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AZD 2066 hydrate
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
AZD 2066 hydrate图片
包装:5mg
市场价:5265元

产品介绍
AZD2066hydrate是一种选择性的，具有口服活性和可透过血脑屏障的mGluR5的拮抗剂。AZD2066hydrate具有镇痛作用。
Canonical SMILESCN1C(C2=CC=NC=C2)=NN=C1O[C@@H](C3=NOC(C4=CC(Cl)=CC=C4)=C3)C.O.[1/4]
分子式C19H16ClN5O2.1/4H2O
分子量386.33
储存条件Store at -20℃
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

AZD 2066 hydrate is a selective, orally active and brain-penetrant antagonist of mGluR5. AZD 2066 hydrate has antinociception effects[1].

AZD 2066 (1-10 μM) inhibits Ca2+ response, with IC50s 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[2].AZD 2066 (1-10 μM) inhibits the oscillatory Ca2+ response which induced by bath application of DHPG, and blocks either DHPG or Quis e?ects in mGlu5/HEK cells[2].AZD 2066 (1-10 μM) has less e?ective in striatal neurons[2].

AZD 2066 (0.03-30 mg/kg; p.o.) shows discriminative effects in rats[1]. Animal Model: Male Wistar rats (weighing 240-250 g)[1]

[1]. Swedberg MDB, et, al. AZD9272 and AZD2066: selective and highly central nervous system penetrant mGluR5 antagonists characterized by their discriminative effects. J Pharmacol Exp Ther. 2014 Aug; 350(2): 212-22. [2]. Jong YJI, et, al. Location and Cell-Type-Specific Bias of Metabotropic Glutamate Receptor, mGlu 5, Negative Allosteric Modulators. ACS Chem Neurosci. 2019 Nov 20; 10(11): 4558-4570.