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77086-21-6

中文名稱 地佐環(huán)平
英文名稱 Dizocilpine
CAS 77086-21-6
分子式 C16H15N
分子量 221.3
MOL 文件 77086-21-6.mol
更新日期 2026/07/16 12:18:31
77086-21-6 結構式 77086-21-6 結構式

基本信息

中文別名
地卓西平
地佐環(huán)平
英文別名
C13737
Dizocilpine
MK-801 (Dizocilpine)
Dizocilpine USP/EP/BP
Dizocilpine free base(MK801)
(5S)-5-Methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5α,10α-imine
5H-Dibenzo[a,d]cyclohepten-5,10-imine, 10,11-dihydro-5-methyl-, (5S,10R)-
[5S,10R,(+)]-10,11-Dihydro-5-methyl-5H-dibenzo[a,d]cyclohepten-5,10-imine
[5S,10R,(+)]-10,11-Dihydro-5-methyl-5H-dibenzo[a,d]cyclohepten-5α,10α-imine
所屬類別
生物化工:GluR 拮抗劑

物理化學性質

熔點68.5-69°
比旋光度20589 +161.4° (c = 0.038 g/2 ml ethanol)
沸點320.3±11.0 °C(Predicted)
密度1.144±0.06 g/cm3(Predicted)
溶解度Soluble in DMSO > 10 mM
酸度系數(shù)(pKa)7.96±0.40(Predicted)
形態(tài)粉末
顏色White to off-white

安全數(shù)據(jù)

毒害物質數(shù)據(jù)77086-21-6(Hazardous Substances Data)
地佐環(huán)平價格(試劑級)
報價日期產品編號產品名稱CAS號包裝價格
2026/06/05HY-15084B地佐環(huán)平
Dizocilpine
77086-21-65 mg300元
2026/06/05HY-15084B地佐環(huán)平
Dizocilpine
77086-21-610 mM * 1 mLin DMSO330元
2026/06/05HY-15084B地佐環(huán)平
Dizocilpine
77086-21-610 mg480元

常見問題列表

生物活性
Dizocilpine (MK-801),一種有效的抗驚厥劑,是一種選擇性非競爭性 NMDA 受體拮抗劑,Kd 為 37.2 nM。Dizocilpine 通過與 NMDA 相關離子通道內的一個位點結合而起作用,從而阻止 Ca2+ 的流動。
靶點

Ki: 37.2 nM (NMDA receptor, in rat brain membrane)

體外研究

Dizocilpine (MK-801) progressively suppresses of current induced by NMDA. Mg 2+ (10 mM) prevents Dizocilpine from blocking the N-Me-D-Asp-induced current, even when Dizocilpine is applied for a long time in the presence of NMDA. Dizocilpine blocks NMDA-activated single-channel activity in outside-out patches.
Dizocilpine (MK-801; <500 μM) inhibits activation of microglia induced by LPS with increased Cox-2 protein expression in BV-2 cells. Dizocilpine (<500 μM) reduces microglial TNF-α output with an EC 50 of 400 μM in BV-2 cells.

體內研究

Dizocilpine (MK 801) (1 mg/kg) treatment before each METH injection reduces the extent of DA depletion by 55% in striatal of mice. Dizocilpine (MK 801) (1 mg/kg) also attenuates the effects of METH on microglial activation in striatal of mice.
Dizocilpine ((+)-MK 801) (0.05, 0.2 mg/kg, i.p.) attenuates subsequent cocaine-primed reinstatement without disruption in rats. Dizocilpine (MK 801) (0.2 mg/kg, i.p.) prior to two reactivation sessions in the home cage shows no suppression on subsequent cocaine-primed reinstatement.
Dizocilpine (0.03, 0.1, 0.3 and 1 mg/kg, i.p.) significantly increases the ambulation of mice at 0.3 and 1 mg/kg, but not at 0.03 and 0.1 mg/kg.

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