòng)過(guò)速和心室顫動(dòng),并可對(duì)抗乙酰膽堿誘發(fā)的心房撲動(dòng)和心房顫動(dòng);可濃度依賴性降低對(duì)心肌快反應(yīng)動(dòng)作電位的Vmax。
生物活性
Guanfu base A 是一種從 Aconitum coreanum 中分離的抗心律失常的生物堿,是一種有效的非競(jìng)爭(zhēng)性 CYP2D6 抑制劑,對(duì)人肝微粒體 (HLM) 的 Ki 為 1.20 μM,對(duì)人重組體 (rCYP2D6) 的 Ki 為 0.37 μM。Guanfu base A 也是 CYP2D 的有效競(jìng)爭(zhēng)抑制劑,對(duì)猴子和狗的微粒體的 Ki 分別為 0.38 μM,2.4 μM。Guanfu base A 還能抑制 HERG 通道電流。
靶點(diǎn)

CYP2D6; HERG channel

體外研究

Guanfu base A has no inhibitory activity on mouse or rat CYP2Ds. Guanfu base A does not exhibit any inhibition activity on human recombinant CYP1A2, 2A6, 2C8, 2C19, 3A4, or 3A5, but shows slight inhibition of 2B6 and 2E1.
Guanfu base A is a potent inhibitor of CYP2D6, with an IC 50 recorded at ~0.46 μM in HLM (Dextromethorphan 5 μM) and 0.12 μM in rCYP2D6 (Bufuralol 5 μM).
The effects of Guanfu base A is investigated in human embryonic kidney 293 (HEK293) cells transiently transfected with HERG complementary DNA using a whole-cell patch clamp technique. Guanfu base A inhibits HERG channel current in concentration-, voltage-, and time-dependent manners with an IC 50 of 1.64 mM. Guanfu base A shifts the activation curve in a negative direction and accelerated channel inactivation but shows no effect on the inactivation curve.

體內(nèi)研究

Beagle dogs treated intravenously with Dextromethorphan (2 mg/mL) after pretreatment with Guanfu base A injection shows reduced CYP2D metabolic activity, with the C max of dextrorphan being one-third that of the saline-treated group and area under the plasma concentration-time curve half that of the saline-treated group.

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