934282-55-0
中文名稱(chēng)
AZD 2066
英文名稱(chēng)
(R)-5-(3-chlorophenyl)-3-(1-((4-Methyl-5-(pyridin-4-yl)-4H-1,2,4-triazol-3-yl)oxy)ethyl)isoxazole
CAS
934282-55-0
分子式
C19H16ClN5O2
分子量
381.82
MOL 文件
934282-55-0.mol
934282-55-0 結(jié)構(gòu)式
基本信息
中文別名
化合物 T10430 英文別名
AZD2066)AZD 2066 (AZD-2066
4-[5-[(1R)-1-[5-(3-Chlorophenyl)-3-isoxazolyl]ethoxy]-4-methyl-4H-1,2,4-triazol-3-yl]pyridine
Pyridine, 4-[5-[(1R)-1-[5-(3-chlorophenyl)-3-isoxazolyl]ethoxy]-4-methyl-4H-1,2,4-triazol-3-yl]-
(R)-5-(3-chlorophenyl)-3-(1-((4-Methyl-5-(pyridin-4-yl)-4H-1,2,4-triazol-3-yl)oxy)ethyl)isoxazole
物理化學(xué)性質(zhì)
熔點(diǎn)140-142°C
沸點(diǎn)626.3±65.0 °C(Predicted)
密度1.39±0.1 g/cm3(Predicted)
儲(chǔ)存條件-20°C Freezer, Under inert atmosphere
溶解度可溶于氯仿（輕微）、Dmso（輕微）、甲醇（輕微）
酸度系數(shù)(pKa)1.91±0.10(Predicted)
形態(tài)固體
顏色白色至灰白色
常見(jiàn)問(wèn)題列表
生物活性
AZD 2066 是一種選擇性的，具有口服活性和可透過(guò)血腦屏障的 mGluR5 的拮抗劑。AZD 2066 具有鎮(zhèn)痛作用。靶點(diǎn)
|
mGluR5
|
體外研究
AZD 2066 (1-10 μM) inhibits Ca
2+
response, with IC
50
s of 27.2±9.1, 3.56±0.52, 96.2±17.8, and 380±78.0 nM in mGlu5/HEK cells and striatal, hippocampal, and cortical cultures respectively.
AZD 2066 (1-10 μM) inhibits the oscillatory Ca
2+
response which induced by bath application of DHPG, and blocks either DHPG or Quis e?ects in mGlu5/HEK cells.
AZD 2066 (1-10 μM) has less e?ective in striatal neurons.
體內(nèi)研究
AZD 2066 (0.3-30 mg/kg; p.o.) shows discriminative effects in rats.
| Animal Model: | Male Wistar rats (weighing 240-250 g) |
| Dosage: | 0.03, 0.1, 0.3, 1, 3, 10, 30 mg/kg |
| Administration: | P.o. (60 minutes after administration) |
| Result: | Caused full and dose-dependent AZD9272-appropriate responding. |